Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTK25J1)

• DTT Name: Adenosine A1 receptor (ADORA1) DTT Info
• Gene Name: ADORA1

Molecule-Related Drug & Molecule List

1 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Caffeine	DMKBJWP	Allergic rhinitis	CA08.0	Approved	[1]

14 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Rolofylline	DMSZPR3	Heart failure	BD10-BD13	Phase 3	[2]
AMP-579	DMJ4GPR	Hyperlipidaemia	5C80	Phase 2	[3]
Apaxifylline	DMQMV9F	Cognitive impairment	6D71	Phase 2	[4]
BAY 1067197	DM4JGNH	Heart failure	BD10-BD13	Phase 2	[5]
Capadenoson	DMYWO62	Atrial fibrillation	BC81.3	Phase 2	[6]
DTI-0009	DMV84OK	Atrial fibrillation	BC81.3	Phase 2	[7]
SELODENOSON	DMQM3IX	Cardiac arrhythmias	BC9Z	Phase 2	[7]
SLV320	DM867BJ	Heart failure	BD10-BD13	Phase 2	[8]
Tonapofylline	DMBH316	Acute and chronic heart failure	BD1Z	Phase 2	[9]
INO-8875	DMKNA94	Glaucoma/ocular hypertension	9C61	Phase 1/2	[10]
AST-004	DM5WMG7	Stroke	8B20	Phase 1	[11]
GS 9667	DMI319T	Hypertriglyceridemia	5C80.1	Phase 1	[12]
KF-17837	DMQ6DLZ	Parkinson disease	8A00.0	Phase 1	[13]
SCH-442416	DMQ2K1V	N. A.	N. A.	Phase 1	[14]

1 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID27387065-Compound-6	DMD4CIU	N. A.	N. A.	Patented	[15]

14 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CVT-124	DM753RT	Autoimmune diabetes	5A10	Discontinued in Phase 3	[16]
N-0861	DMNX0JH	Cardiac disease	BA00-BE2Z	Discontinued in Phase 3	[17]
Tecadenoson	DM9T6MS	Atrial fibrillation	BC81.3	Discontinued in Phase 3	[16]
BRL-61063	DMV3Y8R	Allergy	4A80-4A85	Discontinued in Phase 2	[18]
FK-352	DMHIUGT	Hypertension	BA00-BA04	Discontinued in Phase 2	[19]
FK-453	DMH3DXY	Renal failure	GB60-GB6Z	Discontinued in Phase 2	[20]
FK-838	DMS87T9	Hypertension	BA00-BA04	Discontinued in Phase 2	[21]
GW-493838	DMZ2OBD	Neuropathic pain	8E43.0	Discontinued in Phase 2	[6]
GR-79236	DM9C1LQ	Diabetic complication	5A2Y	Discontinued in Phase 1	[22]
SDZ-WAG-994	DMFLOT4	Hypertension	BA00-BA04	Discontinued in Phase 1	[23]
ARISTEROMYCIN	DMRXB74	N. A.	N. A.	Terminated	[25]
METHYLTHIOADENOSINE	DMC8J6F	Multiple sclerosis	8A40	Terminated	[26]
METRIFUDIL	DMS5CZ4	N. A.	N. A.	Terminated	[27]
ZM-241385	DMWQ38G	N. A.	N. A.	Terminated	[28]

1 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 60-6583	DMTEJV1	Myocardial ischemia	BA6Z	Preclinical	[24]

280 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(1-Phenyl-propyl)-(9-phenyl-9H-purin-6-yl)-amine	DMZU2VG	Discovery agent	N.A.	Investigative	[29]
(1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl	DM4FSTL	Discovery agent	N.A.	Investigative	[30]
(2-Chloro-9-methyl-9H-purin-6-yl)-phenyl-amine	DMCE1SU	Discovery agent	N.A.	Investigative	[29]
(9-Methyl-9H-purin-6-yl)-phenyl-amine	DMWJNFC	Discovery agent	N.A.	Investigative	[29]
(E)-8-(3-chlorostyryl)-caffeine	DMQT15Z	Discovery agent	N.A.	Investigative	[31]
(R,S)-PHPNECA	DMQO71C	Discovery agent	N.A.	Investigative	[32]
(S)-PIA	DM04BHI	Discovery agent	N.A.	Investigative	[33]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione	DMEV8G2	Discovery agent	N.A.	Investigative	[34]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione	DMKYE16	Discovery agent	N.A.	Investigative	[34]
1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione	DMZ80CT	Discovery agent	N.A.	Investigative	[34]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione	DMUL2B3	Discovery agent	N.A.	Investigative	[34]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione	DMSNK98	Discovery agent	N.A.	Investigative	[35]
1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione	DMSTH24	Discovery agent	N.A.	Investigative	[36]
1-METHYLXANTHINE	DM2WQ1E	Discovery agent	N.A.	Investigative	[34]
1-Propyl-3,7-dihydro-purine-2,6-dione	DML5J94	Discovery agent	N.A.	Investigative	[37]
1H-Imidazo[4,5-c]quinolin-4-ylamine HCl	DMME09C	Discovery agent	N.A.	Investigative	[30]
2'-Me-tecadenoson	DMY2GXT	Discovery agent	N.A.	Investigative	[38]
2,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide	DMO4FSH	Discovery agent	N.A.	Investigative	[39]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine	DMMESIU	Discovery agent	N.A.	Investigative	[40]
2,6,8-triphenyl-9H-purine	DM4IFPQ	Discovery agent	N.A.	Investigative	[41]
2,6-bis(4-tolyl)-9H-purine	DM41RZX	Discovery agent	N.A.	Investigative	[41]
2,6-dimethyl-8-ethyl-1-deazapurine	DMRZJU5	Discovery agent	N.A.	Investigative	[42]
2,6-diphenyl-1-deazapurine	DMW2VZ1	Discovery agent	N.A.	Investigative	[42]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine	DMY3C78	Discovery agent	N.A.	Investigative	[42]
2,6-diphenyl-8-ethyl-1-deazapurine	DM0C8BW	Discovery agent	N.A.	Investigative	[42]
2,6-diphenyl-8-methyl-1-deazapurine	DMI79FV	Discovery agent	N.A.	Investigative	[42]
2,6-diphenyl-8-tButyl-1-deazapurine	DM6D1BQ	Discovery agent	N.A.	Investigative	[42]
2,6-diphenyl-9H-purine	DM5SXYI	Discovery agent	N.A.	Investigative	[41]
2,6-Diphenyl-pyrimidin-4-ylamine	DM3JURW	Discovery agent	N.A.	Investigative	[43]
2,6-dphenyl-8-propyl-1-deazapurine	DM8F9KO	Discovery agent	N.A.	Investigative	[42]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline	DM0Y2P1	Discovery agent	N.A.	Investigative	[44]
2-(2''-indolylethyloxy)adenosine	DMCLIN8	Discovery agent	N.A.	Investigative	[45]
2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine	DMXGWOT	Discovery agent	N.A.	Investigative	[46]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine	DMD8Q3E	Discovery agent	N.A.	Investigative	[45]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine	DMITEND	Discovery agent	N.A.	Investigative	[45]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine	DMXRHOY	Discovery agent	N.A.	Investigative	[45]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine	DMR8PGZ	Discovery agent	N.A.	Investigative	[45]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine	DME3IN1	Discovery agent	N.A.	Investigative	[45]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine	DM6BIOP	Discovery agent	N.A.	Investigative	[45]
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine	DMFP0IW	Discovery agent	N.A.	Investigative	[45]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine	DMWA0MN	Discovery agent	N.A.	Investigative	[45]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine	DMGRC24	Discovery agent	N.A.	Investigative	[45]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine	DML39UW	Discovery agent	N.A.	Investigative	[45]
2-(3''-indolylethyloxy)adenosine	DMXRAE3	Discovery agent	N.A.	Investigative	[45]
2-(3''-pyrrolylethyloxy)adenosine	DMNCP8Y	Discovery agent	N.A.	Investigative	[45]
2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline	DM7BHYS	Discovery agent	N.A.	Investigative	[47]
2-(4-chlorophenyl)-6-phenyl-9H-purine	DMAPWNR	Discovery agent	N.A.	Investigative	[41]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline	DMTAVU5	Discovery agent	N.A.	Investigative	[47]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine	DM1C864	Discovery agent	N.A.	Investigative	[48]
2-(4-methoxyphenyl)-6-phenyl-9H-purine	DMXTHOV	Discovery agent	N.A.	Investigative	[41]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline	DMDXIN1	Discovery agent	N.A.	Investigative	[44]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine	DMSIJ17	Discovery agent	N.A.	Investigative	[48]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol	DMRBX1D	Discovery agent	N.A.	Investigative	[49]
2-(6-Cyclopentylamino-purin-9-yl)-ethanol	DMTI1VO	Discovery agent	N.A.	Investigative	[29]
2-(hex-1-ynyl)-N6-methoxyadenosine	DM7YLTS	Discovery agent	N.A.	Investigative	[48]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile	DMVN0EC	Discovery agent	N.A.	Investigative	[50]
2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile	DM53T8Q	Discovery agent	N.A.	Investigative	[50]
2-Amino-4,6-diphenyl-nicotinonitrile	DMO69TS	Discovery agent	N.A.	Investigative	[50]
2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile	DM1MOB9	Discovery agent	N.A.	Investigative	[43]
2-Amino-4,6-diphenyl-pyrimidine	DMI9YGU	Discovery agent	N.A.	Investigative	[43]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile	DMP4NHD	Discovery agent	N.A.	Investigative	[50]
2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile	DMRVTJ1	Discovery agent	N.A.	Investigative	[50]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile	DMUYTXS	Discovery agent	N.A.	Investigative	[50]
2-amino-6-phenyl-4-p-tolylnicotinonitrile	DMAXESK	Discovery agent	N.A.	Investigative	[51]
2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile	DM7M9CL	Discovery agent	N.A.	Investigative	[50]
2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide	DM320RW	Discovery agent	N.A.	Investigative	[52]
2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine	DMBSDIV	Discovery agent	N.A.	Investigative	[53]
2-chloro-2'-C-methyl-tecadenoson	DMD3ZNP	Discovery agent	N.A.	Investigative	[38]
2-chloro-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine	DMPCRLY	Discovery agent	N.A.	Investigative	[54]
2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine	DMC5OQ3	Discovery agent	N.A.	Investigative	[54]
2-chloroadenosine	DMYPQEW	Discovery agent	N.A.	Investigative	[55]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine	DM6CZAN	Discovery agent	N.A.	Investigative	[30]
2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine	DM0BHKM	Discovery agent	N.A.	Investigative	[54]
2-ethyl-4-(furan-3-yl)thieno[3,2-d]pyrimidine	DMR0IEK	Discovery agent	N.A.	Investigative	[54]
2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine	DMWFR16	Discovery agent	N.A.	Investigative	[54]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine	DMWCGE8	Discovery agent	N.A.	Investigative	[54]
2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine	DMIRSQO	Discovery agent	N.A.	Investigative	[54]
2-ethynyl-N6-methoxyadenosine	DM2D78W	Discovery agent	N.A.	Investigative	[48]
2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one	DM3AFXM	Discovery agent	N.A.	Investigative	[56]
2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine	DMIMRCH	Discovery agent	N.A.	Investigative	[56]
2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one	DM1NK2M	Discovery agent	N.A.	Investigative	[56]
2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine	DM9MIC5	Discovery agent	N.A.	Investigative	[56]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine	DMDC6XP	Discovery agent	N.A.	Investigative	[30]
2-phenyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one	DMFE2R1	Discovery agent	N.A.	Investigative	[56]
2-phenyl-2H-pyrazolo[3,4-c]quinolin-4-amine	DM5WOSM	Discovery agent	N.A.	Investigative	[56]
2-phenylpropoxyadenosine	DMZQCEP	Discovery agent	N.A.	Investigative	[45]
2-tolyl-6-phenyl-9H-purine	DM1HABS	Discovery agent	N.A.	Investigative	[41]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine	DMKC1GI	Discovery agent	N.A.	Investigative	[48]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine	DMTNQZU	Discovery agent	N.A.	Investigative	[48]
3,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide	DM4RNOE	Discovery agent	N.A.	Investigative	[39]
3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one	DMI2RH1	Discovery agent	N.A.	Investigative	[44]
3-Benzyl-7-methyl-[1,8]naphthyridin-4-ol	DMHQ467	Discovery agent	N.A.	Investigative	[57]
3-Benzyl-7-methyl-[1,8]naphthyridine-4-thiol	DM12RH3	Discovery agent	N.A.	Investigative	[57]
3-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide	DMAWC7S	Discovery agent	N.A.	Investigative	[39]
3-noradamantyl-1,3-dipropylxanthine	DMFHYAE	Discovery agent	N.A.	Investigative	[58]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[59]
4-(ethylthio)-6-phenyl-1,3,5-triazin-2-amine	DM0GCEK	Discovery agent	N.A.	Investigative	[51]
4-(furan-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine	DMY7035	Discovery agent	N.A.	Investigative	[60]
4-(furan-2-yl)thieno[3,2-d]pyrimidin-2-amine	DM7LVKP	Discovery agent	N.A.	Investigative	[52]
4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine	DMK3J8Q	Discovery agent	N.A.	Investigative	[54]
4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile	DM7X59V	Discovery agent	N.A.	Investigative	[43]
4-Bromo-N-(4-phenyl-thiazol-2-yl)-benzamide	DMJFY9Z	Discovery agent	N.A.	Investigative	[39]
4-Chloro-7-methyl-2-phenyl-[1,8]naphthyridine	DM9SVEB	Discovery agent	N.A.	Investigative	[61]
4-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide	DMVKU4L	Discovery agent	N.A.	Investigative	[39]
4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one	DM8642Z	Discovery agent	N.A.	Investigative	[62]
4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide	DMFKN1M	Discovery agent	N.A.	Investigative	[39]
4-Methyl-N-(4-phenyl-thiazol-2-yl)-benzamide	DMSF5DR	Discovery agent	N.A.	Investigative	[39]
4-Nitro-N-(4-phenyl-thiazol-2-yl)-benzamide	DMKZUWY	Discovery agent	N.A.	Investigative	[39]
4-tert-Butyl-N-(4-phenyl-thiazol-2-yl)-benzamide	DMLFZ6Q	Discovery agent	N.A.	Investigative	[39]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol	DMZLOVB	Discovery agent	N.A.	Investigative	[63]
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol	DM4TIXY	Discovery agent	N.A.	Investigative	[42]
5-Cl-5-deoxy-(+/-)-ENBA	DM109IL	Discovery agent	N.A.	Investigative	[40]
6-(furan-2-yl)-9H-purin-2-amine	DMOYCBH	Discovery agent	N.A.	Investigative	[60]
6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine	DME4GBS	Discovery agent	N.A.	Investigative	[45]
6-guanidino-2-(3''-indolylethyloxy)adenosine	DMM86PK	Discovery agent	N.A.	Investigative	[45]
7-(3,6,9,12-tetraoxatricos-22-enyl)theophylline	DMNQW2B	Discovery agent	N.A.	Investigative	[64]
7-Bromo-2-phenyl-[1,8]naphthyridin-4-ol	DMG8ZJA	Discovery agent	N.A.	Investigative	[65]
7-Chloro-2-phenyl-[1,8]naphthyridin-4-ol	DM9TZH4	Discovery agent	N.A.	Investigative	[65]
7-Dimethylamino-2-phenyl-[1,8]naphthyridin-4-ol	DMNEAU0	Discovery agent	N.A.	Investigative	[65]
7-Methyl-2-propyl-[1,8]naphthyridin-4-ol	DMGB9IE	Discovery agent	N.A.	Investigative	[65]
8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine	DMMQ79W	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-(2-butyl)-9H-adenine	DM5DCPF	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-(2-hydroxypropyl)-9H-adenine	DMKW2PE	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine	DMA258T	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-(but-3-enyl)-9H-adenine	DMXNF3V	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-(sec-butyl)-9H-adenine	DMSQPFM	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-cyclobutyl-9H-adenine	DMUTV76	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-cyclohexyl-9H-adenine	DMLVCON	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-cyclopentyl-9H-adenine	DMCK0O1	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-ethyl-9H-adenine	DM4YAD6	Discovery agent	N.A.	Investigative	[66]
8-bromo-9-isobutyl-9H-purin-6-amine	DMZF3UN	Discovery agent	N.A.	Investigative	[49]
8-Bromo-9-isopropyl-9H-adenine	DMIN9HC	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-methyl-9H-adenine	DM1DS3B	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-phenylethyl-9H-adenine	DMB7EWZ	Discovery agent	N.A.	Investigative	[66]
8-Bromo-9-propyl-9H-adenine	DMRIPU5	Discovery agent	N.A.	Investigative	[66]
8-cyclohexyl-6-(4-tolyl)-2-phenyl-9H-purine	DM79VQM	Discovery agent	N.A.	Investigative	[41]
8-cyclopentyltheophylline	DMMITAJ	Discovery agent	N.A.	Investigative	[67]
8-PHENYL THEOPHYLLINE	DMFGUCY	Discovery agent	N.A.	Investigative	[30]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione	DMHQGOC	Discovery agent	N.A.	Investigative	[68]
8-Phenyl-3,7-dihydro-purine-2,6-dione	DMJB1NI	Discovery agent	N.A.	Investigative	[68]
8-propyl-2,6-diphenyl-9H-purine	DMT6YUF	Discovery agent	N.A.	Investigative	[41]
9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine	DMDYZCH	Discovery agent	N.A.	Investigative	[52]
9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine	DM4X18V	Discovery agent	N.A.	Investigative	[52]
9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine	DMURKL9	Discovery agent	N.A.	Investigative	[52]
9-Allyl-8-bromo-9H-adenine	DM8VZIY	Discovery agent	N.A.	Investigative	[66]
9-benzyl-6-(furan-2-yl)-9H-purin-2-amine	DMO6CB7	Discovery agent	N.A.	Investigative	[52]
9-Benzyl-8-bromo-9H-adenine	DMMWGVI	Discovery agent	N.A.	Investigative	[66]
9-Cyclobutyl-9H-adenine	DM04QWX	Discovery agent	N.A.	Investigative	[66]
9-Cyclopentyl-9H-adenine	DMSGU2L	Discovery agent	N.A.	Investigative	[29]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine	DMRVS2D	Discovery agent	N.A.	Investigative	[69]
9-Ethyl-9H-adenine	DMWV8YX	Discovery agent	N.A.	Investigative	[66]
9-Isopropyl-9H-adenine	DMBQLAI	Discovery agent	N.A.	Investigative	[66]
9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine	DMO4CSP	Discovery agent	N.A.	Investigative	[70]
9-Methyl-9H-adenine	DM6DOVL	Discovery agent	N.A.	Investigative	[26]
9-Phenyl-9H-purin-6-ylamine	DM73O2A	Discovery agent	N.A.	Investigative	[29]
9-Propyl-9H-adenine	DMQTEPY	Discovery agent	N.A.	Investigative	[66]
A-987306	DMU34BK	Discovery agent	N.A.	Investigative	[71]
Anthoptilide C	DMRQVW9	Discovery agent	N.A.	Investigative	[72]
AS100	DMXZ8S9	Discovery agent	N.A.	Investigative	[73]
AS70	DM9CIJP	Discovery agent	N.A.	Investigative	[73]
AS99	DMZ7FJN	Discovery agent	N.A.	Investigative	[73]
ATL802	DMYMCQA	Discovery agent	N.A.	Investigative	[74]
Cirsimarin	DMM10TG	Discovery agent	N.A.	Investigative	[75]
CP608,039	DMTKO7P	Discovery agent	N.A.	Investigative	[76]
CPFPX	DMFE5GX	Discovery agent	N.A.	Investigative	[77]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine	DMLREDJ	Discovery agent	N.A.	Investigative	[78]
Cyclohexyl-(9-ethyl-9H-purin-6-yl)-amine	DM1F7I5	Discovery agent	N.A.	Investigative	[29]
Cyclohexyl-(9-methyl-9H-purin-6-yl)-amine	DMIUCSW	Discovery agent	N.A.	Investigative	[29]
Cyclopentyl-(9-cyclopentyl-9H-purin-6-yl)-amine	DMBDTFQ	Discovery agent	N.A.	Investigative	[29]
Cyclopentyl-(9-ethyl-9H-purin-6-yl)-amine	DMQ6BS2	Discovery agent	N.A.	Investigative	[29]
Cyclopentyl-(9-methyl-9H-purin-6-yl)-amine	DM9DHNZ	Discovery agent	N.A.	Investigative	[29]
Cyclopentyl-(9-phenyl-9H-purin-6-yl)-amine	DMBJV90	Discovery agent	N.A.	Investigative	[29]
DEPX	DM4JM50	Discovery agent	N.A.	Investigative	[79]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate	DMK4T5Y	Discovery agent	N.A.	Investigative	[9]
flavone	DMEQH6J	Discovery agent	N.A.	Investigative	[62]
FR-166124	DMPCBXT	Discovery agent	N.A.	Investigative	[80]
FR194921	DMISP7G	Discovery agent	N.A.	Investigative	[81]
GNF-PF-2224	DM26UKN	Discovery agent	N.A.	Investigative	[82]
GNF-PF-2700	DMC56YJ	Discovery agent	N.A.	Investigative	[49]
Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide	DMJOZYG	Discovery agent	N.A.	Investigative	[83]
isobutylmethylxanthine	DM46F5X	Discovery agent	N.A.	Investigative	[84]
Isoguanosine	DMAFLCJ	Discovery agent	N.A.	Investigative	[85]
KF26777	DMPBDW0	Discovery agent	N.A.	Investigative	[86]
Kuanoniamine D	DMAVM94	Discovery agent	N.A.	Investigative	[87]
L-249313	DMEK65F	Discovery agent	N.A.	Investigative	[13]
L-97-1 intravenous	DMYDR2N	Sepsis	1G40-1G41	Investigative	[88]
LUF-5417	DMUPQED	Discovery agent	N.A.	Investigative	[9]
LUF-5433	DME4O5D	Discovery agent	N.A.	Investigative	[9]
LUF-5735	DM89FBX	Discovery agent	N.A.	Investigative	[83]
LUF-5737	DMXFD3S	Discovery agent	N.A.	Investigative	[83]
LUF-5764	DMQ3VHR	Discovery agent	N.A.	Investigative	[83]
LUF-5767	DMP08QO	Discovery agent	N.A.	Investigative	[83]
LUF-5816	DMQZDMH	Discovery agent	N.A.	Investigative	[42]
LUF-5853	DMZQU90	Discovery agent	N.A.	Investigative	[43]
LUF-5956	DMG4YWM	Discovery agent	N.A.	Investigative	[41]
LUF-5957	DMJFMH9	Discovery agent	N.A.	Investigative	[41]
LUF-5962	DMR6LIE	Discovery agent	N.A.	Investigative	[41]
LUF-5978	DMCTM3L	Discovery agent	N.A.	Investigative	[42]
LUF-5980	DMGOIF5	Discovery agent	N.A.	Investigative	[42]
LUF-5981	DMHO3XL	Discovery agent	N.A.	Investigative	[42]
LUF-6258	DM0K75N	Discovery agent	N.A.	Investigative	[89]
LUF5831	DMYZGIK	Discovery agent	N.A.	Investigative	[90]
MRE 2029F20	DMUK1PA	Discovery agent	N.A.	Investigative	[91]
MRE 3008F20	DM72US0	Discovery agent	N.A.	Investigative	[76]
MRS1041	DMBXKYR	Discovery agent	N.A.	Investigative	[62]
MRS1042	DMVT865	Discovery agent	N.A.	Investigative	[62]
MRS1062	DM50QBR	Discovery agent	N.A.	Investigative	[62]
MRS1065	DMYAHU3	Discovery agent	N.A.	Investigative	[62]
MRS1084	DMKELWG	Discovery agent	N.A.	Investigative	[62]
MRS1086	DM1K5E2	Discovery agent	N.A.	Investigative	[62]
MRS1093	DM801AO	Discovery agent	N.A.	Investigative	[62]
MRS1132	DMY4C0G	Discovery agent	N.A.	Investigative	[62]
MRS1191	DM9WX3C	Discovery agent	N.A.	Investigative	[88]
MRS1523	DM4AONZ	Discovery agent	N.A.	Investigative	[88]
MRS5151	DM1GUTC	Discovery agent	N.A.	Investigative	[92]
MRS923	DMMN42V	Discovery agent	N.A.	Investigative	[62]
MRS928	DMKJ9WM	Discovery agent	N.A.	Investigative	[62]
N(6)-cyclohexyladenosine	DMHINE0	Discovery agent	N.A.	Investigative	[93]
N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine	DM1K2A4	Discovery agent	N.A.	Investigative	[78]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine	DM3C8PJ	Discovery agent	N.A.	Investigative	[78]
N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine	DMCOPR3	Discovery agent	N.A.	Investigative	[78]
N-(2,6-diphenylpyrimidin-4-yl)-2-ethylbutyramide	DMK5AU4	Discovery agent	N.A.	Investigative	[83]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide	DM6HGK4	Discovery agent	N.A.	Investigative	[83]
N-(2,6-diphenylpyrimidin-4-yl)acetamide	DMQ0DMU	Discovery agent	N.A.	Investigative	[83]
N-(2,6-diphenylpyrimidin-4-yl)benzamide	DMBW752	Discovery agent	N.A.	Investigative	[83]
N-(2,6-diphenylpyrimidin-4-yl)butyramide	DM5EF71	Discovery agent	N.A.	Investigative	[83]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide	DMWPZCS	Discovery agent	N.A.	Investigative	[83]
N-(2,6-diphenylpyrimidin-4-yl)propionamide	DM89NGE	Discovery agent	N.A.	Investigative	[83]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide	DMLTROU	Discovery agent	N.A.	Investigative	[94]
N-(4,5-diphenylpyrimidin-2-yl)acetamide	DM34R10	Discovery agent	N.A.	Investigative	[83]
N-(4,6-diphenylpyrimidin-2-yl)-2-ethylbutyramide	DMDP1QG	Discovery agent	N.A.	Investigative	[83]
N-(4,6-diphenylpyrimidin-2-yl)-3-chlorobenzamide	DMQVPK9	Discovery agent	N.A.	Investigative	[83]
N-(4,6-diphenylpyrimidin-2-yl)-3-methylbutyramide	DMOAPJ1	Discovery agent	N.A.	Investigative	[83]
N-(4,6-diphenylpyrimidin-2-yl)benzamide	DMA214F	Discovery agent	N.A.	Investigative	[83]
N-(4,6-diphenylpyrimidin-2-yl)propionamide	DMJZ2IP	Discovery agent	N.A.	Investigative	[83]
N-(4-Phenyl-thiazol-2-yl)-benzamide	DMPA91F	Discovery agent	N.A.	Investigative	[39]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide	DMTF8US	Discovery agent	N.A.	Investigative	[9]
N6-((+/-)-endo-norborn-2-yl)adenosine	DM30KXV	Discovery agent	N.A.	Investigative	[40]
N6-CYCLOPENTYLADENOSINE	DMD6AJO	Discovery agent	N.A.	Investigative	[38]
N6-methoxy-2-phenylethynyladenosine	DMDG59X	Discovery agent	N.A.	Investigative	[48]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine	DMSEL5W	Discovery agent	N.A.	Investigative	[48]
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine	DMP7246	Discovery agent	N.A.	Investigative	[48]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine	DM8LR62	Discovery agent	N.A.	Investigative	[48]
N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine	DM1KA9R	Discovery agent	N.A.	Investigative	[48]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine	DMQ5K8R	Discovery agent	N.A.	Investigative	[48]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine	DM9H3W8	Discovery agent	N.A.	Investigative	[48]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine	DMRBS50	Discovery agent	N.A.	Investigative	[48]
N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine	DM0WMKJ	Discovery agent	N.A.	Investigative	[95]
N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine	DMVNLPF	Discovery agent	N.A.	Investigative	[95]
P-IODOAMPHETAMINE	DMHLBZR	Discovery agent	N.A.	Investigative	[96]
Paeoniflorin	DMJ5TAU	Parkinson disease	8A00.0	Investigative	[88]
PD-115199	DMQ4LRZ	Discovery agent	N.A.	Investigative	[97]
PD-81723	DM5SYTW	Discovery agent	N.A.	Investigative	[98]
PENECA	DMIDSJ9	Discovery agent	N.A.	Investigative	[32]
Pentanoic acid (4,6-diphenylpyrimidin-2-yl)amide	DM3S790	Discovery agent	N.A.	Investigative	[83]
Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol	DMDV1SN	Discovery agent	N.A.	Investigative	[99]
Phenyl-(9-phenyl-9H-purin-6-yl)-amine	DMIQ18W	Discovery agent	N.A.	Investigative	[29]
PSB-0788	DM0FKV9	Discovery agent	N.A.	Investigative	[100]
PSB-10	DMXDWO7	Discovery agent	N.A.	Investigative	[101]
PSB-11	DMGK2PC	Discovery agent	N.A.	Investigative	[101]
PSB-1115	DMOH2VC	Discovery agent	N.A.	Investigative	[100]
PSB-601	DMBIK7D	Discovery agent	N.A.	Investigative	[100]
PSB36	DMBGM1E	Discovery agent	N.A.	Investigative	[102]
PSB603	DM6QERS	Discovery agent	N.A.	Investigative	[100]
R-N6-(phenylisopropyl)adenosine	DM2N3BA	Discovery agent	N.A.	Investigative	[103]
sakuranetin	DMUAQYZ	Discovery agent	N.A.	Investigative	[62]
SB-298	DMU2J3K	Discovery agent	N.A.	Investigative	[100]
SCH-63390	DMAUB9F	Discovery agent	N.A.	Investigative	[104]
ST-1535	DMUTC9Z	Discovery agent	N.A.	Investigative	[70]
TCPA	DMTF4VI	Discovery agent	N.A.	Investigative	[105]
VCP-28	DMG1YZQ	Discovery agent	N.A.	Investigative	[106]
VUF-8507	DMQFWV7	Discovery agent	N.A.	Investigative	[107]
VUF5574	DMUA751	Discovery agent	N.A.	Investigative	[108]
WRC-0571	DM1U29V	Discovery agent	N.A.	Investigative	[109]
xanthine amine congener	DMGYVFD	Discovery agent	N.A.	Investigative	[84]
[3H]CCPA	DMHDGB3	Discovery agent	N.A.	Investigative	[103]
[3H]DPCPX	DM9GY7O	Discovery agent	N.A.	Investigative	[110]
[3H]HEMADO	DMEO6AH	Discovery agent	N.A.	Investigative	[111]
[3H]NECA	DMAO9SH	Discovery agent	N.A.	Investigative	[112]
[3H]OSIP339391	DM4BY5J	Discovery agent	N.A.	Investigative	[49]

References

• [1] Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.
• [2] Association between the PDE4D gene and ischaemic stroke in the Chinese Han population. Clin Sci (Lond). 2009 Aug 17;117(7):265-72.
• [3] Adenosine A1/A2a receptor agonist AMP-579 induces acute and delayed preconditioning against in vivo myocardial stunning. Am J Physiol Heart Circ Physiol. 2004 Dec;287(6):H2746-53.
• [4] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004779)
• [5] Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Current Issue vol. 111 no. 12 Celine Valant, 4614-4619.
• [6] A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008 Dec;17(12):1901-10.
• [7] Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308.
• [8] Role of matrix metalloproteinases and their tissue inhibitors as potential biomarkers of left ventricular remodelling in the athlete's heart. Clin Sci (Lond). 2009 Jul 16;117(4):157-64.
• [9] 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.
• [10] INO-8875, a highly selective A1 adenosine receptor agonist: evaluation of chronotropic, dromotropic, and hemodynamic effects in rats. J Pharmacol Exp Ther. 2013 Jan;344(1):59-67.
• [11] Adenosine A1R/A3R (Adenosine A1 and A3 Receptor) Agonist AST-004 Reduces Brain Infarction in a Nonhuman Primate Model of Stroke. Stroke. 2022 Jan;53(1):238-248.
• [12] Reduction of free fatty acids, safety, and pharmacokinetics of oral GS-9667, an A(1) adenosine receptor partial agonist. J Clin Pharmacol. 2013 Apr;53(4):385-92.
• [13] 2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic gluc... J Med Chem. 2001 Jan 18;44(2):170-9.
• [14] Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using p... J Med Chem. 2000 Nov 16;43(23):4359-62.
• [15] Carbonic anhydrase inhibitors: a review on the progress of patent literature (2011-2016).Expert Opin Ther Pat. 2016 Aug;26(8):947-56.
• [16] CV Therapeutics. Company report from CV Therapeutics, Inc. CV Therapeutics. 2009.
• [17] N-0861 selectively antagonizes adenosine A1 receptors in vivo. Eur J Pharmacol. 1992 May 27;216(1):9-16.
• [18] Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. J Med Chem. 1994 Feb 18;37(4):476-85.
• [19] Adenosine A1 receptor antagonist improves intradialytic hypotension. Kidney Int. 2006 Mar;69(5):877-83.
• [20] Cardiovascular and renal effects of blocking A1 adenosine receptors. J Cardiovasc Pharmacol. 1993 May;21(5):822-8.
• [21] An orally active adenosine A1 receptor antagonist, FK838, increases renal excretion and maintains glomerular filtration rate in furosemide-resistan... Br J Pharmacol. 2003 Aug;139(8):1383-8.
• [22] Effect of the adenosine A1 receptor agonist GR79236 on trigeminal nociception with blink reflex recordings in healthy human subjects. Cephalalgia. 2003 May;23(4):287-92.
• [23] The cardiac effects of a novel A1-adenosine receptor agonist in guinea pig isolated heart. J Pharmacol Exp Ther. 1994 Dec;271(3):1371-82.
• [24] Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion. J Mol Cell Cardiol. 2007 Sep;43(3):262-71.
• [25] Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. J Med Chem. 2000 Jun 1;43(11):2196-203.
• [26] Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique aden... J Med Chem. 2004 Apr 22;47(9):2243-55.
• [27] N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. J Med Chem. 1999 Sep 9;42(18):3463-77.
• [28] 2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a new scaffold to obtain potent and selective human A3 adenosine receptor antagonists: new insights into ... J Med Chem. 2009 Dec 10;52(23):7640-52.
• [29] N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor. J Med Chem. 1991 Sep;34(9):2877-82.
• [30] 1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. J Med Chem. 1991 Mar;34(3):1202-6.
• [31] Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists. J Med Chem. 1993 May 14;36(10):1333-42.
• [32] N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands. J Med Chem. 2002 Jul 18;45(15):3271-9.
• [33] A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding. J Biol Chem. 1994 Jan 28;269(4):2373-6.
• [34] Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. J Med Chem. 1988 Oct;31(10):2034-9.
• [35] Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic... J Med Chem. 2004 Feb 12;47(4):1031-43.
• [36] Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-,... J Med Chem. 1989 Jun;32(6):1231-7.
• [37] Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. J Med Chem. 2002 May 23;45(11):2131-8.
• [38] 5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 ... Bioorg Med Chem. 2008 Jan 1;16(1):336-53.
• [39] Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor. Bioorg Med Chem Lett. 2001 Aug 6;11(15):2017-9.
• [40] N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine recept... J Med Chem. 2009 Apr 23;52(8):2393-406.
• [41] 2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. J Med Chem. 2006 May 18;49(10):2861-7.
• [42] 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34.
• [43] A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. Bioorg Med Chem. 2008 Mar 15;16(6):2741-52.
• [44] Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists. J Med Chem. 2008 Mar 27;51(6):1764-70.
• [45] Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor. J Med Chem. 2007 Apr 19;50(8):1810-27.
• [46] Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. J Med Chem. 2008 Feb 14;51(3):400-6.
• [47] 2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database search... J Med Chem. 2005 Dec 29;48(26):8253-60.
• [48] N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor. J Med Chem. 2007 Mar 22;50(6):1222-30.
• [49] Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods. Eur J Med Chem. 2010 Aug;45(8):3459-71.
• [50] 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem. 2008 Aug 14;51(15):4449-55.
• [51] Identification of non-furan containing A2A antagonists using database mining and molecular similarity approaches. Bioorg Med Chem Lett. 2006 Dec 1;16(23):5993-7.
• [52] Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpu... Bioorg Med Chem Lett. 2008 May 1;18(9):2924-9.
• [53] 2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. J Med Chem. 2006 Dec 14;49(25):7373-83.
• [54] Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3.
• [55] Identification of the adenine binding site of the human A1 adenosine receptor. J Biol Chem. 1999 Feb 5;274(6):3617-21.
• [56] New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluati... J Med Chem. 2007 Aug 23;50(17):4061-74.
• [57] 1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4604-10.
• [58] Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7119-31.
• [59] Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
• [60] Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines. J Med Chem. 2009 Jan 8;52(1):33-47.
• [61] A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives. J Med Chem. 2000 Jul 27;43(15):2814-23.
• [62] Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301.
• [63] Synthesis of eudistomin D analogues and its effects on adenosine receptors. Bioorg Med Chem. 2008 Apr 1;16(7):3825-30.
• [64] Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. Bioorg Med Chem. 2010 Mar 15;18(6):2081-2088.
• [65] Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. J Med Chem. 2004 Jun 3;47(12):3019-31.
• [66] 8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands. Bioorg Med Chem. 2009 Apr 1;17(7):2812-22.
• [67] Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors. Biochem Pharmacol. 1998 Dec 1;56(11):1437-45.
• [68] Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationshi... J Med Chem. 1993 Oct 29;36(22):3341-9.
• [69] Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1931-4.
• [70] 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.
• [71] cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
• [72] Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali. J Nat Prod. 2000 Mar;63(3):318-21.
• [73] Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors. Biochem Pharmacol. 2005 Nov 25;70(11):1601-12.
• [74] Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. J Med Chem. 2000 Mar 23;43(6):1165-72.
• [75] Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis. J Nat Prod. 1997 Jun;60(6):638-41.
• [76] Adenosine receptors as therapeutic targets. Nat Rev Drug Discov. 2006 Mar;5(3):247-64.
• [77] Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging. J Med Chem. 2002 Nov 7;45(23):5150-6.
• [78] Reversine and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem. 2005 Jul 28;48(15):4910-8.
• [79] 125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors. J Med Chem. 1988 Apr;31(4):745-51.
• [80] Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist. Bioorg Med Chem Lett. 1999 Jul 19;9(14):1979-84.
• [81] Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors. J Pharmacol Sci. 2004 Sep;96(1):42-52.
• [82] Minoxidil-induced hair growth is mediated by adenosine in cultured dermal papilla cells: possible involvement of sulfonylurea receptor 2B as a target of minoxidil. J Invest Dermatol. 2001 Dec;117(6):1594-600.
• [83] 2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. J Med Chem. 2004 Dec 16;47(26):6529-40.
• [84] Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor. J Biol Chem. 1994 Dec 23;269(51):32077-84.
• [85] High selectivity of novel isoguanosine analogues for the adenosine A1 receptor. Bioorg. Med. Chem. Lett. 1(9):481-486 (1991).
• [86] KF26777 (2-(4-bromophenyl)-7,8-dihydro-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one dihydrochloride), a new potent and selective adenosine A3 receptor antagonist. Eur J Pharmacol. 2002 May 31;444(3):133-41.
• [87] Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp. J Nat Prod. 1998 Feb;61(2):301-5.
• [88] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 18).
• [89] Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. J Med Chem. 2010 Apr 22;53(8):3028-37.
• [90] Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist. Br J Pharmacol. 2006 Mar;147(5):533-41.
• [91] Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists. J Med Chem. 2004 Mar 11;47(6):1434-47.
• [92] Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2813-9.
• [93] Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors. Pharmacology. 1993;46(2):91-100.
• [94] Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1697-700.
• [95] N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A... Eur J Med Chem. 2008 Aug;43(8):1639-47.
• [96] Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective a... J Med Chem. 1992 Oct 30;35(22):4143-9.
• [97] (E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists. J Med Chem. 1992 Jun 12;35(12):2342-5.
• [98] Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of t... J Med Chem. 2008 Sep 25;51(18):5875-9.
• [99] Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2916-9.
• [100] 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with... J Med Chem. 2009 Jul 9;52(13):3994-4006.
• [101] 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors. Bioorg Med Chem. 2003 Feb 6;11(3):347-56.
• [102] Antinociceptive effects of novel A2B adenosine receptor antagonists. J Pharmacol Exp Ther. 2004 Jan;308(1):358-66.
• [103] Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):1-9.
• [104] Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A... J Med Chem. 1998 Jun 4;41(12):2126-33.
• [105] N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor. J Med Chem. 2003 Apr 10;46(8):1492-503.
• [106] Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists. Bioorg Med Chem. 2010 May 1;18(9):3078-87.
• [107] Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. J Med Chem. 2000 Jun 1;43(11):2227-38.
• [108] A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. J Med Chem. 1998 Oct 8;41(21):3987-93.
• [109] Characterization of 8-(N-methylisopropyl)amino-N6-(5'-endohydroxy- endonorbornyl)-9-methyladenine (WRC-0571), a highly potent and selective, non-xanthine antagonist of A1 adenosine receptors. J Pharmacol Exp Ther. 1996 Feb;276(2):490-9.
• [110] Inhibition of human mast cell activation with the novel selective adenosine A(2B) receptor antagonist 3-isobutyl-8-pyrrolidinoxanthine (IPDX)(2). Biochem Pharmacol. 2001 Nov 1;62(9):1163-73.
• [111] [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor. Eur J Pharmacol. 2007 Feb 5;556(1-3):14-8.
• [112] Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. J Med Chem. 1988 Jun;31(6):1179-83.