Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT2NUT5)

• DTT Name: Adrenergic receptor alpha-2C (ADRA2C)
• Synonyms: Subtype C4; Alpha-2CAR; Alpha-2C adrenoreceptor; Alpha-2C adrenoceptor; Alpha-2C adrenergic receptor; Alpha-2 adrenergic receptor subtype C4; ADRA2RL2; ADRA2L2
• Gene Name: ADRA2C
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: ADA2C_HUMAN
• TTD ID: T01777
• Sequence:
  MASPALAAALAVAAAAGPNASGAGERGSGGVANASGASWGPPRGQYSAGAVAGLAAVVGF
  LIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFG
  QVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISA
  VISFPPLVSLYRQPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLR
  TRTLSEKRAPVGPDGASPTTENGLGAAAGAGENGHCAPPPADVEPDESSAAAERRRRRGA
  LRRGGRRRAGAEGGAGGADGQGAGPGAAESGALTASRSPGPGGRLSRASSRSVEFFLSRR
  RRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQVPGPLFK
  FFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ
• Function: Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
• KEGG Pathway:
  cGMP-PKG signaling pathway (hsa04022)
  Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  Adrenaline signalling through Alpha-2 adrenergic receptor (R-HSA-392023)
  Adrenaline,noradrenaline inhibits insulin secretion (R-HSA-400042)
  G alpha (i) signalling events (R-HSA-418594)
  G alpha (z) signalling events (R-HSA-418597)
  Surfactant metabolism (R-HSA-5683826)
  Adrenoceptors (R-HSA-390696)

Molecular Interaction Atlas (MIA) of This DTT

9 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amezinium	DM6I2WQ	Hypotension	BA20-BA21	Approved	[2]
Amosulalol	DML8QSZ	Hypertension	BA00-BA04	Approved	[1]
Brimonidine	DMQLT4N	Ocular hypertension	9C61.01	Approved	[3]
Dihydroergocristine	DM5SQ1G	Alcohol dependence	6C40.2	Approved	[4]
MOXONIDINE	DMGFB0E	Alcohol dependence	6C40.2	Approved	[5]
Propylhexedrine	DMTBW2O	Obesity	5B81	Approved	[6]
Rilmenidine	DM13PQW	Hypertension	BA00-BA04	Approved	[7]
Tetrahydrozoline	DMT57WC	Ocular disease	1F00.1Z	Approved	[8]
Xylometazoline	DMKV32D	Allergic rhinitis	CA08.0	Phase 4	[9]

8 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
IDAZOXAN HYDROCHLORIDE	DMSP0X8	Neurological disorder	6B60	Phase 3	[10]
TNX-102	DMO1234	Fibromyalgia	MG30.01	Phase 3	[11]
AGN-XX/YY	DMMGAUK	Diabetic nephropathy	GB61.Z	Phase 2	[12]
BAY1193397	DM83IYE	Peripheral arterial disease	BD4Z	Phase 2	[13]
Fadolmidine	DM6RKG3	Neuropathic pain	8E43.0	Phase 2	[14]
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[15]
ORM-12741	DM8ARQW	Alzheimer disease	8A20	Phase 2	[16]
V-101	DMDPFTB	Erythema	ME64.0	Phase 2	[17]

21 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
INDORAMIN	DMNSJFD	Hypertension	BA00-BA04	Withdrawn from market	[18]
Ecabapide	DMFOEVQ	Peptic ulcer	DA61	Discontinued in Preregistration	[19]
Delequamine hydrochloride	DMEMF60	Male sexual disorder	HA02.0	Discontinued in Phase 3	[20]
FLUPAROXAN	DMN1O7E	Depression	6A70-6A7Z	Discontinued in Phase 3	[21]
NOLOMIROLE HYDROCHLORIDE	DMJL5TR	Heart failure	BD10-BD13	Discontinued in Phase 3	[22]
Deriglidole	DMYJ28R	Diabetic complication	5A2Y	Discontinued in Phase 2	[23]
GYKI-16084	DMMZQVS	Prostate disease	GA91	Discontinued in Phase 2	[24]
JTH-601	DMQRKH4	Prostate disease	GA91	Discontinued in Phase 2	[25]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[26]
MK-912	DMMNUZC	N. A.	N. A.	Discontinued in Phase 2	[27]
NMI-870	DMU596F	Sexual dysfunction	HA00-HA01	Discontinued in Phase 2	[28]
SGB-1534	DMBG6LP	Hypotension	BA20-BA21	Discontinued in Phase 2	[29]
GYKI-12743	DMQNX02	Hypertension	BA00-BA04	Discontinued in Phase 1	[30]
A-75169	DMPX37E	Glaucoma/ocular hypertension	9C61	Terminated	[32]
A-80426	DMBC3DG	N. A.	N. A.	Terminated	[33]
ARC239	DMQ52JR	N. A.	N. A.	Terminated	[34]
F-14413	DMGH3QD	Alzheimer disease	8A20	Terminated	[35]
Midaglizole	DM96WKA	Asthma	CA23	Terminated	[36]
SK&F-104078	DMRADBU	N. A.	N. A.	Terminated	[18]
SNAP-5089	DMROJEN	Heart arrhythmia	BC65	Terminated	[37]
WB-4101	DMQU8B1	N. A.	N. A.	Terminated	[38]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
5-(N,N-hexamethylene)-amiloride	DMC4IUQ	Coronavirus infection	1D92	Preclinical	[31]

73 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[39]
(1,2,3,4-Tetrahydro-isoquinolin-3-yl)-methanol	DMF6WHC	Discovery agent	N.A.	Investigative	[40]
(1H-Benzoimidazol-5-yl)-(1H-imidazol-2-yl)-amine	DMPKM9B	Discovery agent	N.A.	Investigative	[41]
(1H-Imidazol-2-yl)-quinoxalin-6-yl-amine	DMRDHL2	Discovery agent	N.A.	Investigative	[41]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine	DM27TH9	Discovery agent	N.A.	Investigative	[41]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine	DM8N79M	Discovery agent	N.A.	Investigative	[41]
(2-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine	DME6MYZ	Discovery agent	N.A.	Investigative	[42]
(3-Ethyl-indol-1-yl)-propyl-pyridin-4-yl-amine	DM5WJBH	Discovery agent	N.A.	Investigative	[42]
(3-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine	DMHED9G	Discovery agent	N.A.	Investigative	[42]
(R)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline	DM98L2X	Discovery agent	N.A.	Investigative	[43]
(S)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline	DMS4JAG	Discovery agent	N.A.	Investigative	[43]
1,2,3,4,4a,5,10,10a-Octahydro-benzo[g]quinoline	DMDYX7P	Discovery agent	N.A.	Investigative	[44]
1,2,3,4,5,6-Hexahydro-benzo[c]azocine	DMTKYFE	Discovery agent	N.A.	Investigative	[43]
1,2,3,4-Tetrahydro-benzo[h]isoquinolin-8-ol	DMHKANE	Discovery agent	N.A.	Investigative	[45]
1,2,3,4-Tetrahydro-isoquinolin-7-ol	DM5VLIE	Discovery agent	N.A.	Investigative	[45]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole	DM3JGVF	Discovery agent	N.A.	Investigative	[46]
1,2,3,4-tetrahydroisoquinoline	DMZGCEQ	Discovery agent	N.A.	Investigative	[47]
1-((S)-2-aminopropyl)-1H-indazol-6-ol	DMU83KP	Discovery agent	N.A.	Investigative	[48]
2,3,4,5-Tetrahydro-1H-benzo[c]azepine	DM1RE9Q	Discovery agent	N.A.	Investigative	[43]
2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine	DM4EZOB	Discovery agent	N.A.	Investigative	[43]
2,3,4,5-Tetrahydro-benzo[f][1,4]oxazepine	DMOFG4M	Discovery agent	N.A.	Investigative	[43]
2,3-Dihydro-1H-isoindole	DMWI9XS	Discovery agent	N.A.	Investigative	[43]
2-BFi	DMFAW4R	Discovery agent	N.A.	Investigative	[49]
3-Fluoromethyl-1,2,3,4-tetrahydro-isoquinoline	DMDPUC7	Discovery agent	N.A.	Investigative	[50]
3-Methoxymethyl-1,2,3,4-tetrahydro-isoquinoline	DMH1RX6	Discovery agent	N.A.	Investigative	[40]
3-Methyl-1,2,3,4-tetrahydro-isoquinoline	DMIWQ7G	Discovery agent	N.A.	Investigative	[43]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole	DMFYBLH	Discovery agent	N.A.	Investigative	[15]
4-(4-Methyl-indan-1-yl)-1H-imidazole	DMYZHXR	Discovery agent	N.A.	Investigative	[51]
5-Aminomethyl-naphthalen-2-ol	DMTP9DB	Discovery agent	N.A.	Investigative	[45]
5-methylurapidil	DMCX9WN	Discovery agent	N.A.	Investigative	[52]
6,7,8,9-Tetrahydro-5-thia-8-aza-benzocycloheptene	DMNOI7B	Discovery agent	N.A.	Investigative	[43]
6-fluoro-noradrenaline	DMF2RGY	Discovery agent	N.A.	Investigative	[53]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline	DMQ1BE8	Discovery agent	N.A.	Investigative	[54]
8-Methoxy-1,2,3,4-tetrahydro-benzo[h]isoquinoline	DMY50UR	Discovery agent	N.A.	Investigative	[45]
A61603	DM7W2ME	Discovery agent	N.A.	Investigative	[55]
all-trans-4-oxo-retinoic acid	DMM2R1N	Discovery agent	N.A.	Investigative	[56]
amidephrine	DMST5VW	Discovery agent	N.A.	Investigative	[53]
Butyl-indol-1-yl-pyridin-4-yl-amine	DM1CX9Y	Discovery agent	N.A.	Investigative	[42]
C-(6-Methoxy-naphthalen-1-yl)-methylamine	DMJ6SYI	Discovery agent	N.A.	Investigative	[45]
C-Naphthalen-1-yl-methylamine	DMFW1JC	Discovery agent	N.A.	Investigative	[45]
Chloroethylclonidine	DMKZIES	Discovery agent	N.A.	Investigative	[57]
Ciproxifan	DM9N8WM	Dementia	6D80-6D86	Investigative	[58]
cirazoline	DMU6JOK	Discovery agent	N.A.	Investigative	[53]
CONESSINE	DM4VYP0	Discovery agent	N.A.	Investigative	[59]
ETHOXY-IDAZOXAN	DMNOTH5	Poison intoxication	NE6Z	Investigative	[60]
Ethyl-indol-1-yl-pyridin-4-yl-amine	DM3CWFR	Discovery agent	N.A.	Investigative	[42]
GNF-PF-2857	DML5QFZ	Discovery agent	N.A.	Investigative	[61]
GNF-PF-3878	DM7BXHQ	Discovery agent	N.A.	Investigative	[61]
indanidine	DM4S81A	Discovery agent	N.A.	Investigative	[53]
Indol-1-yl-methyl-pyridin-4-yl-amine	DMJB876	Discovery agent	N.A.	Investigative	[42]
Indol-1-yl-prop-2-ynyl-pyridin-4-yl-amine	DMR9GNW	Discovery agent	N.A.	Investigative	[42]
Indol-1-yl-pyridin-4-yl-amine	DM1F53L	Discovery agent	N.A.	Investigative	[42]
JP1302	DMMVBK6	Discovery agent	N.A.	Investigative	[62]
METHYLNORADRENALINE	DMOWMPL	Discovery agent	N.A.	Investigative	[38]
MEZILAMINE	DMVYWJS	Discovery agent	N.A.	Investigative	[63]
PIPEROXAN	DMIHO0P	Discovery agent	N.A.	Investigative	[38]
piribedil	DMNP6QD	Discovery agent	N.A.	Investigative	[64]
R-226161	DM4BP7S	Discovery agent	N.A.	Investigative	[65]
S-34324	DMZLQ5W	Discovery agent	N.A.	Investigative	[33]
SK&F-64139	DM60Y3Q	Discovery agent	N.A.	Investigative	[47]
SKF 89748	DMWODHR	Discovery agent	N.A.	Investigative	[53]
SNAP-5150	DM2OLGQ	Discovery agent	N.A.	Investigative	[37]
spiroxatrine	DMPHRXQ	Discovery agent	N.A.	Investigative	[66]
TRACIZOLINE	DM18CV3	Discovery agent	N.A.	Investigative	[54]
Tramazoline	DM3ML0N	Discovery agent	N.A.	Investigative	[38]
TRYPTOLINE	DMV19K7	Discovery agent	N.A.	Investigative	[54]
V-103	DM0KSFN	Contusion	ND56.0	Investigative	[67]
xylazine	DMSXJUW	Discovery agent	N.A.	Investigative	[68]
[125I]BE-2254	DM7GVYF	Discovery agent	N.A.	Investigative	[69]
[125I]HEAT	DMTFP5Q	Discovery agent	N.A.	Investigative	[70]
[3H]MK-912	DMO89N0	Discovery agent	N.A.	Investigative	[71]
[3H]rauwolscine	DMBQZ2H	Discovery agent	N.A.	Investigative	[72]
[3H]RX821002	DM6IRN4	Discovery agent	N.A.	Investigative	[73]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Alzheimer's disease	8A00.0	Entorhinal cortex	1.76E-01	-0.06	-0.28

References

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