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

General Information of DTT (ID: TT0K1SC)

• DTT Name: 5-HT 2B receptor (HTR2B) DTT Info
• Gene Name: HTR2B

Molecule-Related Drug & Molecule List

4 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[1]
Minaprine	DM0EP7M	Depression	6A70-6A7Z	Approved	[2]
Triflupromazine	DMKFQJP	Nausea	MD90	Approved	[3]
SPN-812	DMTV7XH	Attention deficit hyperactivity disorder	6A05.Z	Phase 4	[4]

2 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PRX-08066	DMR7H2V	Pulmonary arterial hypertension	BB01.0	Phase 2	[5]
Vabicaserin	DM9GZW6	Psychotic disorder	6A20-6A25	Phase 2	[6]

9 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pyrazole-3-carboxamide derivative 1	DMVQXZJ	N. A.	N. A.	Patented	[7]
Pyrimidine derivative 23	DM5MLQU	N. A.	N. A.	Patented	[7]
Pyrimidine derivative 24	DMOQ726	N. A.	N. A.	Patented	[7]
Pyrimidine derivative 25	DM51MFS	N. A.	N. A.	Patented	[7]
Pyrimidine derivative 26	DM90WKN	N. A.	N. A.	Patented	[7]
Pyrimidine derivative 27	DMIQSDW	N. A.	N. A.	Patented	[7]
Pyrimidine derivative 28	DM1D2AS	N. A.	N. A.	Patented	[7]
Pyrimidine derivative 29	DMVOYJ8	N. A.	N. A.	Patented	[7]
Quinoline derivative 2	DMNO2BP	N. A.	N. A.	Patented	[7]

6 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
FENDILINE	DMH6NG5	Coronary artery disease	BA80	Withdrawn from market	[8]
Ritanserin	DM0X36Y	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[9]
MT-500	DMCJ1B2	Migraine	8A80	Discontinued in Phase 1	[10]
LY53857	DMY71LJ	N. A.	N. A.	Terminated	[9]
Ro-60-0175	DMZSQU8	N. A.	N. A.	Terminated	[11]
SB 206553	DMS0QEP	N. A.	N. A.	Terminated	[12]

74 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+)-norfenfluramine	DMOZJA5	Discovery agent	N.A.	Investigative	[13]
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[14]
(-)-norfenfluramine	DMOY9J8	Discovery agent	N.A.	Investigative	[13]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine	DMYALON	Discovery agent	N.A.	Investigative	[15]
(5-methoxy-1H-indol-3-yl)methanamine	DMOPMNC	Discovery agent	N.A.	Investigative	[8]
1-((R)-2-aminopropyl)-1H-indazol-6-ol	DM74R0E	Discovery agent	N.A.	Investigative	[15]
1-((S)-2-aminopropyl)-1H-indazol-6-ol	DMU83KP	Discovery agent	N.A.	Investigative	[15]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol	DMRFJNC	Discovery agent	N.A.	Investigative	[15]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol	DM76JVB	Discovery agent	N.A.	Investigative	[15]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol	DMR2SXL	Discovery agent	N.A.	Investigative	[15]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol	DM8MNZG	Discovery agent	N.A.	Investigative	[15]
1-(2-aminoethyl)-1H-indazol-6-ol	DMKWO6A	Discovery agent	N.A.	Investigative	[15]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine	DMX5N3V	Discovery agent	N.A.	Investigative	[16]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol	DMO7NXE	Discovery agent	N.A.	Investigative	[17]
1-naphthylpiperazine	DM6BIWK	Discovery agent	N.A.	Investigative	[18]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine	DM1O0JD	Discovery agent	N.A.	Investigative	[15]
2-methyl-5-HT	DM1S5CB	N. A.	N. A.	Investigative	[18]
3-(2-Amino-propyl)-1H-indol-5-ol	DMQPNUM	Discovery agent	N.A.	Investigative	[15]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol	DMKYZGD	Discovery agent	N.A.	Investigative	[17]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol	DM32MIE	Discovery agent	N.A.	Investigative	[17]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol	DMMJP9D	Discovery agent	N.A.	Investigative	[17]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol	DM7VJPX	Discovery agent	N.A.	Investigative	[17]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol	DM0O2ZB	Discovery agent	N.A.	Investigative	[17]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol	DMDOIJM	Discovery agent	N.A.	Investigative	[17]
3-Dimethylaminomethyl-1H-indol-4-ol	DMSJUOH	Discovery agent	N.A.	Investigative	[17]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[19]
5-CT	DM260KD	Discovery agent	N.A.	Investigative	[18]
5-MEO-DMT	DMG0EL7	Discovery agent	N.A.	Investigative	[15]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine	DM592FB	Discovery agent	N.A.	Investigative	[20]
6-Fluoromelatonin	DMKFUO0	Discovery agent	N.A.	Investigative	[8]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine	DMIMLUO	Discovery agent	N.A.	Investigative	[20]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine	DMVZA27	Discovery agent	N.A.	Investigative	[20]
A-987306	DMU34BK	Discovery agent	N.A.	Investigative	[21]
ADRENOGLOMERULOTROPIN	DMP8NSU	Discovery agent	N.A.	Investigative	[8]
ADS-103253	DMH9A4S	Discovery agent	N.A.	Investigative	[22]
ADS-103274	DMBN6IE	Discovery agent	N.A.	Investigative	[22]
AL-37350A	DMRJ2GK	Discovery agent	N.A.	Investigative	[23]
alpha-methyl-5-HT	DMCAYXF	Discovery agent	N.A.	Investigative	[24]
BRL-15572	DMM61Y2	Discovery agent	N.A.	Investigative	[25]
BW723C86	DME15JU	Discovery agent	N.A.	Investigative	[26]
CHLOROPHENYLPIPERAZINE	DMOA8L2	Discovery agent	N.A.	Investigative	[27]
dihydroergocryptine	DMDW2NL	Discovery agent	N.A.	Investigative	[28]
EGIS-7625	DMLK4X5	Discovery agent	N.A.	Investigative	[29]
LY86057	DM5TYMG	Discovery agent	N.A.	Investigative	[18]
m-chlorophenylpiperazine	DMM1J2D	Discovery agent	N.A.	Investigative	[18]
METHYLENEDIOXYMETHAMPHETAMINE	DMYVU47	Discovery agent	N.A.	Investigative	[30]
norfenfluramine	DMGI4ZW	Discovery agent	N.A.	Investigative	[13]
norfluoxetine	DMKNUP3	Discovery agent	N.A.	Investigative	[13]
Org 12962	DM8JUBG	Discovery agent	N.A.	Investigative	[1]
piribedil	DMNP6QD	Discovery agent	N.A.	Investigative	[31]
R-1	DMK0YP7	Irritable bowel syndrome	DD91.0	Investigative	[32]
Racemic DOI	DM39FSQ	Discovery agent	N.A.	Investigative	[21]
RQ-00310941	DMYK6OU	Irritable bowel syndrome	DD91.0	Investigative	[32]
SB 204741	DM3LQF4	Discovery agent	N.A.	Investigative	[1]
SB 215505	DMCM4LT	Discovery agent	N.A.	Investigative	[33]
SB 216641	DMB3R4Z	Discovery agent	N.A.	Investigative	[25]
SB 221284	DM8DVY2	Discovery agent	N.A.	Investigative	[1]
SB 228357	DMKA8R4	Discovery agent	N.A.	Investigative	[34]
SB 242084	DMISBDC	Discovery agent	N.A.	Investigative	[35]
SEROTONIN	DMOFCRY	Discovery agent	N.A.	Investigative	[11]
spiramide	DM5KNMD	Discovery agent	N.A.	Investigative	[1]
spiroxatrine	DMPHRXQ	Discovery agent	N.A.	Investigative	[36]
TFMPP	DMAC8TP	Discovery agent	N.A.	Investigative	[18]
VER-2692	DM5WAM8	Discovery agent	N.A.	Investigative	[11]
VER-3323	DM7O2K1	Discovery agent	N.A.	Investigative	[37]
VER-5384	DMC2EO9	Discovery agent	N.A.	Investigative	[37]
VER-5593	DMZ2V0A	Discovery agent	N.A.	Investigative	[37]
YM-348	DM38F9T	Discovery agent	N.A.	Investigative	[20]
[125I]DOI	DMQUY08	Discovery agent	N.A.	Investigative	[32]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine	DMDIH96	Discovery agent	N.A.	Investigative	[17]
[3H]5-HT	DMYJXV7	Discovery agent	N.A.	Investigative	[18]
[3H]LSD	DM0YJHS	Discovery agent	N.A.	Investigative	[38]
[3H]mesulergine	DM8K6VF	Discovery agent	N.A.	Investigative	[1]
[3H]rauwolscine	DMBQZ2H	Discovery agent	N.A.	Investigative	[36]

References

• [1] Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.
• [2] Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
• [3] Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat. Br J Pharmacol. 1979 Sep;67(1):79-85.
• [4] New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300.
• [5] Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
• [6] Prediction of Efficacy of Vabicaserin, a 5-HT2C Agonist, for the Treatment of Schizophrenia Using a Quantitative Systems Pharmacology Model.CPT Pharmacometrics Syst Pharmacol.2014 Apr 23;3:e111.
• [7] Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.
• [8] Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify no... J Med Chem. 2010 Nov 11;53(21):7573-86.
• [9] p-Chloroamphetamine, a serotonin-releasing drug, elicited in rats a hyperglycemia mediated by the 5-HT1A and 5-HT2B/2C receptors. Eur J Pharmacol. 1998 Oct 23;359(2-3):185-90.
• [10] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [11] Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2006 Feb;16(3):677-80.
• [12] Strain-dependent effects of diazepam and the 5-HT2B/2C receptor antagonist SB 206553 in spontaneously hypertensive and Lewis rats tested in the elevated plus-maze. Braz J Med Biol Res. 2001 May;34(5):675-82.
• [13] Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation. 2000 Dec 5;102(23):2836-41.
• [14] Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
• [15] 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28.
• [16] The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. Bioorg Med Chem. 2007 Nov 1;15(21):6659-66.
• [17] SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.
• [18] Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor. Mol Pharmacol. 1993 Mar;43(3):419-26.
• [19] 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.
• [20] Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists. Bioorg Med Chem. 2008 Mar 15;16(6):3309-20.
• [21] 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.
• [22] Quinazoline and benzimidazole MCH-1R antagonists. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7.
• [23] A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. J Med Chem. 2003 Sep 11;46(19):4188-95.
• [24] The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60.
• [25] SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.
• [26] Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. Br J Pharmacol. 2003 Sep;140(2):277-84.
• [27] Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33.
• [28] Structural features for functional selectivity at serotonin receptors. Science. 2013 May 3;340(6132):615-9.
• [29] Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther. 2003 Sep-Nov;17(5-6):427-34.
• [30] The origin of MDMA (ecstasy) revisited: the true story reconstructed from the original documents. Addiction. 2006 Sep;101(9):1241-5.
• [31] Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804.
• [32] 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: 7).
• [33] Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4.
• [34] Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J Med Chem. 2000 Mar 23;43(6):1123-34.
• [35] SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
• [36] [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):17-24.
• [37] Indoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.
• [38] Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci. 2003 May 30;73(2):193-207.