General Information of Drug (ID: DMB3R4Z)

Drug Name
SB 216641 Drug Info
Synonyms SB-216,641; SB-216641
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
3292447
ChEBI ID
CHEBI:92537
CAS Number
CAS 170230-39-4
TTD Drug ID
DMB3R4Z

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug(s) Targeting 5-HT 1B receptor (HTR1B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [3]
Eletriptan DMW649X Migraine 8A80 Approved [4]
Zolmitriptan DM1IB4Q Migraine 8A80 Approved [4]
Frovatriptan DM7RE8P Migraine 8A80 Approved [4]
Fluphenazine DMIT8LX Psychotic disorder 6A20-6A25 Approved [4]
Naratriptan DMO50U2 Headache 8A80-8A84 Approved [5]
Prolixin decanoate DMMJ1IS Schizophrenia 6A20 Approved [4]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [6]
NXN-188 DMMBAIH Migraine 8A80 Phase 2 [7]
[N-methyl-3H(3)]AZ-10419369 DMSCV02 Mood disorder 6A60-6E23 Phase 1 [8]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 1D receptor (HTR1D)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [9]
Eletriptan DMW649X Migraine 8A80 Approved [4]
Zolmitriptan DM1IB4Q Migraine 8A80 Approved [4]
Frovatriptan DM7RE8P Migraine 8A80 Approved [4]
Sumatriptan DMVYXR8 Cluster headache 8A81.0 Approved [10]
Rizatriptan DMDJMA3 Migraine 8A80 Approved [11]
Almogran DM7I64Z Migraine 8A80 Approved [12]
Neu-P11 DMIQDFW Alzheimer disease 8A20 Phase 2 [13]
FKB01MD DM2O7NM N. A. N. A. Phase 2 [14]
NXN-188 DMMBAIH Migraine 8A80 Phase 2 [7]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 2B receptor (HTR2B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [15]
Triflupromazine DMKFQJP Nausea MD90 Approved [16]
Minaprine DM0EP7M Depression 6A70-6A7Z Approved [17]
SPN-812 DMTV7XH Attention deficit hyperactivity disorder 6A05.Z Phase 4 [18]
Vabicaserin DM9GZW6 Psychotic disorder 6A20-6A25 Phase 2 [19]
PRX-08066 DMR7H2V Pulmonary arterial hypertension BB01.0 Phase 2 [20]
Pyrimidine derivative 29 DMVOYJ8 N. A. N. A. Patented [21]
Pyrimidine derivative 26 DM90WKN N. A. N. A. Patented [21]
Pyrimidine derivative 23 DM5MLQU N. A. N. A. Patented [21]
Pyrimidine derivative 25 DM51MFS N. A. N. A. Patented [21]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 2A receptor (HTR2A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [15]
ZOTEPINE DMF3VXA Anxiety disorder 6B00-6B0Z Approved [22]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [23]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [24]
Lurasidone hydrochloride DMCVPXO Schizophrenia 6A20 Approved [25]
Aniracetam DMOIFW0 Cerebrovascular ischaemia 8B1Z Approved [26]
lumateperone tosylate DMQ8HOJ Schizophrenia 6A20 Approved [27]
Sarpogrelate DMGLP6S Diabetic complication 5A2Y Approved [28]
Pimavanserin DMR7IVC Parkinson disease 8A00.0 Approved [29]
Zicronapine DMP8ESD Schizophrenia 6A20 Phase 3 [30]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 1A receptor (HTR1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Trazodone DMK1GBJ Depression 6A70-6A7Z Approved [4]
Buspirone DMBS632 Anxiety disorder 6B00-6B0Z Approved [31]
OPC-34712 DMHG57U Major depressive disorder 6A70.3 Approved [32]
Vilazodone DM4LECQ Major depressive disorder 6A70.3 Approved [33]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [24]
Gepirone DMGX5Q0 Major depressive disorder 6A70.3 Approved [34]
TERTATOLOL DM2L3D5 Hypertension BA00-BA04 Approved [35]
Urapidil DMD59GI Hypertension BA00-BA04 Approved [36]
Treximet DMU54QB Migraine 8A80 Approved [37]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [38]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 2C receptor (HTR2C)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [15]
Lorcaserin DMG6OYJ Obesity 5B81 Approved [39]
Tramadol DMRQD04 Osteoarthritis FA00-FA05 Approved [40]
Mirtazapine DML53ZJ Depression 6A70-6A7Z Approved [41]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [42]
Methysergide DM1EF73 Migraine 8A80 Approved [43]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [6]
M100907 DM7ZFBA Sleep-wake disorder 7A00-7B2Z Phase 3 [44]
SR46349B DM1ODMR Primary insomnia 7A00 Phase 3 [45]
Vabicaserin DM9GZW6 Psychotic disorder 6A20-6A25 Phase 2 [19]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Agonist [2]
5-HT 1B receptor (HTR1B) TTK8CXU 5HT1B_HUMAN Agonist [2]
5-HT 1D receptor (HTR1D) TT6MSOK 5HT1D_HUMAN Agonist [2]
5-HT 2A receptor (HTR2A) TTJQOD7 5HT2A_HUMAN Agonist [2]
5-HT 2B receptor (HTR2B) TT0K1SC 5HT2B_HUMAN Agonist [2]
5-HT 2C receptor (HTR2C) TTWJBZ5 5HT2C_HUMAN Agonist [2]

References

1 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. (Ligand id: 28).
2 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.
3 Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. J Neurochem. 1996 Nov;67(5):2096-103.
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5 Triptans in pregnancy. Ther Drug Monit. 2008 Feb;30(1):5-9.
6 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
7 Company report (NeurAxon)
8 5-HT1B and other related serotonergic proteins are altered in APPswe mutation. Neurosci Lett. 2015 May 6;594:137-43.
9 Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol. 1991 Aug;40(2):143-8.
10 Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
11 An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210.
12 Efficacy and tolerability of subcutaneous almotriptan for the treatment of acute migraine: a randomized, double-blind, parallel-group, dose-finding study. Clin Ther. 2001 Nov;23(11):1867-75.
13 Clinical pipeline report, company report or official report of Neurim Pharmaceuticals.
14 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
15 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.
16 Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat. Br J Pharmacol. 1979 Sep;67(1):79-85.
17 Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
18 New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300.
19 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.
20 Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
21 Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.
22 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
23 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
24 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
25 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
26 Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.
27 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
28 Beneficial effects of sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, supplemented with pioglitazone on diabetic model mice. Endocr Res. 2009;34(1-2):18-30.
29 Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2mg/day, but does not enhance efficacy of haloperidol, 2mg/day: comparison with reference dose risperidone, 6mg/day.Schizophr Res.2012 Nov;141(2-3):144-52.
30 Clinical pipeline report, company report or official report of Lundbeck.
31 Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
32 Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.
33 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
34 Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
35 Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile, Bioorg. Med. Chem. Lett. 3(10):2035-2038 (1993).
36 Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
37 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
38 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
39 Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
40 The inhibitory effects of tramadol on 5-hydroxytryptamine type 2C receptors expressed in Xenopus oocytes. Anesth Analg. 2004 May;98(5):1401-6, table of contents.
41 Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulatio... Mol Pharmacol. 2008 Mar;73(3):748-57.
42 Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies. Therapie. 2005 Sep-Oct;60(5):441-60.
43 Spinal serotonin receptor activation modulates the exercise ventilatory response with increased dead space in goats. Respir Physiol Neurobiol. 2008 May 31;161(3):230-8.
44 Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists ... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12.
45 SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. Neuropsychopharmacology. 2002 Sep;27(3):430-41.