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

General Information of Drug (ID: DMISBDC)

• Drug Name: SB 242084 Drug Info
• Synonyms: SB-242,084; SB242084

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 3644637
  CAS Number: CAS 181632-25-7
  TTD Drug ID: DMISBDC

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 2B receptor (HTR2B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[3]
Triflupromazine	DMKFQJP	Nausea	MD90	Approved	[4]
Minaprine	DM0EP7M	Depression	6A70-6A7Z	Approved	[5]
SPN-812	DMTV7XH	Attention deficit hyperactivity disorder	6A05.Z	Phase 4	[6]
Vabicaserin	DM9GZW6	Psychotic disorder	6A20-6A25	Phase 2	[7]
PRX-08066	DMR7H2V	Pulmonary arterial hypertension	BB01.0	Phase 2	[8]
Pyrimidine derivative 29	DMVOYJ8	N. A.	N. A.	Patented	[9]
Pyrimidine derivative 26	DM90WKN	N. A.	N. A.	Patented	[9]
Pyrimidine derivative 23	DM5MLQU	N. A.	N. A.	Patented	[9]
Pyrimidine derivative 25	DM51MFS	N. A.	N. A.	Patented	[9]

Drug(s) Targeting 5-HT 2A receptor (HTR2A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[3]
ZOTEPINE	DMF3VXA	Anxiety disorder	6B00-6B0Z	Approved	[10]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[11]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[12]
Lurasidone hydrochloride	DMCVPXO	Schizophrenia	6A20	Approved	[13]
Aniracetam	DMOIFW0	Cerebrovascular ischaemia	8B1Z	Approved	[14]
lumateperone tosylate	DMQ8HOJ	Schizophrenia	6A20	Approved	[15]
Sarpogrelate	DMGLP6S	Diabetic complication	5A2Y	Approved	[16]
Pimavanserin	DMR7IVC	Parkinson disease	8A00.0	Approved	[17]
Zicronapine	DMP8ESD	Schizophrenia	6A20	Phase 3	[18]

Drug(s) Targeting 5-HT 2C receptor (HTR2C)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[3]
Lorcaserin	DMG6OYJ	Obesity	5B81	Approved	[19]
Tramadol	DMRQD04	Osteoarthritis	FA00-FA05	Approved	[20]
Mirtazapine	DML53ZJ	Depression	6A70-6A7Z	Approved	[21]
Nefazodone	DM4ZS8M	Major depressive disorder	6A70.3	Approved	[22]
Methysergide	DM1EF73	Migraine	8A80	Approved	[23]
Eltoprazine	DMW6C81	Attention deficit hyperactivity disorder	6A05.Z	Phase 3	[24]
M100907	DM7ZFBA	Sleep-wake disorder	7A00-7B2Z	Phase 3	[25]
SR46349B	DM1ODMR	Primary insomnia	7A00	Phase 3	[26]
Vabicaserin	DM9GZW6	Psychotic disorder	6A20-6A25	Phase 2	[7]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 2A receptor (HTR2A)	TTJQOD7	5HT2A_HUMAN	Antagonist	[2]
5-HT 2B receptor (HTR2B)	TT0K1SC	5HT2B_HUMAN	Antagonist	[2]
5-HT 2C receptor (HTR2C)	TTWJBZ5	5HT2C_HUMAN	Antagonist	[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: 193).
• [2] SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
• [3] 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.
• [4] Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat. Br J Pharmacol. 1979 Sep;67(1):79-85.
• [5] Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
• [6] New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300.
• [7] 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.
• [8] Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
• [9] Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.
• [10] Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
• [11] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [12] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [13] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [14] 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.
• [15] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [16] 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.
• [17] 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.
• [18] Clinical pipeline report, company report or official report of Lundbeck.
• [19] Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
• [20] 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.
• [21] 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.
• [22] 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.
• [23] 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.
• [24] Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
• [25] 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.
• [26] 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.