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

General Information of Drug (ID: DMOJA5G)

• Drug Name: Nuplazid Drug Info
• Synonyms: Pimavanserin tartrate; UNII-NA83F1SJSR; 706782-28-7; ACP 103; ACP-103; 706782-28-7 (tartrate); NA83F1SJSR; Pimavanserin tartrate [USAN]; Bis(1-(4-Fluorobenzyl)-1-(1-methylpiperidin-4-yl)-3-(4-(2-methylpropoxy)benzyl)urea) (2R,3R)-2,3-dihydroxybutanedioate; Pimavanserin tartrate (USAN); 1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea, ((2R,3R)-2,3-dihydroxysuccinate) (2:1); Nuplazide (TN); pimavanserin hemitartrate; DTXSID50220958; CHEBI:133014; HMS3886L06; HY-14557A; Pimavanserin Dihydroxysuccinate(2:1); AKOS027327334; CCG-270608; CS-7954; 1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea (2R,3R)-2,3-dihydroxysuccinate; AC-29901; AS-56699; N-(4-Fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1); Urea, N-((4-fluorophenyl)methyl)-N-(1-methyl-4-piperidinyl)-N'-((4-(2-methylpropoxy)phenyl)methyl)-, (2R,3R)-2,3-dihydroxybutanedioate (2:1); D08969; Q27284759; bis(4-{[(4-fluorophenyl)methyl]({[4-(2-methylpropoxy)phenyl]methyl}carbamoyl)amino}-1-methylpiperidin-1-ium) (2R,3R)-2,3-dihydroxybutanedioate; bis{N-[(4-fluorophenyl)methyl]-N-(1-methylpiperidin-4-yl)-N'-{[4-(2-methylpropoxy)phenyl]methyl}urea} (2R,3R)-2,3-dihydroxybutanedioate

Indication

Disease Entry	ICD 11	Status	REF
Alzheimer disease	8A20	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 11672491
  ChEBI ID: CHEBI:133014
  CAS Number: CAS 706782-28-7
  TTD Drug ID: DMOJA5G

Molecule-Related Drug Atlas

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	[4]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[5]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[6]
Lurasidone hydrochloride	DMCVPXO	Schizophrenia	6A20	Approved	[7]
Aniracetam	DMOIFW0	Cerebrovascular ischaemia	8B1Z	Approved	[8]
lumateperone tosylate	DMQ8HOJ	Schizophrenia	6A20	Approved	[9]
Sarpogrelate	DMGLP6S	Diabetic complication	5A2Y	Approved	[10]
Pimavanserin	DMR7IVC	Parkinson disease	8A00.0	Approved	[11]
Zicronapine	DMP8ESD	Schizophrenia	6A20	Phase 3	[12]

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	[13]
Tramadol	DMRQD04	Osteoarthritis	FA00-FA05	Approved	[14]
Mirtazapine	DML53ZJ	Depression	6A70-6A7Z	Approved	[15]
Nefazodone	DM4ZS8M	Major depressive disorder	6A70.3	Approved	[16]
Methysergide	DM1EF73	Migraine	8A80	Approved	[17]
Eltoprazine	DMW6C81	Attention deficit hyperactivity disorder	6A05.Z	Phase 3	[18]
M100907	DM7ZFBA	Sleep-wake disorder	7A00-7B2Z	Phase 3	[19]
SR46349B	DM1ODMR	Primary insomnia	7A00	Phase 3	[20]
Vabicaserin	DM9GZW6	Psychotic disorder	6A20-6A25	Phase 2	[21]

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	Agonist	[2]
5-HT 2C receptor (HTR2C)	TTWJBZ5	5HT2C_HUMAN	Agonist	[2]

References

• [1] ClinicalTrials.gov (NCT02035553) A Study of the Safety and Efficacy of Pimavanserin in Patients With Alzheimer's Disease Psychosis. U.S. National Institutes of Health.
• [2] The neuropharmacology of sleep paralysis hallucinations: serotonin 2A activation and a novel therapeutic drug. Psychopharmacology (Berl). 2018 Nov;235(11):3083-3091.
• [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] Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
• [5] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [6] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [7] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [8] 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.
• [9] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [10] 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.
• [11] 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.
• [12] Clinical pipeline report, company report or official report of Lundbeck.
• [13] Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
• [14] 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.
• [15] 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.
• [16] 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.
• [17] 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.
• [18] Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
• [19] 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.
• [20] 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.
• [21] 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.