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

General Information of Drug (ID: DMP6B59)

• Drug Name: Ocaperidone Drug Info
• Synonyms: Ocaperidona; 129029-23-8; UNII-26HUS7139V; 3-(2-(4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidino)ethyl)-2,9-dimethyl-4H-pyrido(1,2-a)pyrimidin-4-one; 26HUS7139V; Ocaperidonum; Ocaperidonum [INN-Latin]; Ocaperidona [INN-Spanish]; 4H-Pyrido[1,2-a]pyrimidin-4-one,3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2,9-dimethyl-; Ocaperidone (USAN); Ocaperidone [USAN:INN:BAN]; 3-[2-[4-(6-Fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl]ethyl]-2,9-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one; Ocaperidona; 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2,9-dimethylpyrido[1,2-a]pyrimidin-4-one; 8-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-1-piperidyl]ethyl]-2,9-dimethyl-6,10-diazabicyclo[440]deca-2,4,8,10-tetraen-7-one; FG-3019

Indication

Disease Entry	ICD 11	Status	REF
Idiopathic pulmonary fibrosis	CB03.4	Phase 2	[1]
Pancreatic cancer	2C10	Phase 2	[2]
Schizoaffective disorder	6A21	Phase 2	[3]
Schizophrenia	6A20	Phase 2	[3]
Type-2 diabetes	5A11	Phase 2	[1]
Diabetic nephropathy	GB61.Z	Phase 1b	[1]

• Cross-matching ID:
  PubChem CID: 71351
  CAS Number: CAS 129029-23-8
  TTD Drug ID: DMP6B59

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	[6]
ZOTEPINE	DMF3VXA	Anxiety disorder	6B00-6B0Z	Approved	[7]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[8]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[9]
Lurasidone hydrochloride	DMCVPXO	Schizophrenia	6A20	Approved	[10]
Aniracetam	DMOIFW0	Cerebrovascular ischaemia	8B1Z	Approved	[11]
lumateperone tosylate	DMQ8HOJ	Schizophrenia	6A20	Approved	[12]
Sarpogrelate	DMGLP6S	Diabetic complication	5A2Y	Approved	[13]
Pimavanserin	DMR7IVC	Parkinson disease	8A00.0	Approved	[14]
Zicronapine	DMP8ESD	Schizophrenia	6A20	Phase 3	[15]

Drug(s) Targeting Dopamine D2 receptor (D2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dopamine	DMPGUCF	Acromegaly	5A60.0	Approved	[16]
Haloperidol	DM96SE0	Delirium		Approved	[17]
Perphenazine	DMA4MRX	Schizophrenia	6A20	Approved	[18]
Perazine	DM2AOTZ	Psychotic disorder	6A20-6A25	Approved	[19]
Domperidone	DMBDPY0	Gastrointestinal disease	DE2Z	Approved	[20]
Levodopa	DMN3E57	Parkinson disease	8A00.0	Approved	[21]
Quetiapine	DM1N62C	Anorexia nervosa cachexia	6B80	Approved	[22]
Pimozide	DMW83TP	Schizophrenia	6A20	Approved	[23]
Chlorpromazine	DMBGZI3	Acute intermittent hepatic porphyria	5C58.11	Approved	[24]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[8]

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	Modulator	[4]
Connective tissue growth factor (CTGF)	TTSECX1	CTGF_HUMAN	Inhibitor	[5]
Dopamine D2 receptor (D2R)	TTEX248	DRD2_HUMAN	Modulator	[4]

References

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• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] 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: 46).
• [4] Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). J Pharmacol Exp Ther. 1992 Jan;260(1):146-59.
• [5] Current and emerging drugs for idiopathic pulmonary fibrosis. Expert Opin Emerg Drugs. 2007 Nov;12(4):627-46.
• [6] 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.
• [7] Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
• [8] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [9] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [10] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [11] 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.
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [13] 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.
• [14] 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.
• [15] Clinical pipeline report, company report or official report of Lundbeck.
• [16] The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
• [17] Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
• [18] CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
• [19] Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
• [20] Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
• [21] 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: 3639).
• [22] Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
• [23] [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
• [24] Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.