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

General Information of Drug (ID: DMN6CAG)

• Drug Name: Tiapride Drug Info
• Synonyms: tiapride; 51012-32-9; Thiapride; Tiapridal; N-(2-(Diethylamino)ethyl)-2-methoxy-5-(methylsulfonyl)benzamide; Tiapridum [INN-Latin]; Tiaprida [INN-Spanish]; UNII-LAH70H9JPH; FLO 1347; Tiapride [INN:BAN:DCF]; Tiapride HCl; EINECS 256-907-9; LAH70H9JPH; BRN 2390588; JTVPZMFULRWINT-UHFFFAOYSA-N; BENZAMIDE, N-(2-(DIETHYLAMINO)ETHYL)-2-METHOXY-5-(METHYLSULFONYL)-; N-(2-(Diethylamino)ethyl)-5-(methylsulfonyl)-o-anisamide; Tiapridum; Tiaprida; Benzamide, N-[2-(diethylamino)ethyl]-2-methoxy-5-(methylsulfonyl)-; NCGC00015996-02; SPI-860

Indication

Disease Entry	ICD 11	Status	REF
Alcohol dependence	6C40.2	Approved	[1]
Neuropathic pain	8E43.0	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 5467
  ChEBI ID: CHEBI:94666
  CAS Number: CAS 51012-32-9
  TTD Drug ID: DMN6CAG

Molecule-Related Drug Atlas

Drug(s) Targeting Voltage-gated sodium channel alpha Nav1.8 (SCN10A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Rilpivirine	DMJ0QOW	Human immunodeficiency virus infection	1C62	Approved	[4]
Ropivacaine	DMSPJG2	Anaesthesia	9A78.6	Approved	[5]
Bupivacaine	DM4PRFC	Anaesthesia	9A78.6	Approved	[5]
Tetracaine	DM9J6C2	Spinal anesthesia	MB40.3	Approved	[6]
Proparacaine	DMLS39E	Anaesthesia	9A78.6	Approved	[5]
Conatumumab	DM2UOSN	Colorectal cancer	2B91.Z	Phase 2	[7]
VX-150	DMGDB21	Neuropathic pain	8E43.0	Phase 2	[8]
DSP-2230	DM0WTMD	Neuropathic pain	8E43.0	Phase 1	[9]
PF-01247324	DM93LMS	Pain	MG30-MG3Z	Phase 1	[10]
VX-128	DMC8J0G	Pain	MG30-MG3Z	Phase 1	[8]

Drug(s) Targeting Dopamine D2 receptor (D2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dopamine	DMPGUCF	Acromegaly	5A60.0	Approved	[11]
Haloperidol	DM96SE0	Delirium		Approved	[12]
Perphenazine	DMA4MRX	Schizophrenia	6A20	Approved	[13]
Perazine	DM2AOTZ	Psychotic disorder	6A20-6A25	Approved	[14]
Domperidone	DMBDPY0	Gastrointestinal disease	DE2Z	Approved	[15]
Levodopa	DMN3E57	Parkinson disease	8A00.0	Approved	[16]
Quetiapine	DM1N62C	Anorexia nervosa cachexia	6B80	Approved	[17]
Pimozide	DMW83TP	Schizophrenia	6A20	Approved	[18]
Chlorpromazine	DMBGZI3	Acute intermittent hepatic porphyria	5C58.11	Approved	[19]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dopamine D2 receptor (D2R)	TTEX248	DRD2_HUMAN	Antagonist	[3]
Voltage-gated sodium channel alpha Nav1.8 (SCN10A)	TT90XZ8	SCNAA_HUMAN	Inhibitor	[2]

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [2] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [3] The treatment of Tourette's syndrome: current opinions. Expert Opin Pharmacother. 2002 Jul;3(7):899-914.
• [4] Structures of muO-conotoxins from Conus marmoreus. I nhibitors of tetrodotoxin (TTX)-sensitive and TTX-resistant sodium channels in mammalian senso... J Biol Chem. 2004 Jun 11;279(24):25774-82.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [6] Heterologous expression and functional analysis of rat Nav1.8 (SNS) voltage-gated sodium channels in the dorsal root ganglion neuroblastoma cell line ND7-23. Neuropharmacology. 2004 Mar;46(3):425-38.
• [7] Pathobiology of visceral pain: molecular mechanisms and therapeutic implications. II. Genetic approaches to pain therapy. Am J Physiol Gastrointest Liver Physiol. 2000 Apr;278(4):G507-12.
• [8] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [9] Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
• [10] Oral Administration of PF-01247324, a Subtype-Selective Nav1.8 Blocker, Reverses Cerebellar Deficits in a Mouse Model of Multiple Sclerosis. PLoS One. 2015; 10(3): e0119067.
• [11] 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.
• [12] Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
• [13] CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
• [14] 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.
• [15] Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
• [16] 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).
• [17] Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
• [18] [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
• [19] 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.
• [20] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.