Drug Information
| Drug General Information | Top | |||
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| Drug ID |
D0K5HI
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| Former ID |
DCL000241
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| Drug Name |
Talnetant
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| Synonyms |
Talnetant [INN]; SB 223412; SB-223412; N-((S)-alpha-Ethylbenzyl)-3-hydroxy-2-phenylcinchoninamide;N-(alpha-Ethylbenzyl)-3-hydroxy-2-phenylquinoline-4-carboxamide; 3-hydroxy-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide
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| Drug Type |
Small molecular drug
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| Indication | Schizophrenia [ICD-11: 6A20] | Phase 2 | [1] | |
| Irritable bowel syndrome [ICD-11: DD91.0; ICD-10: K55-K64, K58; ICD-9: 564.1, 787.91] | Discontinued in Phase 2 | [2], [3] | ||
| Schizoaffective disorder [ICD-11: 6A21] | Discontinued in Phase 2 | [2], [3] | ||
| Company |
GlaxoSmithKline
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| Structure |
 |
Download2D MOL |
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| Formula |
C25H22N2O2
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| Canonical SMILES |
CCC(C1=CC=CC=C1)NC(=O)C2=C(C(=NC3=CC=CC=C32)C4=CC=CC=C4)O
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| InChI |
1S/C25H22N2O2/c1-2-20(17-11-5-3-6-12-17)27-25(29)22-19-15-9-10-16-21(19)26-23(24(22)28)18-13-7-4-8-14-18/h3-16,20,28H,2H2,1H3,(H,27,29)/t20-/m0/s1
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| InChIKey |
BIAVGWDGIJKWRM-FQEVSTJZSA-N
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| CAS Number |
CAS 174636-32-9
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| PubChem Compound ID | ||||
| PubChem Substance ID | ||||
| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Neuromedin-K receptor (TACR3) | Target Info | Antagonist | [4], [5], [6] |
| KEGG Pathway | Calcium signaling pathway | |||
| Neuroactive ligand-receptor interaction | ||||
| Reactome | G alpha (q) signalling events | |||
| WikiPathways | Gastrin-CREB signalling pathway via PKC and MAPK | |||
| Peptide GPCRs | ||||
| GPCR ligand binding | ||||
| GPCR downstream signaling | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | ClinicalTrials.gov (NCT00300963) Effect Of Talnetant Versus Risperidone Versus Placebo On Psychotic Symptoms In Schizophrenic Patients in GlaxoSmithKline. | |||
| REF 2 | 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: 2132). | |||
| REF 3 | Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313. | |||
| REF 4 | Pharmacological characterization of senktide-induced tail whips. Neuropharmacology. 2010 Jan;58(1):259-67. | |||
| REF 5 | The tachykinin NK3 receptor agonist senktide induces locomotor activity in male Mongolian gerbils. Eur J Pharmacol. 2008 Dec 14;600(1-3):87-92. | |||
| REF 6 | Augmentation of antipsychotic-induced neurochemical changes by the NK3 receptor antagonist talnetant (SB-223412). Neuropharmacology. 2009 Feb;56(2):342-9. | |||
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