Talnetant

Talnetant
Clinical data
ATC code	none;
Identifiers
	IUPAC name 3-hydroxy-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide;
CAS Number	174636-32-9 ;
PubChem CID	133090;
IUPHAR/BPS	2124;
ChemSpider	117450 ;
UNII	CZ3T9T146K;
ECHA InfoCard	100.236.526
Chemical and physical data
Formula	C25H22N2O2
Molar mass	382.454 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCC(C1=CC=CC=C1)NC(=O)C2=C(C(=NC3=CC=CC=C32)C4=CC=CC=C4)O;
	InChI 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) ; Key:BIAVGWDGIJKWRM-UHFFFAOYSA-N ;
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Talnetant (SB-223,412) is a neurokinin 3 receptor antagonist developed by GlaxoSmithKline, which is being researched for several functions (primarily treatment of irritable bowel syndrome, despite a 2007 study finding no statistically significant improvement in rectal hypersensitivity over placebo). Its use as a potential antipsychotic drug for the treatment of schizophrenia has also been discontinued.[1][2][3][4]

References

"UPDATE 1-GlaxoSmithKline prunes new drug pipeline". Reuters. Oct 15, 2007.
Evangelista S (July 2005). "Talnetant GlaxoSmithKline". Current Opinion in Investigational Drugs. 6 (7): 717–21. PMID 16044668.
Houghton LA, Cremonini F, Camilleri M, Busciglio I, Fell C, Cox V, et al. (September 2007). "Effect of the NK(3) receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans". Neurogastroenterology and Motility. 19 (9): 732–43. doi:10.1111/j.1365-2982.2007.00934.x. PMID 17727393.
Dawson LA, Cato KJ, Scott C, Watson JM, Wood MD, Foxton R, et al. (June 2008). "In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia". Neuropsychopharmacology. 33 (7): 1642–52. doi:10.1038/sj.npp.1301549. PMID 17728699.

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[1] "UPDATE 1-GlaxoSmithKline prunes new drug pipeline". Reuters. Oct 15, 2007.

[2] Evangelista S (July 2005). "Talnetant GlaxoSmithKline". Current Opinion in Investigational Drugs. 6 (7): 717–21. PMID 16044668.

[3] Houghton LA, Cremonini F, Camilleri M, Busciglio I, Fell C, Cox V, et al. (September 2007). "Effect of the NK(3) receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans". Neurogastroenterology and Motility. 19 (9): 732–43. doi:10.1111/j.1365-2982.2007.00934.x. PMID 17727393.

[4] Dawson LA, Cato KJ, Scott C, Watson JM, Wood MD, Foxton R, et al. (June 2008). "In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia". Neuropsychopharmacology. 33 (7): 1642–52. doi:10.1038/sj.npp.1301549. PMID 17728699.

Neurokinin receptor modulators
NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant
NK₂	Agonists: Neurokinin A Antagonists: GR-159897 Ibodutant Nepadutant Saredutant
NK₃	Agonists: Neurokinin B Senktide Antagonists: Fezolinetant (ESN-364) Osanetant (SR-142,801) Pavinetant (MLE-4901, AZD-2624, AZD-4901) SB-218,795 SB-222,200 Talnetant (SB-223,412)
See also: Receptor/signaling modulators • Signaling peptide/protein receptor modulators

Talnetant

See also

References