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
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. Talnetant GlaxoSmithKline. Current Opinion on Investigational Drugs. 2005 Jul;6(7):717-21. PMID 16044668
↑ Houghton LA, Cremonini F, Camilleri M, Busciglio I, Fell C, Cox V, Alpers DH, Dewit OE, Dukes GE, Gray E, Lea R, Zinsmeister AR, Whorwell PJ. Effect of the NK(3) receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans. Neurogastroenterology and Motility. 2007 Sep;19(9):732-43. PMID 17727393
↑ Dawson LA, Cato KJ, Scott C, Watson JM, Wood MD, Foxton R, de la Flor R, Jones GA, Kew JN, Cluderay JE, Southam E, Murkitt GS, Gartlon J, Pemberton DJ, Jones DN, Davies CH, Hagan J. In Vitro and In Vivo Characterization of the Non-peptide NK(3) Receptor Antagonist SB-223412 (Talnetant): Potential Therapeutic Utility in the Treatment of Schizophrenia. Neuropsychopharmacology. 2008 Jun;33(7):1642-52. PMID 17728699

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

[2] Evangelista S. Talnetant GlaxoSmithKline. Current Opinion on Investigational Drugs. 2005 Jul;6(7):717-21. PMID 16044668

[3] Houghton LA, Cremonini F, Camilleri M, Busciglio I, Fell C, Cox V, Alpers DH, Dewit OE, Dukes GE, Gray E, Lea R, Zinsmeister AR, Whorwell PJ. Effect of the NK(3) receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans. Neurogastroenterology and Motility. 2007 Sep;19(9):732-43. PMID 17727393

[4] Dawson LA, Cato KJ, Scott C, Watson JM, Wood MD, Foxton R, de la Flor R, Jones GA, Kew JN, Cluderay JE, Southam E, Murkitt GS, Gartlon J, Pemberton DJ, Jones DN, Davies CH, Hagan J. In Vitro and In Vivo Characterization of the Non-peptide NK(3) Receptor Antagonist SB-223412 (Talnetant): Potential Therapeutic Utility in the Treatment of Schizophrenia. Neuropsychopharmacology. 2008 Jun;33(7):1642-52. 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

Clinical data

ATC code	none
Identifiers
IUPAC name 3-hydroxy-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide
CAS Number	174636-32-9^Y
PubChem CID	133090
IUPHAR/BPS	2124
ChemSpider	117450^N
UNII	CZ3T9T146K
ECHA InfoCard	100.236.526
Chemical and physical data
Formula	C₂₅H₂₂N₂O₂
Molar mass	382.454 g/mol
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)^N Key:BIAVGWDGIJKWRM-UHFFFAOYSA-N^N
^NY (what is this?) (verify)

Talnetant

See also

References