Talnetant

Talnetant is an antagonist of the neurokinin-3 (NK3) receptor (Ki = 1 nM). It is selective for NK3 over NK1 and NK2 receptors (Kis = 144 and >100,000 nM, respectively, in CHO cells expressing recombinant human receptors). Talnetant inhibits calcium mobilization induced by neurokinin B (Cay-24542) in HEK293 cells expressing human NK3 receptors (IC50 = 16.6 nM). It inhibits contractions induced by the NK3 receptor agonist senktide (Cay-16721) in isolated rabbit iris sphincter muscle (pD2 = 9.1). Talnetant (5-20 mg/kg) reduces senktide-induced head shakes and tail whips in mice. It also inhibits senktide-induced wet-dog shakes, increases extracellular dopamine and norepinephrine in the medial prefrontal cortex, and attenuates haloperidol-induced increases in nucleus accumbens dopamine levels in guinea pigs.Formal Name: 3-hydroxy-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide. CAS Number: 174636-32-9. Synonyms: SB-223412. Molecular Formula: C25H22N2O2. Formula Weight: 382.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 25 mg/ml. lambdamax: 230, 252 nm. SMILES: OC1=C(C(N[C@@H](CC)C2=CC=CC=C2)=O)C(C=CC=C3)=C3N=C1C4=CC=CC=C4. InChi Code: 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. InChi Key: BIAVGWDGIJKWRM-FQEVSTJZSA-N.