talnetant-sb-223412

Description: Talnetant (formerly also known as SB 223412) is a potent and selective NK3 receptor antagonist with ki value of 1.4 nM (hNK-3-CHO); Selectivity studies versus the other neurokinin receptors (hNK-2-CHO and hNK-1-CHO) revealed that Talnetant is about 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 microM. In vitro studies demonstrated that Talnetant is a potent functional antagonist of the hNK-3 receptor (reversal of senktide-induced contractions in rabbit isolated iris sphincter muscles and reversal of NKB-induced Ca2+ mobilization in CHO cells stably expressing the hNK-3 receptor), while in vivo this compound showed oral and intravenous activity in NK-3 receptor-driven models (senktide-induced behavioral responses in mice and senktide-induced miosis in rabbits). Overall, the biological data indicate that Talnetant may serve as a pharmacological tool in animal models of disease to assess the functional and pathophysiological role of the NK-3 receptor and to establish therapeutic indications for non-peptide NK-3 receptor antagonists.

References: J Med Chem. 1999 Mar 25; 42(6):1053-65; Neuropsychopharmacology. 2008 Jun; 33(7):1642-52.

Related CAS#: 204519-66-4 (HCl salt)