SB 223412

Talnetant (SB-223,412) is a neurokinin 3 receptor antagonist developed by GlaxoSmithKline, which is being researched for several different functions, primarily for irritable bowel syndrome and as a potential antipsychotic drug for the treatment of schizophrenia.

Talnetant is an antagonist of the neurokinin-3 (NK3) receptor (Ki= 1 nM). It is selective for NK3over NK1and NK2receptors (Kis = 144 and >100,000 nM, respectively, in CHO cells expressing recombinant human receptors). Talnetant inhibits calcium mobilization induced by neurokinin B in HEK293 cells expressing human NK3receptors (IC50= 16.6 nM). It inhibits contractions induced by the NK3receptor agonist senktide 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.

Talnetant acts as a neurokinin 3 (NK3) receptor antagonist used as an antispychotic.

Molecular Weight:382.5
XLogP3:5.7
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:5
Exact Mass:382.168127949
Monoisotopic Mass:382.168127949
Topological Polar Surface Area:62.2
Heavy Atom Count:29
Complexity:527
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes