A nonpeptide NK3 antagonist (Ki = 1 nM); selective for NK3 over NK1 and NK2 receptors (Kis = 144 and >100

Talnetant – 250 mg

Brand:
Cayman
CAS:
174636-32-9
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Talnetant is an antagonist of the neurokinin-3 (NK3) receptor (Ki = 1 nM).{28052} 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 (Item No. 24542) in HEK293 cells expressing human NK3 receptors (IC50 = 16.6 nM). It inhibits contractions induced by the NK3 receptor agonist senktide (Item No. 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.{53729}  

 

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SKU: 29699 - 250 mg Category:

Description

A nonpeptide NK3 antagonist (Ki = 1 nM); selective for NK3 over NK1 and NK2 receptors (Kis = 144 and >100,000 nM, respectively, in CHO cells expressing recombinant human receptors); inhibits neurokinin B-induced calcium mobilization in HEK293 cells expressing human NK3 receptors (IC50 = 16.6 nM); inhibits senktide-induced contractions in isolated rabbit iris sphincter muscle (pD2 = 9.1); reduces senktide-induced head shakes and tail whips in mice from 5-20 mg/kg; 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

Synonyms:  SB-223412

Molecular weight: 382.5

CAS: 174636-32-9

Purity: ≥98%

Formulation: A crystalline solid

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