产品描述:
GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor.{60141} It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.{60142}