[Lys5,MeLeu9,Nle10]-Neurokinin A (4-10) (trifluoroacetate s

[Lys5,MeLeu9,Nle10]-Neurokinin A (4-10) is a neurokinin-2 (NK2) receptor agonist and derivative of neurokinin A (Cay-24221). It binds to NK2 receptors in isolated human colon circular muscle membranes in a radioligand binding assay (IC50 = 0. nM). [Lys5,MeLeu9,Nle10]-Neurokinin A (4-10) induces contraction of isolated rat bladder and fundus strips (EC50s = 10 and 117 nM, respectively), effects that can be inhibited by the NK2 receptor antagonists SR48968 and MEN10627. It also induces contraction of uterine horns isolated from rats in proestrus/estrus and diestrus/metestrus (EC50s = 25. and 51. nM, respectively). [Lys5,MeLeu9,Nle10]-Neurokinin A (4-10) induces urination and defecation in conscious dogs but also induces emesis and hypotension at similar doses.. Solulibility: DMSO: Soluble: = 10 mg/ml: Ethanol: Sparingly soluble: 1-10 mg/ml, PBS (pH 7.2): Soluble: = 10 mg/ml.