Tachykinin antagonist I: Specific, competitive and tissue-selective neurokinin B antagonists on contractile activity in smooth muscles.
Two neurokinin B (NKB) analogs, [Gly6]-NKB [3-10] and [Arg3, D-Ala6]-NKB [3-10], were tested for agonistic activity as well as for their ability to antagonize the myotropic actions of NKB, neurokinin A, substance P, physalaemin and eledoisin in isolated guinea-pig ileum, guinea-pig urinary bladder, rat duodenum, rat vas deferens and rat portal vein. [Gly6]-NKB [3-10] in the guinea-pig ileum and rat portal vein and [Arg3, D-Ala6]-NKB [3-10] in the guinea-pig ileum were found to be the first specific and competitive antagonists against NKB.
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects*; D015287:Neurokinin B; D009479:Neuropeptides / Q000037:antagonists & inhibitors*; D011169:Portal Vein / Q000187:drug effects; D051381:Rats; D015320:Tachykinins
D009479:Neuropeptides; D015320:Tachykinins; D015287:Neurokinin B