title: Some pharmacological actions of nisoxetine, a bicyclic inhibitor of noradrenaline uptake.
abstract: Some peripheral actions of the phenoxyphenylpropylamine, nisoxetine, have been compared with those of the tricyclic antidepressant, desipramine. The two drugs were equipotent in inhibiting the accumulation of 3H-noradrenaline by the sympathetic nerve terminals of the rat vas deferens; and, in low doses, equipotent in potentiating the actions of noradrenaline at both alpha 1- and alpha 2-adrenoceptors in this tissue. In the vas deferens, the alpha 1-adrenoceptor blocking action of desipramine was evident at concentrations of 0.1 mumol l-1 and above; nisoxetine was less potent. Neither drug exhibited antagonist actions at alpha 2-adrenoceptors. Nisoxetine was also less potent than desipramine in inhibiting responses to histamine, carbachol and bradykinin on the guinea-pig isolated ileum. Thus nisoxetine is the more specific of the two neuronal uptake inhibitors and may be a useful tool to block neuronal uptake in experiments designed to classify adrenoceptors in other tissues.
mesh_terms: D000818:Animals; D001920:Bradykinin / Q000494:pharmacology; D002217:Carbachol / Q000494:pharmacology; D003891:Desipramine / Q000494:pharmacology; D005473:Fluoxetine / Q000031:analogs & derivatives / Q000494:pharmacology*; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009474:Neurons / Q000378:metabolism; D009638:Norepinephrine / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D011437:Propylamines / Q000494:pharmacology*; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects; D012110:Reserpine / Q000494:pharmacology; D014649:Vas Deferens / Q000187:drug effects; D014991:Xylazine / Q000494:pharmacology
chemical_list: D011437:Propylamines; D011942:Receptors, Adrenergic, alpha; D005473:Fluoxetine; C011386:nisoxetine; D014991:Xylazine; D006632:Histamine; D012110:Reserpine; D002217:Carbachol; D001920:Bradykinin; D003891:Desipramine; D009638:Norepinephrine