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pubmed-article:1709018pubmed:abstractTextTwo members of a new class of non-peptide antagonists of substance P, (+-)-cis-3-(2-methoxybenzylamino)-2-benzhydrylquinuclidine [(+/-)-CP-96,345; I] and (+-)-cis-3-(2-chlorobenzylamino)-2-benzhydrylquinuclidine [II], were tested for their ability to antagonize neurokinin-induced contractions of the rabbit cava and jugular veins (NK-1), the rabbit pulmonary artery (NK-2) and the rat portal vein (NK-3 system). Compound 1 is the most potent NK-1 receptor antagonist identified until now; its apparent affinity (pA2 = 9.52) is at least two log units higher than those of other NK-1 antagonists. Compound II is less active. Both compounds have been found to be almost inactive as NK-2 and NK-3 antagonists and should, therefore, be considered as selective for the NK-1 receptor. The new compounds have no direct myotropic effects and are specific for neurokinin (NK-1) receptors since they do not affect the myotropic effects of angiotensin, noradrenaline and bradykinin in the rabbit cava and jugular veins.lld:pubmed
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pubmed-article:1709018pubmed:articleTitleSelectivity and specificity of new, non-peptide, quinuclidine antagonists of substance P.lld:pubmed
pubmed-article:1709018pubmed:affiliationDepartment of Pharmacology, Medical School, University of Sherbrooke, Quebec, Canada.lld:pubmed
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pubmed-article:1709018pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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