rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
2
|
pubmed:dateCreated |
1991-6-6
|
pubmed:abstractText |
Two 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.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Apr
|
pubmed:issn |
0006-291X
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
30
|
pubmed:volume |
176
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
894-901
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1709018-Angiotensin II,
pubmed-meshheading:1709018-Animals,
pubmed-meshheading:1709018-Blood Vessels,
pubmed-meshheading:1709018-Bradykinin,
pubmed-meshheading:1709018-Cell Line,
pubmed-meshheading:1709018-Guinea Pigs,
pubmed-meshheading:1709018-Humans,
pubmed-meshheading:1709018-Muscle Contraction,
pubmed-meshheading:1709018-Norepinephrine,
pubmed-meshheading:1709018-Quinuclidines,
pubmed-meshheading:1709018-Rabbits,
pubmed-meshheading:1709018-Rats,
pubmed-meshheading:1709018-Rats, Inbred Strains,
pubmed-meshheading:1709018-Receptors, Neurokinin-1,
pubmed-meshheading:1709018-Receptors, Neurotransmitter,
pubmed-meshheading:1709018-Substance P
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pubmed:year |
1991
|
pubmed:articleTitle |
Selectivity and specificity of new, non-peptide, quinuclidine antagonists of substance P.
|
pubmed:affiliation |
Department of Pharmacology, Medical School, University of Sherbrooke, Quebec, Canada.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|