Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
|
pubmed:dateCreated |
1989-5-11
|
pubmed:abstractText |
3H-Quinuclidinyl benzylate (3H-QNB) and 3H-cis-methyldioxolane (3H-CD) binding to cholinergic muscarinic receptors have been carried out on the same membrane preparation from the rat brain cortex. Inhibition of 3H-QNB and 3H-CD binding by cholinergic muscarinic agonists and antagonists has been studied with determination of the IC50 values for each ligand. Antagonists were as potent at inhibiting 3H-QNB binding as 3H-CD binding. Muscarinic agonists were much less potent at inhibiting 3H-QNB binding than 3H-CD binding. The ratio of the IC50 values for the inhibition of the binding of 3H-QNB and 3H-CD was between 1 and 10 for antagonists and between 500 and 5000 for agonists. It is suggested that the determination of this ratio predicts agonist or antagonist activity of unknown compounds and represents a useful tool for their screening.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-methyldioxolane,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxolanes,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxoles,
http://linkedlifedata.com/resource/pubmed/chemical/Parasympathomimetics,
http://linkedlifedata.com/resource/pubmed/chemical/Quinuclidines,
http://linkedlifedata.com/resource/pubmed/chemical/Quinuclidinyl Benzilate,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic
|
pubmed:status |
MEDLINE
|
pubmed:month |
Oct
|
pubmed:issn |
0379-0355
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
10
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
619-21
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:3236936-Animals,
pubmed-meshheading:3236936-Binding, Competitive,
pubmed-meshheading:3236936-Dioxolanes,
pubmed-meshheading:3236936-Dioxoles,
pubmed-meshheading:3236936-Male,
pubmed-meshheading:3236936-Parasympathomimetics,
pubmed-meshheading:3236936-Quinuclidines,
pubmed-meshheading:3236936-Quinuclidinyl Benzilate,
pubmed-meshheading:3236936-Rats,
pubmed-meshheading:3236936-Rats, Inbred Strains,
pubmed-meshheading:3236936-Receptors, Muscarinic
|
pubmed:year |
1988
|
pubmed:articleTitle |
Potency ratio for the inhibition of 3H-QNB and 3H-cis-methyldioxolane binding predicts agonist or antagonist activity on muscarinic receptors.
|
pubmed:affiliation |
Department of Biochemical Pharmacology, Centre de Recherche Pierre Fabre, Castre, France.
|
pubmed:publicationType |
Journal Article,
In Vitro
|