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rdf:type |
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lifeskim:mentions |
umls-concept:C0001613,
umls-concept:C0007776,
umls-concept:C0013227,
umls-concept:C0022655,
umls-concept:C0027849,
umls-concept:C0034792,
umls-concept:C0034826,
umls-concept:C0205345,
umls-concept:C0270699,
umls-concept:C0456603,
umls-concept:C0599278,
umls-concept:C0682002,
umls-concept:C0682770,
umls-concept:C0918012,
umls-concept:C1510827,
umls-concept:C1744687
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pubmed:issue |
2
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pubmed:dateCreated |
1988-5-27
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pubmed:abstractText |
1. Radioligand binding assays using [3H]-N-methylscopolamine (NMS) and [3H]-oxotremorine M (Oxo-M) have been devised to predict the efficacy of test compounds at muscarinic receptors in rat cerebral cortex. 2. Muscarinic antagonists, including non-selective and both M1- and M2-selective compounds, displayed similar affinity for both binding assays. 3. Full agonists such as carbachol and muscarine possessed a ratio of potencies against the antagonist versus the agonist ligand (NMS/Oxo-M ratio) of greater than 4000. 4. Compounds which have been shown previously to display partial agonist activity in functional assays e.g. pilocarpine and RS86 had intermediate NMS/Oxo-M ratios of 100-150. A second group of compounds which included oxotremorine had somewhat higher ratios (500-1400). 5. The ratio of affinity constants for the two assays predicted the ability of agonists to stimulate cortical phosphatidyl-inositol turnover. 6. These results suggest that the NMS/Oxo-M ratio may be a useful prediction of efficacy for novel compounds acting at cortical muscarinic receptors.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-13743787,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-14907713,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-2411866,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-2937502,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-2981282,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-2982089,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-3004418,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-3546321,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-3585909,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-3732391,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-3754580,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-3754610,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-3754611,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-3762520,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-3839571,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-4058422,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-4202581,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-6088696,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-6102394,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-6188035,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-6323632,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-6418552,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-686171,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-6863248,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-714021,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-714022,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-7350532,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3359114-954813
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
93
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
437-45
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:3359114-Animals,
pubmed-meshheading:3359114-Binding, Competitive,
pubmed-meshheading:3359114-Cerebral Cortex,
pubmed-meshheading:3359114-Inositol,
pubmed-meshheading:3359114-Male,
pubmed-meshheading:3359114-N-Methylscopolamine,
pubmed-meshheading:3359114-Oxotremorine,
pubmed-meshheading:3359114-Phospholipids,
pubmed-meshheading:3359114-Rats,
pubmed-meshheading:3359114-Receptors, Cholinergic,
pubmed-meshheading:3359114-Receptors, Muscarinic,
pubmed-meshheading:3359114-Scopolamine Derivatives,
pubmed-meshheading:3359114-Synaptosomes
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pubmed:year |
1988
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pubmed:articleTitle |
Relative affinities of drugs acting at cholinoceptors in displacing agonist and antagonist radioligands: the NMS/Oxo-M ratio as an index of efficacy at cortical muscarinic receptors.
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pubmed:affiliation |
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex.
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pubmed:publicationType |
Journal Article,
In Vitro
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