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Evidence for both inverse agonism at the cannabinoid CB 1 receptor and the lack of an endogenous cannabinoid tone in the rat and guinea‐pig isolated ileum myenteric plexus‐longitudinal muscle preparation
Author(s) -
Makwana R,
Molleman A,
Parsons ME
Publication year - 2010
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.2010.00717.x
Subject(s) - cannabinoid , cannabinoid receptor , pharmacology , endocannabinoid system , inverse agonist , cannabinoid receptor agonists , rimonabant , anandamide , agonist , chemistry , cannabinoid receptor antagonist , depolarization induced suppression of inhibition , fatty acid amide hydrolase , medicine , endocrinology , am251 , receptor , biology , biochemistry
Cannabinoid receptor agonists reduce intestinal propulsion in rodents through the CB(1) receptor. In addition to its antagonistic activity at this receptor, rimonabant (N-(piperidino)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazole-carboxyamide) alone augments intestinal transit. Using rat and guinea-pig ileum MPLM (myenteric plexus-longitudinal muscle) preparations, we investigated whether the latter effect was through inverse agonism or antagonism of endocannabinoid agonist(s).