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Ross 98, Forebrain vs. Intestine, Br J Pharmacol

Ross 98, Forebrain vs. Intestine, Br J Pharmacol

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Published by: Matias Ceballos Guzman on Dec 10, 2010
Copyright:Attribution Non-commercial

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08/11/2013

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Comparison of cannabinoid binding sites in guinea-pigforebrainand small intestine
1
Ruth A. Ross,
1
Heather C. Brockie,
1
Susanthi R. Fernando,
2
Bijali Saha,
2
Raj K.Razdan &
1,3
Roger G. Pertwee
1Department of Biomedical Sciences, Institute of Medical Sciences, University of Aberdeen, Foresterhill, AberdeenAB25 2ZDScotland; 2Organix Inc., 240 Salem Street, Woburn, Massachusetts 01801 U.S.A.1 We have investigated the nature of cannabinoid receptors in guinea-pig small intestine by establishingwhether this tissue contains cannabinoid receptors with similar binding properties to those receptors. Thecannabinoids used were antagonist SR144528, the novel cannabinoid the receptor CB1-selective ligand, antagonist 6'-azidohex-2'-yne-D8-tetrahydrocannabinolSR141716A, the of CBbrain 2-selectiveCB1(O-1184), and the agonists CP55940, which binds WIN55212-2, which shows marginal CB2selectivity.equally well to CB1and CB2receptors, and2 [3H]-CP55940 (1 nM) underwent extensive speci®c binding both to forebrain membranes (76.3%) andto membranes obtained by sucrose density gradient fractionation of homogenates of myenteric plexus-longitudinal muscle of guinea-pig small intestine (65.2%).3 (2092 Its fmol binding mg71). capacity However, (Bmaxthe ) (2.29 and 1.75 nMrespectively). was higher in forebrain (4281 fmol mg71) than in intestinal membranescorresponding KDvalues were not signi®cantly di erent from each other 1184, SR141716A and Nor SR144528 did from the forebrain Kivalues for its membranes displacement (0.87, by CP55940, 4.15, 2.85, WIN55212-2, 5.32 O-and 371.9respectively) di er signi®cantly from the intestinal membranes (0.99, 5.03, 3.16, 4.95 corresponding and 361.5 nMrespectively).K

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