Literature DB >> 9346339

SR141716A is an inverse agonist at the human cannabinoid CB1 receptor.

R S Landsman1, T H Burkey, P Consroe, W R Roeske, H I Yamamura.   

Abstract

The effects of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4- benzoxazin-yl]-(1-napthalenyl)methanone mesylate (WIN 55,212-2) and N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazo le-carboxamide (SR141716A) on guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS) binding to membranes isolated from human cannabinoid CB1 receptor-transfected Chinese hamster ovary (CHO) cells were examined. WIN 55,212-2 stimulated [35S]GTPgammaS binding 76.3% above basal levels whereas SR141716A produced a 22.3% decrease in basal [35S]GTPgammaS binding. These findings demonstrate that WIN 55,212-2 is an agonist and SR141716A is an inverse agonist in this system.

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Year:  1997        PMID： 9346339     DOI： 10.1016/s0014-2999(97)01160-6

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  75 in total

1.  Pharmacological analysis of cannabinoid receptor activity in the rat vas deferens.

Authors:  A Christopoulos; P Coles; L Lay; M J Lew; J A Angus
Journal:  Br J Pharmacol       Date:  2001-03       Impact factor: 8.739

2.  Structural domains of the CB1 cannabinoid receptor that contribute to constitutive activity and G-protein sequestration.

Authors:  J Nie; D L Lewis
Journal:  J Neurosci       Date:  2001-11-15       Impact factor: 6.167

3.  Δ9-tetrahydrocannabinol and endocannabinoid degradative enzyme inhibitors attenuate intracranial self-stimulation in mice.

Authors:  Jason M Wiebelhaus; Travis W Grim; Robert A Owens; Matthew F Lazenka; Laura J Sim-Selley; Rehab A Abdullah; Micah J Niphakis; Robert E Vann; Benjamin F Cravatt; Jenny L Wiley; S Stevens Negus; Aron H Lichtman
Journal:  J Pharmacol Exp Ther       Date:  2014-11-14       Impact factor: 4.030

4.  Are CB(1) Receptor Antagonists Nootropic or Cognitive Impairing Agents?

Authors:  Stephen A Varvel; Laura E Wise; Aron H Lichtman
Journal:  Drug Dev Res       Date:  2009-12-01       Impact factor: 4.360

5.  Modulation of the release of endogenous adenosine by cannabinoids in the myenteric plexus-longitudinal muscle preparation of the guinea-pig ileum.

Authors:  M Begg; N Dale; E Llaudet; A Molleman; M E Parsons
Journal:  Br J Pharmacol       Date:  2002-12       Impact factor: 8.739

Review 6.  Efficacy in CB1 receptor-mediated signal transduction.

Authors:  Allyn C Howlett
Journal:  Br J Pharmacol       Date:  2004-08       Impact factor: 8.739

Review 7.  Cannabinoid CB1 receptor-interacting proteins: novel targets for central nervous system drug discovery?

Authors:  Tricia H Smith; Laura J Sim-Selley; Dana E Selley
Journal:  Br J Pharmacol       Date:  2010-06       Impact factor: 8.739

8.  A novel peripherally restricted cannabinoid receptor antagonist, AM6545, reduces food intake and body weight, but does not cause malaise, in rodents.

Authors:  N L Cluny; V K Vemuri; A P Chambers; C L Limebeer; H Bedard; J T Wood; B Lutz; A Zimmer; L A Parker; A Makriyannis; K A Sharkey
Journal:  Br J Pharmacol       Date:  2010-10       Impact factor: 8.739

9.  Disruption of CB(1) receptor signaling impairs extinction of spatial memory in mice.

Authors:  S A Varvel; E A Anum; A H Lichtman
Journal:  Psychopharmacology (Berl)       Date:  2004-12-24       Impact factor: 4.530

Review 10.  Activation of G-proteins in brain by endogenous and exogenous cannabinoids.

Authors:  Steven R Childers
Journal:  AAPS J       Date:  2006-03-10       Impact factor: 4.009
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