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SR141716A, a potent and selective antagonist of the brain cannabinoid receptor
Expression of central and peripheral cannabinoid receptors in human immune tissues and leukocyte subpopulations.
The results suggest that CB1 and CB2 can be considered as tissue-selective antigens of the central nervous system and immune system, respectively, and cannabinoids may exert specific receptor-mediated actions on the immune system through the CB2 receptor.
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
- M. Rinaldi-Carmona, F. Barth, G. Le Fur
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 February 1998
It is expected that SR 144528 will provide a powerful tool to investigate the in vivo functions of the cannabinoid system in the immune response.
Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1.
It is shown here that cannabinoid treatment induces both phosphorylation and activation of mitogen-activated protein (MAP) kinases, and that these effects are inhibited by SR 141716A, a selective CB1 antagonist.
A Selective Inverse Agonist for Central Cannabinoid Receptor Inhibits Mitogen-activated Protein Kinase Activation Stimulated by Insulin or Insulin-like Growth Factor 1
- M. Bouaboula, Sylvie Perrachon, P. Casellas
- Biology, ChemistryThe Journal of Biological Chemistry
- 29 August 1997
Chinese hamster ovary cells transfected with human central cannabinoid receptor (CB1) exhibit high constitutive activity at both levels of mitogen-activated protein kinase (MAPK) and adenylyl cyclase, and the CB1-selective ligand, SR 141716A, that functions as an inverse agonist is proposed as a novel model for receptor/ligand interactions.
Anandamide induced PPARgamma transcriptional activation and 3T3-L1 preadipocyte differentiation.
The cannabinoid CB1 receptor antagonist SR141716 increases Acrp30 mRNA expression in adipose tissue of obese fa/fa rats and in cultured adipocyte cells.
Results show that SR141716 stimulated Acrp30 mRNA expression in adipose tissue by an effect on adipocytes, and reduced hyperinsulinemia in obese (fa/fa) rats, and suggest a role of metabolic regulation in the antiobesity effect of SR 141716.
The CB1 receptor antagonist rimonabant reverses the diet‐induced obesity phenotype through the regulation of lipolysis and energy balance
- O. Jbilo, C. Ravinet-Trillou, P. Casellas
- BiologyFASEB journal : official publication of the…
- 1 September 2005
The data clearly indicated that SR141716 reversed the phenotype of obese adipocytes at both macroscopic and genomic levels, and strongly indicate that the endocannabinoid system has a major role in the regulation of energy metabolism.
Signaling pathway associated with stimulation of CB2 peripheral cannabinoid receptor. Involvement of both mitogen-activated protein kinase and induction of Krox-24 expression.
Findings provide evidence for a functional role of the CB2 receptor in gene induction mediated by the MAP kinase network in time- and dose-dependent manners.
Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors.
- C. Serradeil-Le Gal, J. Wagnon, G. Le Fur
- Biology, MedicineThe Journal of clinical investigation
- 1 July 1993
SR 49059 is the most potent and selective nonpeptide AVP V1a antagonist described so far, with marked affinity, selectivity, and efficacy toward both animal and human receptors.