Prejunctional and peripheral effects of the cannabinoid CB1 receptor inverse agonist rimonabant (SR 141716)
نویسندگان
چکیده
منابع مشابه
SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist.
In the present report, we investigated in detail the effects of SR 144528, a selective antagonist of the peripheral cannabinoid receptor (CB2), on two well-characterized functions mediated by CB2: the induction of the early response gene krox24 and the inhibition of adenylyl cyclase. We generated Chinese hamster ovary cells doubly transfected with human CB2 and a luciferase reporter gene linked...
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Introduction: The hypoxic state, in which experimental animals were subjected to an atmosphere of 5% O2 and %95 N2, has been used to screen agents for possible cerebral protection by measuring their ability to prolong survival time in mice exposed to hypoxia. Researchers showed that rimonabant and AM251 allosteric potentiate all but the β1 subunit containing GABAA receptors at nM...
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To date, the endogenous ligands described for cannabinoid receptors have been derived from membrane lipids. To identify a peptide ligand for CB(1) cannabinoid receptors, we used the recently described conformation-state sensitive antibodies and screened a panel of endogenous peptides from rodent brain or adipose tissue. This led to the identification of hemopressin (PVNFKFLSH) as a peptide liga...
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We have investigated the adaptive changes of the human central cannabinoid receptor (CB1) stably expressed in Chinese hamster ovary cells (CHO-CB1), after agonist (CP 55,940) or selective CB1 inverse agonist (SR 141716) treatment. CB1 receptor density and affinity constant as measured by binding assays with both tritiated ligands remained essentially unchanged after varying period exposure of C...
متن کاملA method for parallel solid-phase synthesis of iodinated analogues of the CB1 receptor inverse agonist rimonabant.
A method for the parallel solid-phase synthesis (SPS) of iodinated analogues of Sanofi-Aventis' type 1 cannabinoid (CB1) receptor inverse agonist rimonabant (acomplia) has been developed. The method allows the synthesis of a range of C3 amide/hydrazide derivatives from a resin-bound C3 ester precursor. The C-Ge linkage to the Hypogel-200 resin is stable to the diversification conditions but all...
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ژورنال
عنوان ژورنال: Naunyn-Schmiedeberg's Archives of Pharmacology
سال: 2008
ISSN: 0028-1298,1432-1912
DOI: 10.1007/s00210-008-0327-2