Cannabinoid receptor 1 antagonist Rimonabant attenuates mu-opiod receptor G-protein activation in mice forebrain
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1
Hung Acad Sci., Inst Biochem, Biol Res Ctr, Hungary
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2
Univ of Heidelberg Im Neuenheimer Feld, Pharm Inst, Germany
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3
Semmelweis Univ, Dept Human Morphol & Develop Biol, Hungary
Opioids, cannabinoids and their receptors are well known for their overlapping pharmacological properties. These two systems are in tight interactions partly achieving their effects by altering each others receptor activity via direct and/or indirect mechanisms. A prototype cannabinoid-CB(1) receptor antagonist SR141716 (Rimonabant) is known as anorectic, anti-obesity drug. Our aim was to investigated the effect of acute, intraperitoneal (i.p.) Rimonabant treatment on mu-opioid receptor (MOR) activation performing functional [35S]GTPgammaS binding assays and the direct binding of Rimonabant to MORs applying radioligand binding competition experiments in the forebrain of CB(1) receptor knockout (CB(1) –/–) mice. For both functional and receptor binding assays, we have used [d-Ala2,NMePhe4,Gly5-ol]enkephalin (DAMGO), a synthetic peptide ligand with excellent MOR specifity. Acute i.p. injection of Rimonabant caused prominent decrease in the aspect of MORs G-protein activation both in CB(1)+/+ wild type and CB(1) –/– forebrain. Direct application of 1microM Rimonabant also signifiacantly decreased the efficacy of DAMGO in both types of forebrain tissues. In competition binding assay we haven’t seen any direct effect of Rimonabant on MOR binding sites both in CB(1)+/+ and in CB(1) –/– forebrain membrane fractions. Based on our data we assume that Rimonabant causes attenuation on the level of MOR G-protein activation without binding directly to the MORs.
Keywords:
Neuroendocrinology,
Neuroscience
Conference:
13th Conference of the Hungarian Neuroscience Society (MITT), Budapest, Hungary, 20 Jan - 22 Jan, 2011.
Presentation Type:
Abstract
Topic:
Neuroendocrinology
Citation:
Zádor
F,
Páldy
E,
Wenger
T and
Benyhe
S
(2011). Cannabinoid receptor 1 antagonist Rimonabant attenuates mu-opiod receptor G-protein activation in mice forebrain.
Front. Neurosci.
Conference Abstract:
13th Conference of the Hungarian Neuroscience Society (MITT).
doi: 10.3389/conf.fnins.2011.84.00075
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Received:
03 Mar 2011;
Published Online:
23 Mar 2011.
*
Correspondence:
Dr. F. Zádor, Hung Acad Sci., Inst Biochem, Biol Res Ctr, Szeged, Hungary, mcferenc@gmail.com