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Differences in G-protein activation by mu- and delta-opioid, and cannabinoid, receptors in rat striatum.
Eur J Pharmacol. 1996 Jun 20; 307(1):97-105.EJ

Abstract

Receptor activation of G-proteins can be measured by agonist-stimulated [35S]GTP gamma S binding in the presence of excess guanosine diphosphate (GDP). To determine whether opioid and cannabinoid receptor-mediated G-protein activation correlate with their receptor densities, this study compared opioid- and cannabinoid-stimulated [35S]guanylyl-5'-O-(gamma-thio)-triphosphate (GTP gamma S) binding with the corresponding Bmax values of receptor binding in rat striatum. Scatchard analysis revealed that the Bmax of cannabinoid receptor binding was approximately ten times higher than that of mu- or delta-opioid receptor binding. However, comparable levels of cannabinoid- and mu- and delta-opioid-stimulated [35S]GTP gamma S binding were observed in the caudate-putamen by [35S]GTP gamma S autoradiography in brain sections. Scatchard analysis of net agonist-stimulated [35S]GTP gamma S binding in membranes showed that the Bmax of cannabinoid-stimulated binding was only twice that of mu- or delta-opioid-stimulated binding. Thus, the calculated amplification factors for mu- and delta-opioid receptors are seven times that of cannabinoid receptors.

Authors+Show Affiliations

Department of Physiology and Pharmacology, Bowman Gray School of Medicine, Wake Forest University, Winston-Salem, NC 27157, USA.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

8831110

Citation

Sim, L J., et al. "Differences in G-protein Activation By Mu- and Delta-opioid, and Cannabinoid, Receptors in Rat Striatum." European Journal of Pharmacology, vol. 307, no. 1, 1996, pp. 97-105.
Sim LJ, Selley DE, Xiao R, et al. Differences in G-protein activation by mu- and delta-opioid, and cannabinoid, receptors in rat striatum. Eur J Pharmacol. 1996;307(1):97-105.
Sim, L. J., Selley, D. E., Xiao, R., & Childers, S. R. (1996). Differences in G-protein activation by mu- and delta-opioid, and cannabinoid, receptors in rat striatum. European Journal of Pharmacology, 307(1), 97-105.
Sim LJ, et al. Differences in G-protein Activation By Mu- and Delta-opioid, and Cannabinoid, Receptors in Rat Striatum. Eur J Pharmacol. 1996 Jun 20;307(1):97-105. PubMed PMID: 8831110.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Differences in G-protein activation by mu- and delta-opioid, and cannabinoid, receptors in rat striatum. AU - Sim,L J, AU - Selley,D E, AU - Xiao,R, AU - Childers,S R, PY - 1996/6/20/pubmed PY - 1996/6/20/medline PY - 1996/6/20/entrez SP - 97 EP - 105 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 307 IS - 1 N2 - Receptor activation of G-proteins can be measured by agonist-stimulated [35S]GTP gamma S binding in the presence of excess guanosine diphosphate (GDP). To determine whether opioid and cannabinoid receptor-mediated G-protein activation correlate with their receptor densities, this study compared opioid- and cannabinoid-stimulated [35S]guanylyl-5'-O-(gamma-thio)-triphosphate (GTP gamma S) binding with the corresponding Bmax values of receptor binding in rat striatum. Scatchard analysis revealed that the Bmax of cannabinoid receptor binding was approximately ten times higher than that of mu- or delta-opioid receptor binding. However, comparable levels of cannabinoid- and mu- and delta-opioid-stimulated [35S]GTP gamma S binding were observed in the caudate-putamen by [35S]GTP gamma S autoradiography in brain sections. Scatchard analysis of net agonist-stimulated [35S]GTP gamma S binding in membranes showed that the Bmax of cannabinoid-stimulated binding was only twice that of mu- or delta-opioid-stimulated binding. Thus, the calculated amplification factors for mu- and delta-opioid receptors are seven times that of cannabinoid receptors. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/8831110/Differences_in_G_protein_activation_by_mu__and_delta_opioid_and_cannabinoid_receptors_in_rat_striatum_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0014299996002117 DB - PRIME DP - Unbound Medicine ER -