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Interaction of brain cannabinoid receptors with guanine nucleotide binding protein: a radioligand binding study.
Biochem Pharmacol. 1997 Dec 01; 54(11):1267-70.BP

Abstract

The binding of a classical cannabinoid agonist, [3H]R-(+)-(2,3-dihydro-5-methyl-3-[(4-morpholinyl)methyl]pyrol[1,2 ,3-de]-1,4-benzoxazin-6-yl)(1-napthalenyl)methanone monomethanesulfonate ([3H] WIN55212-2), and a selective cannabinoid receptor (CB1) antagonist, N-(piperidin-1-yl)-5-(4-chlorophenyl)1-(2,4-dichlorophenyl)-4-meth yl-1H-pyrazole-3-carboxamide hydrochloride ([3H]SR141716A), to rat cannabinoid receptors was evaluated using rat cerebellar membranes. Guanine nucleotides inhibited [3H]WIN55212-2 binding by approximately 50% at 10 microM and enhanced [3H]SR141716A binding very slightly. In the same tissue, the binding of guanosine 5'-O-[gamma-[35S]thio]triphosphate ([35S]GTP-gamma-S) was characterized and the influence of cannabinomimetics evaluated on this binding. Cannabinoid receptor agonists enhanced [35S]GTP-gamma-S binding, whereas SR141716A was devoid of action by itself but antagonized the action of cannabinoid receptor agonists. The good correlation obtained between the half maximum efficient concentration (EC50) values in [35S]GTP-gamma-S binding and the IC50 values [3H]WIN55212-2 binding shows that [35S]GTP-gamma-S binding could be a good functional assay for brain cannabinoid receptors.

Authors+Show Affiliations

Neurochemistry Department, Rhône-Poulenc Rorer S.A., Vitry-sur-Seine, France. francois.petitet@rp.frNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

9416978

Citation

Petitet, F, et al. "Interaction of Brain Cannabinoid Receptors With Guanine Nucleotide Binding Protein: a Radioligand Binding Study." Biochemical Pharmacology, vol. 54, no. 11, 1997, pp. 1267-70.
Petitet F, Jeantaud B, Capet M, et al. Interaction of brain cannabinoid receptors with guanine nucleotide binding protein: a radioligand binding study. Biochem Pharmacol. 1997;54(11):1267-70.
Petitet, F., Jeantaud, B., Capet, M., & Doble, A. (1997). Interaction of brain cannabinoid receptors with guanine nucleotide binding protein: a radioligand binding study. Biochemical Pharmacology, 54(11), 1267-70.
Petitet F, et al. Interaction of Brain Cannabinoid Receptors With Guanine Nucleotide Binding Protein: a Radioligand Binding Study. Biochem Pharmacol. 1997 Dec 1;54(11):1267-70. PubMed PMID: 9416978.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Interaction of brain cannabinoid receptors with guanine nucleotide binding protein: a radioligand binding study. AU - Petitet,F, AU - Jeantaud,B, AU - Capet,M, AU - Doble,A, PY - 1998/1/7/pubmed PY - 1998/1/7/medline PY - 1998/1/7/entrez SP - 1267 EP - 70 JF - Biochemical pharmacology JO - Biochem Pharmacol VL - 54 IS - 11 N2 - The binding of a classical cannabinoid agonist, [3H]R-(+)-(2,3-dihydro-5-methyl-3-[(4-morpholinyl)methyl]pyrol[1,2 ,3-de]-1,4-benzoxazin-6-yl)(1-napthalenyl)methanone monomethanesulfonate ([3H] WIN55212-2), and a selective cannabinoid receptor (CB1) antagonist, N-(piperidin-1-yl)-5-(4-chlorophenyl)1-(2,4-dichlorophenyl)-4-meth yl-1H-pyrazole-3-carboxamide hydrochloride ([3H]SR141716A), to rat cannabinoid receptors was evaluated using rat cerebellar membranes. Guanine nucleotides inhibited [3H]WIN55212-2 binding by approximately 50% at 10 microM and enhanced [3H]SR141716A binding very slightly. In the same tissue, the binding of guanosine 5'-O-[gamma-[35S]thio]triphosphate ([35S]GTP-gamma-S) was characterized and the influence of cannabinomimetics evaluated on this binding. Cannabinoid receptor agonists enhanced [35S]GTP-gamma-S binding, whereas SR141716A was devoid of action by itself but antagonized the action of cannabinoid receptor agonists. The good correlation obtained between the half maximum efficient concentration (EC50) values in [35S]GTP-gamma-S binding and the IC50 values [3H]WIN55212-2 binding shows that [35S]GTP-gamma-S binding could be a good functional assay for brain cannabinoid receptors. SN - 0006-2952 UR - https://www.unboundmedicine.com/medline/citation/9416978/Interaction_of_brain_cannabinoid_receptors_with_guanine_nucleotide_binding_protein:_a_radioligand_binding_study_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0006-2952(97)00384-5 DB - PRIME DP - Unbound Medicine ER -