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Comparison of cannabinoid ligands affinities and efficacies in murine tissues and in transfected cells expressing human recombinant cannabinoid receptors.
Eur J Pharm Sci. 2004 Nov; 23(3):233-43.EJ

Abstract

Affinities and efficacies of several reference cannabinoid ligands were investigated at central and peripheral cannabinoid receptors in three different species (rat, mouse, and human). The tested compounds belong to different chemical classes such as classical and non-classical terpene derivatives (Delta(8)-THC, Delta(9)-THC, HU 210, CP 55,940, CP 55,244, CP 55,243 and CP 47,947), aminoalkylindole (WIN 55,212-2, WIN 55,212-3) and diarylpyrazole cannabinoids (SR 141716A, SR 144528). As cannabinoid receptors have been shown to be mainly coupled to Gi/o type G- proteins, and by using the [(35)S]-GTPgammaS nucleotide binding modulation, we characterized the functional activity of these ligands which can act as agonists (positive intrinsic activity), partial agonists (partial positive intrinsic activity), antagonists (no intrinsic activity), or inverse agonists (negative intrinsic activity). To our knowledge, some derivatives (Delta(8)-THC, WIN 55,212-3, CP 55,243 and CP 47,947) have never been characterized in [(35)S]-GTPgammaS binding assays and up to now, this study represents the largest survey of reference cannabinoids performed in unique experimental conditions and in the same laboratory.

Authors+Show Affiliations

Unité de Chimie Pharmaceutique et de Radiopharmacie, Ecole de Pharmacie, Université catholique de Louvain, 73 Avenue E. Mounier, B-1200 Brussels, Belgium.No affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15489124

Citation

Govaerts, Sophie J., et al. "Comparison of Cannabinoid Ligands Affinities and Efficacies in Murine Tissues and in Transfected Cells Expressing Human Recombinant Cannabinoid Receptors." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 23, no. 3, 2004, pp. 233-43.
Govaerts SJ, Hermans E, Lambert DM. Comparison of cannabinoid ligands affinities and efficacies in murine tissues and in transfected cells expressing human recombinant cannabinoid receptors. Eur J Pharm Sci. 2004;23(3):233-43.
Govaerts, S. J., Hermans, E., & Lambert, D. M. (2004). Comparison of cannabinoid ligands affinities and efficacies in murine tissues and in transfected cells expressing human recombinant cannabinoid receptors. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 23(3), 233-43.
Govaerts SJ, Hermans E, Lambert DM. Comparison of Cannabinoid Ligands Affinities and Efficacies in Murine Tissues and in Transfected Cells Expressing Human Recombinant Cannabinoid Receptors. Eur J Pharm Sci. 2004;23(3):233-43. PubMed PMID: 15489124.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparison of cannabinoid ligands affinities and efficacies in murine tissues and in transfected cells expressing human recombinant cannabinoid receptors. AU - Govaerts,Sophie J, AU - Hermans,Emmanuel, AU - Lambert,Didier M, PY - 2004/04/03/received PY - 2004/07/08/revised PY - 2004/07/26/accepted PY - 2004/10/19/pubmed PY - 2005/5/25/medline PY - 2004/10/19/entrez SP - 233 EP - 43 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 23 IS - 3 N2 - Affinities and efficacies of several reference cannabinoid ligands were investigated at central and peripheral cannabinoid receptors in three different species (rat, mouse, and human). The tested compounds belong to different chemical classes such as classical and non-classical terpene derivatives (Delta(8)-THC, Delta(9)-THC, HU 210, CP 55,940, CP 55,244, CP 55,243 and CP 47,947), aminoalkylindole (WIN 55,212-2, WIN 55,212-3) and diarylpyrazole cannabinoids (SR 141716A, SR 144528). As cannabinoid receptors have been shown to be mainly coupled to Gi/o type G- proteins, and by using the [(35)S]-GTPgammaS nucleotide binding modulation, we characterized the functional activity of these ligands which can act as agonists (positive intrinsic activity), partial agonists (partial positive intrinsic activity), antagonists (no intrinsic activity), or inverse agonists (negative intrinsic activity). To our knowledge, some derivatives (Delta(8)-THC, WIN 55,212-3, CP 55,243 and CP 47,947) have never been characterized in [(35)S]-GTPgammaS binding assays and up to now, this study represents the largest survey of reference cannabinoids performed in unique experimental conditions and in the same laboratory. SN - 0928-0987 UR - https://www.unboundmedicine.com/medline/citation/15489124/Comparison_of_cannabinoid_ligands_affinities_and_efficacies_in_murine_tissues_and_in_transfected_cells_expressing_human_recombinant_cannabinoid_receptors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(04)00198-8 DB - PRIME DP - Unbound Medicine ER -