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Molecular Pharmacology

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Research ArticleArticle

Selective Ligands and Cellular Effectors of a G Protein-Coupled Endothelial Cannabinoid Receptor

László Offertáler, Fong-Ming Mo, Sándor Bátkai, Jie Liu, Malcolm Begg, Raj K. Razdan, Billy R. Martin, Richard D. Bukoski and George Kunos
Molecular Pharmacology March 2003, 63 (3) 699-705; DOI: https://doi.org/10.1124/mol.63.3.699
László Offertáler
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Fong-Ming Mo
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Sándor Bátkai
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Jie Liu
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Malcolm Begg
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Raj K. Razdan
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Billy R. Martin
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Richard D. Bukoski
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George Kunos
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Abstract

The cannabinoid analog abnormal cannabidiol [abn-cbd; (−)-4-(3–3,4-trans-p-menthadien-[1,8]-yl)-olivetol] does not bind to CB1 or CB2 receptors, yet it acts as a full agonist in relaxing rat isolated mesenteric artery segments. Vasorelaxation by abn-cbd is endothelium-dependent, pertussis toxin-sensitive, and is inhibited by the BKCa channel inhibitor charybdotoxin, but not by the nitric-oxide synthase inhibitor N ω-nitro-l-arginine methyl ester or by the vanilloid VR1 receptor antagonist capsazepine. The cannabidiol analog O-1918 does not bind to CB1 or CB2 receptors and does not cause vasorelaxation at concentrations up to 30 μM, but it does cause concentration-dependent (1–30 μM) inhibition of the vasorelaxant effects of abn-cbd and anandamide. In anesthetized mice, O-1918 dose-dependently inhibits the hypotensive effect of abn-cbd but not the hypotensive effect of the CB1 receptor agonist (−)-11-OH-Δ9-tetrahydrocannabinol dimethylheptyl. In human umbilical vein endothelial cells, abn-cbd induces phosphorylation of p42/44 mitogen-activated protein kinase and protein kinase B/Akt, which is inhibited by O-1918, by pertussis toxin or by phosphatidylinositol 3 (PI3) kinase inhibitors. These findings indicate that abn-cbd is a selective agonist and that O-1918 is a selective, silent antagonist of an endothelial “anandamide receptor”, which is distinct from CB1 or CB2 receptors and is coupled through Gi/Go to the PI3 kinase/Akt signaling pathway.

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Molecular Pharmacology: 63 (3)
Molecular Pharmacology
Vol. 63, Issue 3
1 Mar 2003
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Research ArticleArticle

Selective Ligands and Cellular Effectors of a G Protein-Coupled Endothelial Cannabinoid Receptor

László Offertáler, Fong-Ming Mo, Sándor Bátkai, Jie Liu, Malcolm Begg, Raj K. Razdan, Billy R. Martin, Richard D. Bukoski and George Kunos
Molecular Pharmacology March 1, 2003, 63 (3) 699-705; DOI: https://doi.org/10.1124/mol.63.3.699

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Research ArticleArticle

Selective Ligands and Cellular Effectors of a G Protein-Coupled Endothelial Cannabinoid Receptor

László Offertáler, Fong-Ming Mo, Sándor Bátkai, Jie Liu, Malcolm Begg, Raj K. Razdan, Billy R. Martin, Richard D. Bukoski and George Kunos
Molecular Pharmacology March 1, 2003, 63 (3) 699-705; DOI: https://doi.org/10.1124/mol.63.3.699
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