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Pharmacological characterization of receptor types mediating the dilator action of anandamide on blood vessels of the rat knee joint.
Life Sci. 2007 Mar 27; 80(16):1495-502.LS

Abstract

This study investigates the actions of N-(2-hydroxyethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide (anandamide) on blood flow of the rat knee joint. Topical bolus administration of anandamide (10-1000 nmol) onto the exposed knee joint capsules produced dose-dependent increases in the knee joint blood flow. Various antagonists were tested on the vasodilator response to 100 nmol anandamide. Capsazepine (N-[2-(4-chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide), an antagonist of the transient receptor potential vanilloid type 1 (TRPV1) receptor, given at 10 and 100 nmol, suppressed the response by a maximum of 71%. A cannabinoid CB(1) receptor antagonist AM281 (10 nmol) and a CB(2) receptor antagonist AM630 (10 nmol) shortened its duration from 15 min to 5 min. O-1918 (1 nmol), an antagonist of the putative endothelial anandamide/abnormal-cannabidiol receptor, on its own or combined with capsazepine and the two cannabinoid receptor antagonists produced 38% and 24% inhibition on the peak vasodilator response to anandamide, respectively. URB597 (1 nmol), an inhibitor of fatty acid amide hydrolase (FAAH) suppressed the response by 40%, and an anandamide transporter inhibitor [N-(4-hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide] (AM404; 1 nmol) or a cyclo-oxygenase (COX) inhibitor flurbiprofen (20 nmol) abolished the response. These findings suggest the vasodilator action of anandamide in the rat knee joint involved hydrolysis of the compound by FAAH, production of COX-derived eicosanoid(s), activation of TRPV1 receptors, and a small component involved activation of endothelial anandamide/abnormal-cannabidiol receptors; a minor delayed dilator response was mediated by activation of conventional cannabinoid receptors.

Authors+Show Affiliations

Li Ka Shing Institute of Health Sciences, and The Department of Pharmacology, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong. FrancisLam@cuhk.edu.hk <FrancisLam@cuhk.edu.hk>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

17275857

Citation

Lam, Francis F Y., et al. "Pharmacological Characterization of Receptor Types Mediating the Dilator Action of Anandamide On Blood Vessels of the Rat Knee Joint." Life Sciences, vol. 80, no. 16, 2007, pp. 1495-502.
Lam FF, Luk PW, Ng ES. Pharmacological characterization of receptor types mediating the dilator action of anandamide on blood vessels of the rat knee joint. Life Sci. 2007;80(16):1495-502.
Lam, F. F., Luk, P. W., & Ng, E. S. (2007). Pharmacological characterization of receptor types mediating the dilator action of anandamide on blood vessels of the rat knee joint. Life Sciences, 80(16), 1495-502.
Lam FF, Luk PW, Ng ES. Pharmacological Characterization of Receptor Types Mediating the Dilator Action of Anandamide On Blood Vessels of the Rat Knee Joint. Life Sci. 2007 Mar 27;80(16):1495-502. PubMed PMID: 17275857.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacological characterization of receptor types mediating the dilator action of anandamide on blood vessels of the rat knee joint. AU - Lam,Francis F Y, AU - Luk,Phoebe W S, AU - Ng,Ethel S K, Y1 - 2007/01/18/ PY - 2006/07/01/received PY - 2006/12/16/revised PY - 2007/01/10/accepted PY - 2007/2/6/pubmed PY - 2007/6/29/medline PY - 2007/2/6/entrez SP - 1495 EP - 502 JF - Life sciences JO - Life Sci. VL - 80 IS - 16 N2 - This study investigates the actions of N-(2-hydroxyethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide (anandamide) on blood flow of the rat knee joint. Topical bolus administration of anandamide (10-1000 nmol) onto the exposed knee joint capsules produced dose-dependent increases in the knee joint blood flow. Various antagonists were tested on the vasodilator response to 100 nmol anandamide. Capsazepine (N-[2-(4-chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide), an antagonist of the transient receptor potential vanilloid type 1 (TRPV1) receptor, given at 10 and 100 nmol, suppressed the response by a maximum of 71%. A cannabinoid CB(1) receptor antagonist AM281 (10 nmol) and a CB(2) receptor antagonist AM630 (10 nmol) shortened its duration from 15 min to 5 min. O-1918 (1 nmol), an antagonist of the putative endothelial anandamide/abnormal-cannabidiol receptor, on its own or combined with capsazepine and the two cannabinoid receptor antagonists produced 38% and 24% inhibition on the peak vasodilator response to anandamide, respectively. URB597 (1 nmol), an inhibitor of fatty acid amide hydrolase (FAAH) suppressed the response by 40%, and an anandamide transporter inhibitor [N-(4-hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide] (AM404; 1 nmol) or a cyclo-oxygenase (COX) inhibitor flurbiprofen (20 nmol) abolished the response. These findings suggest the vasodilator action of anandamide in the rat knee joint involved hydrolysis of the compound by FAAH, production of COX-derived eicosanoid(s), activation of TRPV1 receptors, and a small component involved activation of endothelial anandamide/abnormal-cannabidiol receptors; a minor delayed dilator response was mediated by activation of conventional cannabinoid receptors. SN - 0024-3205 UR - https://www.unboundmedicine.com/medline/citation/17275857/Pharmacological_characterization_of_receptor_types_mediating_the_dilator_action_of_anandamide_on_blood_vessels_of_the_rat_knee_joint_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0024-3205(07)00043-4 DB - PRIME DP - Unbound Medicine ER -