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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Guagnini, F. Rinaldi-carmona, M. Mukenge, S. Ferla, G. Croci, T. Manara, L. Aureggi, G. Le Fur, G. Maffrand, J. P. |
| Description | Author Affiliation: Croci T ( Research Center Sanofi Midy, Milan, Italy.) |
| Abstract | We investigated the effect of the cannabinoid agonist (+)WIN-55212-2 on human ileum longitudinal smooth muscle preparations, either electrically stimulated or contracted by carbachol. Electrical field stimulation mostly activated cholinergic neurons, since atropine and tetrodotoxin (TTX), alone or coincubated, reduced twitch responses to a similar degree (85%). (+)WIN-55212-2 concentration-dependently inhibited twitch responses (IC50 73 nM), but had no additive effect with atropine or TTX. The cannabinoid CB1 receptor antagonist SR 141716 (pA2 8.2), but not the CB2 receptor antagonist, SR 144528, competitively antagonized twitch inhibition by (+)WIN-55212-2. Atropine but not (+)WIN-55212-2 or TTX prevented carbachol-induced tonic contraction. These results provide functional evidence of the existence of prejunctional cannabinoid CB1-receptors in the human ileum longitudinal smooth muscle. Agonist activation of these receptors prevents responses to electrical field stimulation, presumably by inhibiting acetylcholine release. SR 141716 is a potent and competitive antagonist of cannabinoid CB1 receptors naturally expressed in the human gut. |
| ISSN | 00071188 |
| e-ISSN | 14765381 |
| Journal | British Journal of Pharmacology |
| Issue Number | 7 |
| Volume Number | 125 |
| Language | English |
| Publisher | Wiley Online Library(on behalf of The British Pharmacological Society) |
| Publisher Date | 1998-12-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | Open |
| Subject Keyword | Ileum Metabolism Muscle, Smooth Receptors, Drug Benzoxazines Calcium Channel Blockers Pharmacology Carbachol Dose-Response Relationship, Drug Electric Stimulation Drug Effects In Vitro Techniques Morpholines Muscle Contraction Naphthalenes Neurons Piperidines Pyrazoles Receptors, Cannabinoid Antagonists & Inhibitors Tetrodotoxin |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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