Discovery of 5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole, a Novel in Vivo Cannabinoid Antagonist Containing a 1,2,4-Triazole Motif

A new series of 1,2,4-triazoles have been prepared and the evaluation of their cannabinoid properties have been carried out. Compound 8 showed cannabinoid silent antagonist activity in mouse vas deferens and guinea pig ileum preparations and in vivo assays (cannabinoid tetrad) in mouse. It did not h...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2004-05, Vol.47 (11), p.2939-2942
Main Authors: Jagerovic, Nadine, Hernandez-Folgado, Laura, Alkorta, Ibon, Goya, Pilar, Navarro, Miguel, Serrano, Antonia, Rodriguez de Fonseca, Fernando, Dannert, M. Teresa, Alsasua, Angela, Suardiaz, Margarita, Pascual, David, Martín, Maria Isabel
Format: Article
Language:English
Subjects:
Animals
Behavior, Animal - drug effects
Binding, Competitive
Biological and medical sciences
Cannabinoid Receptor Agonists
Cannabinoid Receptor Antagonists
Cerebellum - metabolism
Guinea Pigs
Ileum - drug effects
Ileum - physiology
In Vitro Techniques
Male
Medical sciences
Mice
Miscellaneous
Muscle Contraction - drug effects
Muscle, Smooth - drug effects
Muscle, Smooth - physiology
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Radioligand Assay
Rats
Triazoles - chemical synthesis
Triazoles - chemistry
Triazoles - pharmacology
Vas Deferens - drug effects
Vas Deferens - physiology
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Summary:A new series of 1,2,4-triazoles have been prepared and the evaluation of their cannabinoid properties have been carried out. Compound 8 showed cannabinoid silent antagonist activity in mouse vas deferens and guinea pig ileum preparations and in vivo assays (cannabinoid tetrad) in mouse. It did not have intrinsic activity in these bioassays, and therefore, it did not behave as a partial agonist or an inverse agonist.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm031099y