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J Med Chem. 2004 May 20;47(11):2939-42.

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.

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  • 1Instituto de Química Médica, Consejo Superior de Investigaciones Científicas, Juan de la Cierva, 3, E-28006 Madrid, Spain. nadine@iqm.csic.es

Abstract

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.

PMID:
15139773
[PubMed - indexed for MEDLINE]
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