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Bioorg Med Chem Lett. 2007 Apr 15;17(8):2184-7. Epub 2007 Feb 2.

Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.

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  • 1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.

Abstract

Sulfonamide analogues of the potent CB1R inverse agonist taranabant were prepared and optimized for potency and selectivity for CB1R. They were variably more potent than the corresponding amide analogues. The most potent representative 22 had good pharmacokinetic and brain levels, but was modestly active in blocking CB1R agonist-mediated hypothermia.

PMID:
17293109
[PubMed - indexed for MEDLINE]
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