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

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Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, Guthikonda R, Truong Q, Chang LL, Quaker G, Colandrea VJ, Tong X, Wang J, Xu S, Fong TM, Shen CP, Lao J, Chen J, Shearman LP, Stribling DS, Rosko K, Strack A, Ha S, Van der Ploeg L, Goulet MT, Hagmann WK

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

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

PubMed ID
17293109 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RimonabantCannabinoid receptor 1IC 50 (nM)6.1N/AN/ADetails