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Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Apr 15; Vol. 17 (8), pp. 2184-7. Date of Electronic Publication: 2007 Feb 02. - Publication Year :
- 2007
-
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.
- Subjects :
- Animals
Anti-Obesity Agents chemical synthesis
Anti-Obesity Agents pharmacology
Brain Chemistry
Cannabinoid Receptor Modulators pharmacology
Humans
Hypothermia drug therapy
Inhibitory Concentration 50
Pharmacokinetics
Rats
Receptor, Cannabinoid, CB1 agonists
Structure-Activity Relationship
Sulfonamides pharmacology
Cannabinoid Receptor Modulators chemical synthesis
Receptor, Cannabinoid, CB1 drug effects
Sulfonamides chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17293109
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.01.087