期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 2, 页码 234-237出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm8012932
关键词
-
资金
- Pfizer, Inc.
We report the structure-activity relationships, design, and synthesis of the novel cannabinoid type 1 (CB1) receptor antagonist 3a (CP-945,598). Compound 3a showed subnanomolar potency at human CB1 receptors in binding (K-i = 0.7 nM) and functional assays (K-i = 0.12 nM). In vivo, compound 3a reversed cannabinoid agonist-mediated responses, reduced food intake, and increased energy expenditure and fat oxidation in rodents.
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