CANNABINOID RECEPTOR CB1 ANTAGONISTS: STATE OF THE ART AND CHALLENGES

被引:16
作者
Bifulco, Maurizio [1 ]
Santoro, Antonietta [1 ]
Laezza, Chiara [2 ]
Malfitano, Anna Maria [1 ]
机构
[1] Univ Salerno, Dipartimento Sci Farmaceut, I-84100 Salerno, Italy
[2] CNR, Ist Endocrinol & Oncol Sperimentale, I-80125 Naples, Italy
来源
VITAMINS AND HORMONES: ANANDAMIDE AN ENDOGENOUS CANNABINOID | 2009年 / 81卷
关键词
CARDIOMETABOLIC RISK-FACTORS; ENDOCANNABINOID SYSTEM; INVERSE AGONIST; IN-VIVO; CELL-PROLIFERATION; SELECTIVE ANTAGONIST; OVERWEIGHT PATIENTS; METABOLIC SYNDROME; ABDOMINAL OBESITY; ADIPOSE-TISSUE;
D O I
10.1016/S0083-6729(09)81007-8
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
070307 [化学生物学]; 071010 [生物化学与分子生物学];
摘要
The discovery of cannabinoid receptors led to the development of several compounds targeted against these receptors. In particular, CB1 receptor antagonists have been described to possess key functions in the treatment of obesity and obesity-related pathologies. Numerous clinical trials revealed the advantage of strategies designed to block CB1 receptor but also evidenced the limitations due to side effects exerted by these substances. Recent studies have highlighted that CB1 antagonists could have other effects and find applications even in other pathologies like hepatic fibrosis, chronic inflammatory conditions, diabetes, and cancer. Since the suspending sales of the lead compound, rimonabant, and the discontinuation of all ongoing clinical trials of CB1 blockers, alternative strategies could emerge and lead to the development of further basic research studies to redirect these compounds.
引用
收藏
页码:159 / 189
页数:31
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