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利莫那班:仅仅是一种减肥药?关于其多效性作用的当前证据。

Rimonabant: just an antiobesity drug? Current evidence on its pleiotropic effects.

作者信息

Bifulco Maurizio, Grimaldi Claudia, Gazzerro Patrizia, Pisanti Simona, Santoro Antonietta

机构信息

Department of Pharmaceutical Sciences, University of Salerno, Fisciano, Salerno, Italy.

出版信息

Mol Pharmacol. 2007 Jun;71(6):1445-56. doi: 10.1124/mol.106.033118. Epub 2007 Feb 27.

DOI:10.1124/mol.106.033118
PMID:17327463
Abstract

The advent of the highly selective cannabinoid receptor (CB1) antagonist, rimonabant (SR141716; Acomplia) can revolutionize the ability of the clinicians to manage obesity. Large-scale clinical trials have demonstrated that rimonabant therapy can reduce obesity. Although, the precise mechanisms of action of rimonabant have to be further dissected, it is emerging, from both preclinical and clinical research, that not only is rimonabant an antiobesity drug, but also its pleiotropic functions affect a broad range of diseases, from obesity-related comorbidities to drug dependence and cancer. Here we review recent data from the literature and discuss the full pharmacological potential of this drug.

摘要

高选择性大麻素受体(CB1)拮抗剂利莫那班(SR141716;Acomplia)的出现,可能会彻底改变临床医生治疗肥胖症的能力。大规模临床试验表明,利莫那班治疗可减轻肥胖。尽管利莫那班的确切作用机制还有待进一步剖析,但临床前和临床研究均显示,利莫那班不仅是一种抗肥胖药物,其多效性功能还会影响从肥胖相关合并症到药物依赖和癌症等多种疾病。在此,我们回顾文献中的最新数据,并探讨该药物的全部药理学潜力。

相似文献

1
Rimonabant: just an antiobesity drug? Current evidence on its pleiotropic effects.利莫那班:仅仅是一种减肥药?关于其多效性作用的当前证据。
Mol Pharmacol. 2007 Jun;71(6):1445-56. doi: 10.1124/mol.106.033118. Epub 2007 Feb 27.
2
Is the cannabinoid CB1 receptor antagonist rimonabant advancing the treatment of obesity?大麻素CB1受体拮抗剂利莫那班是否正在推动肥胖症的治疗?
Expert Opin Pharmacother. 2005 Oct;6(12):2141-4. doi: 10.1517/14656566.6.12.2141.
3
[Pharmacological therapy of obesity].[肥胖症的药物治疗]
G Ital Cardiol (Rome). 2008 Apr;9(4 Suppl 1):83S-93S.
4
Cannabinoid receptor 1 antagonist treatment induces glucagon release and shows an additive therapeutic effect with GLP-1 agonist in diet-induced obese mice.大麻素受体1拮抗剂治疗可诱导胰高血糖素释放,并在饮食诱导的肥胖小鼠中与胰高血糖素样肽-1激动剂显示出相加的治疗效果。
Can J Physiol Pharmacol. 2014 Dec;92(12):975-83. doi: 10.1139/cjpp-2014-0310. Epub 2014 Sep 29.
5
An overview of the metabolic effects of rimonabant in randomized controlled trials: potential for other cannabinoid 1 receptor blockers in obesity.利莫那班在随机对照试验中的代谢作用概述:其他大麻素 1 型受体阻滞剂在肥胖症中的应用潜力。
J Clin Pharm Ther. 2011 Feb;36(1):10-8. doi: 10.1111/j.1365-2710.2010.01164.x.
6
CB1 antagonists for obesity--what lessons have we learned from rimonabant?CB1 拮抗剂治疗肥胖——我们从利莫那班中学到了什么?
Nat Rev Endocrinol. 2009 Nov;5(11):633-8. doi: 10.1038/nrendo.2009.197.
7
[Rimonabant (Acomplia), specific inhibitor of the endocannabinoid system].[利莫那班(Acomplia),内源性大麻素系统的特异性抑制剂]
J Pharm Belg. 2005;60(3):89-91.
8
[Rimonabant (Acomplia)].利莫那班(Acomplia)
J Pharm Belg. 2008 Mar;63(1):27-8.
9
End of the line for cannabinoid receptor 1 as an anti-obesity target? An opinion.大麻素受体1作为抗肥胖靶点之路走到尽头了?一种观点。
Nat Rev Drug Discov. 2009 Jul;8(7):594. doi: 10.1038/nrd2775-c1.
10
Rimonabant: a selective blocker of the cannabinoid CB1 receptors for the management of obesity, smoking cessation and cardiometabolic risk factors.利莫那班:一种用于治疗肥胖、戒烟及心血管代谢危险因素的大麻素CB1受体选择性阻滞剂。
Expert Opin Investig Drugs. 2006 Mar;15(3):307-15. doi: 10.1517/13543784.15.3.307.

引用本文的文献

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Countering the Modern Metabolic Disease Rampage With Ancestral Endocannabinoid System Alignment.通过使内源性大麻素系统与祖先状态一致来对抗现代代谢疾病的肆虐。
Front Endocrinol (Lausanne). 2019 May 17;10:311. doi: 10.3389/fendo.2019.00311. eCollection 2019.
2
High-throughput screening for selective appetite modulators: A multibehavioral and translational drug discovery strategy.高通量筛选选择性食欲调节剂:一种多行为和转化的药物发现策略。
Sci Adv. 2018 Oct 31;4(10):eaav1966. doi: 10.1126/sciadv.aav1966. eCollection 2018 Oct.
3
Review: The Role of Cannabinoids on Esophageal Function-What We Know Thus Far.
综述:大麻素对食管功能的作用——目前我们所了解的情况。
Cannabis Cannabinoid Res. 2017 Oct 1;2(1):252-258. doi: 10.1089/can.2017.0031. eCollection 2017.
4
Role of cannabinoid receptor 1 in human adipose tissue for lipolysis regulation and insulin resistance.大麻素受体1在人体脂肪组织中对脂肪分解调节和胰岛素抵抗的作用。
Endocrine. 2017 Mar;55(3):839-852. doi: 10.1007/s12020-016-1172-6. Epub 2016 Nov 17.
5
Cannabinoid receptor CB1 regulates STAT3 activity and its expression dictates the responsiveness to SR141716 treatment in human glioma patients' cells.大麻素受体CB1调节信号转导和转录激活因子3(STAT3)的活性,其表达决定了人类胶质瘤患者细胞对SR141716治疗的反应性。
Oncotarget. 2015 Jun 20;6(17):15464-81. doi: 10.18632/oncotarget.3895.
6
RP-HPLC Method Development and Its Validation for Quantitative Determination of Rimonabant in Human Plasma.反相高效液相色谱法发展及其在人血浆中利莫那班定量测定的验证。
J Anal Methods Chem. 2012;2012:625979. doi: 10.1155/2012/625979. Epub 2012 Apr 23.
7
Plasma and brain pharmacokinetic profile of cannabidiol (CBD), cannabidivarine (CBDV), Δ⁹-tetrahydrocannabivarin (THCV) and cannabigerol (CBG) in rats and mice following oral and intraperitoneal administration and CBD action on obsessive-compulsive behaviour.大鼠和小鼠经口服和腹腔给药后,大麻二酚(CBD)、大麻二酚酸(CBDV)、Δ⁹-四氢大麻酚酸(THCV)和大麻环萜酚(CBG)的血浆和脑药代动力学特征及 CBD 对强迫症行为的作用。
Psychopharmacology (Berl). 2012 Feb;219(3):859-73. doi: 10.1007/s00213-011-2415-0. Epub 2011 Jul 28.
8
Gemcitabine/cannabinoid combination triggers autophagy in pancreatic cancer cells through a ROS-mediated mechanism.吉西他滨/大麻素联合通过 ROS 介导的机制触发胰腺癌细胞自噬。
Cell Death Dis. 2011 Apr 28;2(4):e152. doi: 10.1038/cddis.2011.36.
9
Perspectives of CB1 Antagonist in Treatment of Obesity: Experience of RIO-Asia.CB1拮抗剂在肥胖治疗中的前景:亚洲地区RIO研究经验
J Obes. 2011;2011:957268. doi: 10.1155/2011/957268. Epub 2010 Dec 29.
10
Synthesis and biological evaluation of bivalent ligands for the cannabinoid 1 receptor.合成和生物评价大麻素 1 受体的双价配体。
J Med Chem. 2010 Oct 14;53(19):7048-60. doi: 10.1021/jm1006676.