朝向大麻素受体 1（CB1）拮抗剂外周选择性的合理设计。
Towards rational design of cannabinoid receptor 1 (CB1) antagonists for peripheral selectivity.
机构信息
Pharmacology and Toxicology, RTI International, 3040 Cornwallis Rd., Research Triangle Park, NC 27709-2194, USA.
出版信息
Bioorg Med Chem Lett. 2011 Oct 1;21(19):5711-4. doi: 10.1016/j.bmcl.2011.08.032. Epub 2011 Aug 11.
Abstract
CB1 receptor antagonists that are peripherally restricted were targeted. Compounds with permanent charge as well as compounds that have increased polar surface area were made and tested against CB1 for binding and activity. Sulfonamide and sulfamide with high polar surface area and good activity at CB1 were rationally designed and pharmacologically tested. Further optimization of these compounds and testing could lead to the development of a new class of therapeutics to treat disorders where the CB1 receptor system has been implicated.
摘要
研究人员针对具有外周限制作用的 CB1 受体拮抗剂进行了研究。他们设计并合成了具有永久电荷和增加极性表面积的化合物，并对其与 CB1 的结合和活性进行了测试。研究人员还合理设计并药理学测试了具有高极性表面积和良好 CB1 活性的磺酰胺和磺酰胺类化合物。进一步优化这些化合物并进行测试，可能会开发出一类新的治疗药物，用于治疗与 CB1 受体系统有关的疾病。
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