使用生物测定法评估高效力植物大麻素以确定大麻素受体1和大麻素受体2的构效关系
Evaluation of Phytocannabinoids from High Potency using Bioassays to Determine Structure-Activity Relationships for Cannabinoid Receptor 1 and Cannabinoid Receptor 2.
作者信息
Husni Afeef S, McCurdy Christopher R, Radwan Mohamed M, Ahmed Safwat A, Slade Desmond, Ross Samir A, ElSohly Mahmoud A, Cutler Stephen J
机构信息
Department of Medicinal Chemistry, School of Pharmacy, University of Mississippi, University, MS 38677, USA.
Department of Medicinal Chemistry, School of Pharmacy, University of Mississippi, University, MS 38677, USA ; National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University Mississippi 38677, USA.
出版信息
Med Chem Res. 2014 Sep 1;23(9):4295-4300. doi: 10.1007/s00044-014-0972-6.
has been around for thousands of years and has been used recreationally, medicinally, and for fiber. Over 500 compounds have been isolated from with approximately 105 being cannabinoids. Of those 105 compounds, Δ-tetrahydrocannabinol has been determined as the primary constituent, which is also responsible for the psychoactivity associated with . Cannabinoid receptors belong to the large superfamily of G protein-coupled receptors. Targeting the cannabinoid receptors has the potential to treat a variety of conditions such as pain, neurodegeneration, appetite, immune function, anxiety, cancer, and others. Developing bioassays to determine binding and functional activity of compounds has the ability to lead researchers to develop a safe and effective drug that may target the cannabinoid receptors. Using radioligand binding and functional bioassays, a structure-activity relationship for major and minor cannabinoids was developed.
已经存在了数千年，被用于娱乐、药用和获取纤维。从 中已分离出500多种化合物，其中约105种为大麻素。在这105种化合物中，Δ-四氢大麻酚已被确定为主要成分，它也与 相关的精神活性有关。大麻素受体属于G蛋白偶联受体的大型超家族。针对大麻素受体有可能治疗多种病症，如疼痛、神经退行性变、食欲、免疫功能、焦虑、癌症等。开发用于确定化合物结合和功能活性的生物测定法有能力引导研究人员开发出一种可能靶向大麻素受体的安全有效的药物。利用放射性配体结合和功能生物测定法，建立了主要和次要大麻素的构效关系。
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