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Small Molecules from Nature Targeting G-Protein Coupled Cannabinoid Receptors: Potential Leads for Drug Discovery and Development

机译:大自然靶向G蛋白偶联大麻受体的小分子:药物发现和开发的潜在线索。

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摘要

The cannabinoid molecules are derived from Cannabis sativa plant which acts on the cannabinoid receptors types 1 and 2 (CB1 and CB2) which have been explored as potential therapeutic targets for drug discovery and development. Currently, there are numerous cannabinoid based synthetic drugs used in clinical practice like the popular ones such as nabilone, dronabinol, and Δ9-tetrahydrocannabinol mediates its action through CB1/CB2 receptors. However, these synthetic based Cannabis derived compounds are known to exert adverse psychiatric effect and have also been exploited for drug abuse. This encourages us to find out an alternative and safe drug with the least psychiatric adverse effects. In recent years, many phytocannabinoids have been isolated from plants other than Cannabis. Several studies have shown that these phytocannabinoids show affinity, potency, selectivity, and efficacy towards cannabinoid receptors and inhibit endocannabinoid metabolizing enzymes, thus reducing hyperactivity of endocannabinoid systems. Also, these naturally derived molecules possess the least adverse effects opposed to the synthetically derived cannabinoids. Therefore, the plant based cannabinoid molecules proved to be promising and emerging therapeutic alternative. The present review provides an overview of therapeutic potential of ligands and plants modulating cannabinoid receptors that may be of interest to pharmaceutical industry in search of new and safer drug discovery and development for future therapeutics.
机译:大麻素分子衍生自对1型和2型大麻素受体(CB1和CB2)起作用的大麻植物,大麻素受体已被开发为药物发现和开发的潜在治疗靶标。目前,临床上有许多基于大麻素的合成药物,如流行的诸如萘比隆,屈大麻酚和Δ 9 -四氢大麻酚通过CB1 / CB2受体介导其作用。然而,已知这些合成的基于大麻的化合物发挥出不良的精神病学作用,并且还被用于药物滥用。这鼓励我们寻找一种对精神病副作用最小的替代安全药物。近年来,从大麻以外的植物中分离出许多植物大麻素。几项研究表明,这些植物大麻素显示出对大麻素受体的亲和力,效力,选择性和功效,并抑制内源性大麻素代谢酶,从而降低了内源性大麻素系统的活性。而且,这些天然来源的分子与合成来源的大麻素相反,具有最小的不利影响。因此,基于植物的大麻素分子被证明是有前途的新兴治疗选择。本综述概述了调配大麻素受体的配体和植物的治疗潜力,这可能是制药业为寻找新的和更安全的药物发现和开发未来治疗方法而感兴趣的植物。

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