The cannabis derivative marijuana is the most widely used recreational drug in the Western world and is consumed by an estimated 83 million individuals (~3% of the world population). In recent years, there has been a marked transformation in society regarding the risk perception of cannabis, driven by its legalization and medical use in many states in the United States and worldwide. Compelling research evidence and the Food and Drug Administration cannabis-derived cannabidiol approval for severe childhood epilepsy have confirmed the large therapeutic potential of cannabidiol itself, ⁹-tetrahydrocannabinol and other plant-derived cannabinoids (phytocannabinoids). Of note, our body has a complex endocannabinoid system (ECS)—made of receptors, metabolic enzymes, and transporters—that is also regulated by phytocannabinoids. The first endocannabinoid to be discovered 30 years ago was anandamide (N-arachidonoyl-ethanolamine); since then, distinct elements of the ECS have been the target of drug design programs aimed at curing (or at least slowing down) a number of human diseases, both in the central nervous system and at the periphery. Here a critical review of our knowledge of the goods and bads of the ECS as a therapeutic target is presented to define the benefits of ECS-active phytocannabinoids and ECS-oriented synthetic drugs for human health.

大麻衍生品大麻是西方世界使用最广泛的娱乐药物，估计有 8300 万人（约占世界人口的 3%）消费。近年来，在美国和世界各地大麻合法化和医疗用途的推动下，社会对大麻的风险认知发生了显着转变。令人信服的研究证据以及美国食品和药物管理局对大麻衍生的大麻二酚治疗严重儿童癫痫的批准，证实了大麻二酚本身、^9-四氢大麻酚和其他植物衍生的大麻素（植物大麻素）的巨大治疗潜力。值得注意的是，我们的身体有一个复杂的内源性大麻素系统 (ECS) ——由受体、代谢酶和转运蛋白组成-这也受到植物大麻素的调节。30 年前发现的第一个内源性大麻素是 anandamide（N-花生四烯酰乙醇胺）；从那时起，ECS的不同元素就成为药物设计项目的目标，旨在治愈（或至少减缓）许多人类疾病，包括中枢神经系统和外周疾病。本文对我们对 ECS 作为治疗靶点的优点和缺点的了解进行了批判性回顾，以确定 ECS 活性植物大麻素和 ECS 导向的合成药物对人类健康的益处。