Phytocannabinoids and Cannabimimetic Drugs: Recent Patents in Central Nervous System Disorders.

Recent patents on CNS drug discovery Pub Date : 2016-01-01
Roberta Ranieri, Daniela Marasco, Maurizio Bifulco, Anna M Malfitano
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Abstract

Background: Starting from the chemical structure of phytocannabinoids, isolated from Cannabis sativa plant, research groups designed numerous cannabimimetic drugs. These compounds according to their activities can be partial, full agonists and antagonists of cannabinoid receptors. Anecdotal reports and scientific studies described beneficial properties of cannabinoids and their derivatives in several pathological conditions like neurological and neuropsychiatric disorders, and in many other diseases ranging from cancer, atherosclerosis, stroke, hypertension, inflammatory related disorders, and autoimmune diseases.

Methods: In this study, starting from the endocannabinoid mechanism of action in neuronal signaling, we highlight and discuss potential application and recent patents of cannabimimetic drugs in neurological disorders.

Results: The cannabinoid CB1 receptor was considered particularly interesting for therapeutic approaches in neurological diseases, because primarily expressed by neurons of the central nervous system. In many experimental models, these drugs act via this receptor, however, CB1 receptor independent mechanisms have been also described. Furthermore, endogenous ligands of cannabinoid receptors, the endocannabinoids, are potent modulators of the synaptic function in the brain. In neurological diseases, numerous studies reported modulation of the levels of endocannabinoids according to the phase of the disease and its progression.

Conclusions: Finally, although the study of the mechanisms of action of these compounds is still unsolved, many reports and patents strongly suggest therapeutic potential of these compounds in neurological diseases.

植物大麻素和拟大麻药物:中枢神经系统疾病的最新专利。
背景:从从大麻植物中分离的植物大麻素的化学结构出发,研究小组设计了许多大麻类药物。这些化合物根据其活性可以是大麻素受体的部分、完全激动剂和拮抗剂。轶事报道和科学研究描述了大麻素及其衍生物在几种病理条件下的有益特性,如神经和神经精神疾病,以及许多其他疾病,包括癌症、动脉粥样硬化、中风、高血压、炎症相关疾病和自身免疫性疾病。方法:本研究从内源性大麻素在神经元信号传导中的作用机制出发,重点讨论了拟大麻药物在神经系统疾病中的潜在应用和近期专利。结果:大麻素CB1受体被认为对神经系统疾病的治疗方法特别感兴趣,因为它主要由中枢神经系统的神经元表达。在许多实验模型中,这些药物通过该受体起作用,然而,也描述了CB1受体独立的机制。此外,内源性大麻素受体配体内源性大麻素是大脑突触功能的有效调节剂。在神经系统疾病中,许多研究报告了内源性大麻素水平的调节根据疾病的阶段及其进展。结论:最后,尽管对这些化合物的作用机制的研究仍未得到解决,但许多报告和专利强烈表明这些化合物在神经系统疾病中的治疗潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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