muscarinic receptors

毒蕈碱受体
  • 文章类型: Journal Article
    在七千万患有癫痫的人中,其中40%的人对一种以上的抗癫痫药物产生抗药性,并且死亡的可能性更高。虽然癫痫的经典定义是由于兴奋性谷氨酸能和抑制性γ-氨基丁酸(GABA)-能信号之间的不平衡,大量证据表明毒蕈碱受体参与神经兴奋性的调节。
    大麻素已显示出在几种癫痫模型中通过用调节其活性的药物激活毒蕈碱受体来降低癫痫发作活性和神经元兴奋性。大麻素也有效降低药物耐药个体的抗癫痫活性;然而,其在颞叶癫痫中的作用机制尚不清楚。
    这篇综述旨在阐明癫痫中毒蕈碱和大麻素受体与神经兴奋性之间的关系。
    UNASSIGNED: Of the seventy million people who suffer from epilepsy, 40 percent of them become resistant to more than one antiepileptic medication and have a higher chance of death. While the classical definition of epilepsy was due to the imbalance between excitatory glutamatergic and inhibitory γ-aminobutyric acid (GABA)-ergic signalling, substantial evidence implicates muscarinic receptors in the regulation of neural excitability.
    UNASSIGNED: Cannabinoids have shown to reduce seizure activity and neuronal excitability in several epileptic models through the activation of muscarinic receptors with drugs which modulate their activity. Cannabinoids also have been effective in reducing antiepileptic activity in pharmaco-resistant individuals; however, the mechanism of its effects in temporal lobe epilepsy is not clear.
    UNASSIGNED: This review seeks to elucidate the relationship between muscarinic and cannabinoid receptors in epilepsy and neural excitability.
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  • 文章类型: Journal Article
    尽管精神分裂症的多巴胺假说解释了所有可用的抗精神病药物在临床使用中的作用,越来越需要开发治疗阳性的新药,负,和慢性精神病的认知症状。Xanomeline-trospium(KarXT)是一种药物组合,基于乙酰胆碱在调节认知过程中以及该神经递质与中枢神经系统其他信号通路之间的相互作用中所起的重要作用,在精神分裂症的发病中起着潜在的作用,老年痴呆症,和物质使用障碍。包括四个电子数据库(PubMed,科克伦,Clarivate/WebofScience,和GoogleScholar)和美国国家医学图书馆的临床试验数据库检测到21个来源,这些来源涉及针对KarXT的14项研究,其中只有四个有可用的结果。根据这些试验的结果,黄松松药的短期疗效和耐受性良好,但在该药物组合可能被推荐用于临床之前,还需要更多的数据.然而,在理论层面上,KarXT的探索有助于增加研究人员发现新事物的兴趣,非多巴胺能,可以用作单一疗法或附加药物的抗精神病药。
    Although the dopamine hypothesis of schizophrenia explains the effects of all the available antipsychotics in clinical use, there is an increasing need for developing new drugs for the treatment of the positive, negative, and cognitive symptoms of chronic psychoses. Xanomeline-trospium (KarXT) is a drug combination that is based on the essential role played by acetylcholine in the regulation of cognitive processes and the interactions between this neurotransmitter and other signaling pathways in the central nervous system, with a potential role in the onset of schizophrenia, Alzheimer\'s disease, and substance use disorders. A systematic literature review that included four electronic databases (PubMed, Cochrane, Clarivate/Web of Science, and Google Scholar) and the US National Library of Medicine database for clinical trials detected twenty-one sources referring to fourteen studies focused on KarXT, out of which only four have available results. Based on the results of these trials, the short-term efficacy and tolerability of xanomeline-trospium are good, but more data are needed before this drug combination may be recommended for clinical use. However, on a theoretical level, the exploration of KarXT is useful for increasing the interest of researchers in finding new, non-dopaminergic, antipsychotics that could be used either as monotherapy or as add-on drugs.
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