Sutko J L, Airey J A, Welch W, Ruest L
Department of Pharmacology, University of Nevada School of Medicine, Reno 89557, USA.
Pharmacol Rev. 1997 Mar;49(1):53-98.
The goal of this review has been to describe the current state of the pharmacology of ryanodine and related compounds relative to the vertebrate RyRs. Resolution of questions concerning the molecular properties of RyR channel function and the contributions made by the RyR isoforms to cellular signaling in a variety of tissues will require the production of new pharmacological agents directed against these proteins. Novel naturally occurring ryanodine congeners have been identified, and significant advances have been made in developing chemical approaches that permit the structure of ryanodine to be derivatized in selective ways. Moreover, several of these changes have yielded compounds that differ in their binding affinities and in their abilities to modify the properties of the RyR channels. These advances give substance to the possibility of designing the required pharmacological agents based on rational design changes of the structure ryanodine.
本综述的目的是描述相对于脊椎动物兰尼碱受体（RyRs）而言，兰尼碱及相关化合物的药理学现状。要解决有关RyR通道功能的分子特性以及不同RyR亚型对多种组织中细胞信号传导所做贡献的问题，将需要研发针对这些蛋白质的新型药理学试剂。已鉴定出新型天然存在的兰尼碱类似物，并且在开发化学方法方面取得了重大进展，这些方法能够以选择性方式对兰尼碱的结构进行衍生化。此外，其中一些改变产生了在结合亲和力以及改变RyR通道特性的能力方面存在差异的化合物。这些进展使基于兰尼碱结构的合理设计改变来设计所需药理学试剂成为可能。
