Swanson Geoffrey T, Sakai Ryuichi
Department of Molecular Pharmacology and Biological Chemistry, Northwestern University, Feinberg School of Medicine, 303 E. Chicago Ave., Chicago, IL 60611, USA.
Prog Mol Subcell Biol. 2009;46:123-57. doi: 10.1007/978-3-540-87895-7_5.
Marine-derived small molecules and peptides have played a central role in elaborating pharmacological specificities and neuronal functions of mammalian ionotropic glutamate receptors (iGluRs), the primary mediators of excitatory synaptic transmission in the central nervous system (CNS). As well, the pathological sequelae elicited by one class of compounds (the kainoids) constitute a widely-used animal model for human mesial temporal lobe epilepsy (mTLE). New and existing molecules could prove useful as lead compounds for the development of therapeutics for neuropathologies that have aberrant glutamatergic signaling as a central component. In this chapter we discuss natural source origins and pharmacological activities of those marine compounds that target ionotropic glutamate receptors.
源自海洋的小分子和肽在阐释哺乳动物离子型谷氨酸受体(iGluRs)的药理学特异性和神经元功能方面发挥了核心作用,iGluRs是中枢神经系统(CNS)兴奋性突触传递的主要介质。此外,一类化合物(海人藻酸类)引发的病理后遗症构成了一种广泛应用于人类内侧颞叶癫痫(mTLE)的动物模型。新的和现有的分子可能被证明是有用的先导化合物,可用于开发针对以谷氨酸能信号异常为核心成分的神经病理学的治疗方法。在本章中,我们将讨论那些靶向离子型谷氨酸受体的海洋化合物的天然来源及药理活性。