Pharmacological profile of novel cyclic analogs of 2-amino-7-phosphonoheptanoic acid.
Pharmacological profile of novel cyclic analogs of 2-amino-7-phosphonoheptanoic acid.
复制标题
2-氨基-7-膦酰庚酸新型环状类似物的药理学概况。
DOI：
10.1016/b978-0-444-89710-7.50033-1
复制
发表时间：
1992
期刊：
影响因子：
--
通讯作者：
Patch,R
中科院分区：
文献类型：
--
作者：
Ferkany,JW;Kyle,DJ;Ellenberger,WP;Narayanan,BA;Ellenberger,SR;Hudkins,R;Guzewska,ME;Rzeszotarski,WJ;Conti,L;Patch,R
兴奋性氨基酸（EAA）是哺乳动物大脑中最普遍和最广泛的神经递质之一。与神经递质或神经调节剂的功能一致，FAA 的多种受体已被鉴定。最初根据激动剂药理学进行分类，分为红藻氨酸 (KA)、使君子酸和 N-甲基-D-天冬氨酸 (NMDA) 识别位点 (30)。尽管这种分类仍然有效，但最近的研究表明 FAA 受体和 EAA 神经传递比最初建议的更加微妙和复杂。例如，除了上述三个离子型识别位点之外，还鉴定出对使君子酸敏感并与磷酸肌醇周转或细胞内 Ca 动员直接相关的代谢型受体 (19,25,27)。此外，NMDA 受体现在被认为是受二价阳离子以及氨基酸甘氨酸调节的复杂分子实体。后者可作为正向调节剂，或作为受体复合物的共递质 (9-11)。人们对 EAA 介导的传递的兴趣日益浓厚，人们越来越认识到 EAA 在中枢神经系统的生理和病理功能中所起的作用。由于激动剂和拮抗剂的出现较早，人们对 NMDA 受体活性的了解也最为深入。虽然激动剂如NMDA、内源性色氨酸代谢物喹啉(QUIN)。
Excitatory amino acids (EAA) are among the most prevalent and widespread neurotransmitters in the mammalian brain. Consistent with a function as neu-rotransmitters or neuromodulators, multiple receptors for FAAs have been identified. Originally classified according to agonist pharmacology, these were divided into kainic acid (KA), quisqualic acid, and N-methyl-D-aspartatic acid (NMDA) recognition sites (30). Although this classification remains valid, more recent work indicates that FAA receptors and EAA neurotransmission are even more subtle and complex than first suggested. For example, beyond the three ionotropic recognition sites mentioned above, meta-botropic receptors have been identified that are sensitive to quisqualate and directly linked to inositol phosphate turnover or intracellular Ca mobilization (19, 25, 27). Furthermore, the NMDA receptor is now believed to be a complex molecular entity regulated by divalent cations as well as is the amino acid glycine. The latter may function as either a positive modulator, or as a cotransmitter at the receptor com plex (9-11).The growing interest in EAA mediated transmission has led to an increasing awareness of the role EAAs play in physiological and pathological function of the central nervous system. Because of the early availability of agonists and antagonists, the under standing of NMDA receptor activity is most advanced. Although agonists such as NMDA, the endogenous tryptophan metabolite, quinolinate (QUIN).