Ryzhov I V, Slepokurov M V, Lapin I P, Mandel'shtam Iu E, Aleksandrov V G
Biull Eksp Biol Med. 1986 Mar;101(3):322-5.
All excitatory amino acid antagonists studied: diethyl esters of aspartic (DEEA) and glutamic (DEEG) acids, 2-amino-3-phosphono-propionic acid (APPA) and 2-amino-4-phosphono-butanoic acid (APBA), diminished the amplitude of excitatory postsynaptic potentials (EPP) of the locust (Locusta migratoria migratorioides) muscle fibers and arbitrary blocked glutamate (GLU) and aspartate (ASP) responses. Kynurenine (KYN) and quinolinic (QUI) acid had no effect on EPP even at a concentration of 2 X 10(-2) M. The antagonists were not strictly selective against intracerebroventricularly administered endogenous convulsants: GLU, ASP, KYN and QUI and in simulation of experimental seizures in mice. The antagonists structurally similar to ASP prevented ASP- and KYN-induced seizures in lower doses than GLU derivatives. Anti-KYN, but not anti-QUI DEEA, DEEG, APPA and APBA efficacy suggests that KYN and QUI act on different structures or binding sites.
天冬氨酸二乙酯(DEEA)和谷氨酸二乙酯(DEEG)、2-氨基-3-膦酰丙酸(APPA)和2-氨基-4-膦酰丁酸(APBA),均降低了蝗虫(飞蝗)肌肉纤维兴奋性突触后电位(EPP)的幅度,并随意阻断了谷氨酸(GLU)和天冬氨酸(ASP)反应。犬尿氨酸(KYN)和喹啉酸(QUI)即使在浓度为2×10⁻² M时对EPP也无影响。这些拮抗剂对脑室内注射的内源性惊厥剂:GLU、ASP、KYN和QUI以及在模拟小鼠实验性癫痫发作时,并非严格具有选择性。与ASP结构相似的拮抗剂在比GLU衍生物更低的剂量下可预防ASP和KYN诱导的癫痫发作。抗KYN,而非抗QUI的DEEA、DEEG、APPA和APBA的功效表明,KYN和QUI作用于不同的结构或结合位点。