钙离子通道激动剂Bay k-8644对N-甲基-D-天冬氨酸（NMDA）和非NMDA受体拮抗剂抗惊厥活性的影响。
Influence of a Ca2+ channel agonist, Bay k-8644, on the anticonvulsant activity of NMDA and non-NMDA receptor antagonists.
作者信息
Czuczwar S J, Gasior M, Turski W A, Kleinrok Z
机构信息
Department of Pharmacology and Toxicology, Medical School, Lublin, Poland.
出版信息
Eur J Pharmacol. 1994 Oct 13;264(1):103-6. doi: 10.1016/0014-2999(94)90644-0.
Bay k-8644 (methyl-1,4-dihydro-2,6-dimethyl-3-nitro-4-(2-trifluoro- methylphenyl)-pyridine-5-carboxylate) (a Ca2+ channel agonist of the dihydropyridine class) at 5 mg/kg (s.c.) impaired the anticonvulsant activities of two competitive NMDA receptor antagonists, CGP 37849 (D,L-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid) and D-CPP-ene (3-(2-carboxypiperazine-4-yl)-1-propenyl-1-phosphonic acid) (given i.p.), against electroconvulsions. In contrast, the Ca2+ channel agonist did not affect the protection afforded by the AMPA receptor antagonists, NBQX (2,3-dihydroxy-6-nitro-7-sulfamoylbenzo(F)quinoxaline) and GYKI 52466 (1-(4-aminophenyl)-4-methyl-7,8-methylendioxy-5-2,3-benzodiazepine ), or by a non-competitive NMDA receptor antagonist, MK-801 (dizocilpine), all being injected i.p. It may be concluded that the anticonvulsive activity of competitive NMDA receptor antagonists can be impaired by Ca2+ ion influx.
Bay k - 8644（甲基 - 1,4 - 二氢 - 2,6 - 二甲基 - 3 - 硝基 - 4 -（2 - 三氟甲基苯基）吡啶 - 5 - 羧酸酯）（一种二氢吡啶类钙离子通道激动剂），腹腔注射剂量为5mg/kg时，会损害两种竞争性N - 甲基 - D - 天冬氨酸（NMDA）受体拮抗剂CGP 37849（D，L -（E） - 2 - 氨基 - 4 - 甲基 - 5 - 膦酰基 - 3 - 戊烯酸）和D - CPP - ene（3 -（2 - 羧基哌嗪 - 4 - 基） - 1 - 丙烯基 - 1 - 膦酸）（腹腔注射）对电惊厥的抗惊厥活性。相比之下，这种钙离子通道激动剂并不影响α - 氨基 - 3 - 羟基 - 5 - 甲基 - 4 - 异恶唑丙酸（AMPA）受体拮抗剂NBQX（2,3 - 二羟基 - 6 - 硝基 - 7 - 氨磺酰基苯并（F）喹喔啉）和GYKI 52466（1 -（4 - 氨基苯基） - 4 - 甲基 - 7,8 - 亚甲基二氧基 - 5 - 2,3 - 苯并二氮杂卓），或非竞争性NMDA受体拮抗剂MK - 801（地佐环平）（均为腹腔注射）所提供的保护作用。可以得出结论，竞争性NMDA受体拮抗剂的抗惊厥活性可能会因钙离子内流而受损。
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