Walker R J, Roberts C J
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1984;77(2):371-80. doi: 10.1016/0742-8413(84)90031-8.
Intracellular recordings were made from central neurons of Limulus polyphemus and from Retizu cells of the leech, Hirudo medicinalis. The effects of carbachol, amino acids and octopamine were examined on these neurons. Octopamine was found to have a mainly inhibitory effect on a few Limulus neurons. The effects of octopamine were mimicked by clonidine and napthazoline but not by xylazine. Both compounds were slightly more potent than octopamine. Yohimbine, metoclopramide, chlorpromazine and chlordimeform failed to antagonize this octopamine response. The excitatory effect of carbachol was blocked by alpha-bungarotoxin, 10(-7)M. Neither this concentration nor higher concentrations of alpha-bungarotoxin had any effect on L-glutamate excitation. m-Carboxyphenyl derivatives of alanine and glycine acted differentially on Limulus neurons responding to L-glutamate. m- Carboxyphenylglycine only inhibited neurones which showed a biphasic response to L-glutamate while m- carboxyphenylalanine only excited these neurons. Both compounds excited leech Retzius cells, with m- carboxyphenylalanine being about 20 times more potent than m- carboxyphenylglycine . The actions of alpha- ketokainate and allo-alpha- ketokainate were compared to kainate, dihydrokainate and L-glutamate on leech Retzius cells. The equipotent molar ratios for kainate, dihydrokainate , alpha- ketokainate and allo-alpha- ketokainate were 0.0029 +/- 0.0004, 0.021 +/- 0.047, 0.029 +/- 0.005 and 0.14 +/- 0.0093 respectively with L-glutamate as one. All the analogues were more potent than L-glutamate. Quinolinic acid had no glutamate-like activity on either Limulus or Hirudo neurons. Methyltetrahydrofolate was inactive on Limulus neurons but excited leech Retzius cells, being slightly less potent than L-glutamate. Dibutyl cAMP terminated the excitatory actions of kainate on both Limulus and Hirudo neurons. Anisatin , a putative GABA antagonist, was a potent antagonist of GABA inhibition on Limulus neurons.
对美洲鲎的中枢神经元以及医用水蛭的Retizu细胞进行了细胞内记录。研究了卡巴胆碱、氨基酸和章鱼胺对这些神经元的影响。发现章鱼胺对一些美洲鲎神经元主要起抑制作用。可乐定和萘甲唑啉可模拟章鱼胺的作用,但赛拉嗪不能。这两种化合物的效力均略强于章鱼胺。育亨宾、甲氧氯普胺、氯丙嗪和杀虫脒未能拮抗这种章鱼胺反应。10(-7)M的α-银环蛇毒素可阻断卡巴胆碱的兴奋作用。该浓度及更高浓度的α-银环蛇毒素对L-谷氨酸的兴奋作用均无影响。丙氨酸和甘氨酸的间羧基苯基衍生物对响应L-谷氨酸的美洲鲎神经元有不同作用。间羧基苯基甘氨酸仅抑制对L-谷氨酸呈双相反应的神经元,而间羧基苯基丙氨酸仅使这些神经元兴奋。两种化合物均能兴奋水蛭的Retzius细胞,间羧基苯基丙氨酸的效力约为间羧基苯基甘氨酸的20倍。比较了α-酮 kainate和别-α-酮 kainate与kainate、二氢kainate和L-谷氨酸对水蛭Retzius细胞的作用。以L-谷氨酸为参照,kainate、二氢kainate、α-酮 kainate和别-α-酮 kainate的等摩尔效力比分别为0.0029±0.0004、0.021±0.047、0.029±0.005和0.14±0.0093。所有类似物的效力均强于L-谷氨酸。喹啉酸对美洲鲎或水蛭神经元均无类似谷氨酸的活性。甲基四氢叶酸对美洲鲎神经元无活性,但能兴奋水蛭的Retzius细胞,效力略低于L-谷氨酸。二丁酰环磷腺苷终止了kainate对美洲鲎和水蛭神经元的兴奋作用。茴香毒素是一种假定的GABA拮抗剂,是GABA对美洲鲎神经元抑制作用的有效拮抗剂。