离体视神经和楔束核中对甘氨酸、β-丙氨酸和蝇蕈醇的去极化反应。
Depolarizing responses to glycine, beta-alanine and muscimol in isolated optic nerve and cuneate nucleus.
作者信息
Simmonds M A
出版信息
Br J Pharmacol. 1983 Jul;79(3):799-806. doi: 10.1111/j.1476-5381.1983.tb10018.x.
Abstract
Concentration-dependent depolarizations were evoked by glycine and beta-alanine 5 X 10(-4)-10(-2)M and by the gamma-aminobutyric acid (GABA) analogue, muscimol 10(-6)-10(-4)M. The maximal response to glycine was several-fold higher than that to muscimol on optic nerve but the reverse was found on the dorsal funiculus fibres in the cuneate nucleus. beta-Alanine evoked a similar maximal response to glycine on optic nerve but a considerably higher maximum than glycine in the cuneate nucleus. Strychnine was 19.5 times more potent as a glycine antagonist (pA2 = 6.58) than as a muscimol antagonist. Bicuculline was 156 times more potent as a muscimol antagonist than as a glycine antagonist. Other antagonists of muscimol, i.e. tubocurarine, picrotoxin and leptazol, and potentiators of muscimol, i.e. pentobarbitone and flurazepam, had little or no effect on responses to glycine. Responses to beta-alanine had pharmacological properties compatible with a mixed action on both GABA and glycine receptors. The rat isolated optic nerve appears to be a useful preparation for studying the pharmacology of the neuronal glycine receptor plus chloride ionophore complex.
摘要
5×10⁻⁴ - 10⁻²M的甘氨酸和β-丙氨酸以及10⁻⁶ - 10⁻⁴M的γ-氨基丁酸（GABA）类似物蝇蕈醇可引起浓度依赖性去极化。在视神经上，对甘氨酸的最大反应比对蝇蕈醇的最大反应高几倍，但在楔束核的背索纤维上则相反。β-丙氨酸在视神经上引起的最大反应与甘氨酸相似，但在楔束核中其最大值比甘氨酸高得多。士的宁作为甘氨酸拮抗剂的效力比作为蝇蕈醇拮抗剂的效力高19.5倍（pA2 = 6.58）。荷包牡丹碱作为蝇蕈醇拮抗剂的效力比作为甘氨酸拮抗剂的效力高156倍。其他蝇蕈醇拮抗剂，即筒箭毒碱、苦味毒和戊四氮，以及蝇蕈醇增强剂，即戊巴比妥和氟西泮，对甘氨酸反应几乎没有影响。对β-丙氨酸的反应具有与对GABA和甘氨酸受体的混合作用相符合的药理学特性。大鼠离体视神经似乎是研究神经元甘氨酸受体加氯离子载体复合物药理学的有用标本。
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