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美洲大蠊骨骼肌γ-氨基丁酸门控氯离子通道的药理学

Pharmacology of skeletal muscle GABA-gated chloride channels in the cockroach Periplaneta americana.

作者信息

Schnee M, Rauh J, Buckingham S D, Sattelle D B

机构信息

DuPont Agricultural Products, Stine-Haskell Research Center, P.O. Box 30, Newark, DE 19714, USA.

出版信息

J Exp Biol. 1997 Dec;200(Pt 23):2947-55. doi: 10.1242/jeb.200.23.2947.

Abstract

The pharmacology of -aminobutyric acid (GABA)-gated chloride channels of the coxal levator (182c,d) muscle of the cockroach Periplaneta americana has been investigated and the data compared with similar findings for the cell body of the cockroach fast coxal depressor motor neurone (Df). Muscle GABA receptors resembled those of the motor neurone cell body in their sensitivity to picrotoxinin and insensitivity to bicuculline. However, muscle GABA receptors were insensitive to the neuronal GABA receptor agonists isoguvacine (10(-4) mol l-1) and 3-aminopropane sulphonic acid (10(-3 )mol l-1). The benzodiazepine flunitrazepam, which at 10(-6 )mol l-1 greatly enhances the amplitude of the motor neurone GABA-induced responses, failed to affect muscle responses to GABA when tested at the same and at a higher (10(-4 )mol l-1) concentration. The convulsant t-butylbicyclophosphorothionate was a weak antagonist of cockroach muscle GABA receptors, whereas several cyclodienes were much more effective antagonists. Thus, studies using a benzodiazepine and several convulsant antagonists reveal differences in the pharmacology of muscle and neuronal GABA receptors of the cockroach Periplaneta americana.

摘要

对美洲大蠊后足提肌(182c,d)中γ-氨基丁酸(GABA)门控氯离子通道的药理学进行了研究,并将数据与美洲大蠊快速后足降肌运动神经元(Df)细胞体的类似研究结果进行了比较。肌肉GABA受体在对印防己毒素的敏感性和对荷包牡丹碱的不敏感性方面与运动神经元细胞体的GABA受体相似。然而,肌肉GABA受体对神经元GABA受体激动剂异鹅去甲肾上腺素(10^(-4) mol/L)和3-氨基丙烷磺酸(10^(-3) mol/L)不敏感。苯二氮䓬类药物氟硝西泮在10^(-6) mol/L时能极大增强运动神经元GABA诱导的反应幅度,但在相同浓度和更高浓度(10^(-4) mol/L)下测试时,未能影响肌肉对GABA的反应。惊厥剂叔丁基双环磷硫酰亚胺是蟑螂肌肉GABA受体的弱拮抗剂,而几种环二烯类药物是更有效的拮抗剂。因此,使用苯二氮䓬类药物和几种惊厥拮抗剂的研究揭示了美洲大蠊肌肉和神经元GABA受体在药理学上的差异。

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