巴氯芬在大鼠离体新皮质脑片标本中由GABAB受体介导的作用：GABA膦酸类似物的拮抗作用

GABAB-receptor-mediated actions of baclofen in rat isolated neocortical slice preparations: antagonism by phosphono-analogues of GABA.

作者信息

Kerr D I, Ong J, Johnston G A, Prager R H

机构信息

Department of Pharmacology, University of Sydney, N.S.W., Australia.

出版信息

Brain Res. 1989 Feb 20;480(1-2):312-6. doi: 10.1016/0006-8993(89)90198-4.

DOI:10.1016/0006-8993(89)90198-4

PMID:2540879

Abstract

Baclofen, 3-amino-propylphosphonic acid (3-APPA), and beta-phenyl-GABA (BPG), each reduced the frequency of spontaneous paroxysmal discharges in rat neocortical slices maintained in Mg2+-free medium, reversibly antagonised by phaclofen and 4-amino-butylphosphonic acid (4-ABPA). At lower concentrations, not influencing the discharges, both 3-APPA and BPG also reversibly antagonised this action of baclofen. However, des-chloro-phaclofen was inactive. Thus, phaclofen and 4-ABPA are GABAB-receptor antagonists in neocortex, whereas both 3-APPA and BPG have partial agonist/antagonist activity at cortical GABAB-receptors.

摘要

巴氯芬、3-氨基丙基膦酸（3-APPA）和β-苯基-GABA（BPG）均可降低无镁培养基中大鼠新皮质切片的自发性阵发性放电频率，该作用可被法氯芬和4-氨基丁基膦酸（4-ABPA）可逆性拮抗。在较低浓度下，3-APPA和BPG均不影响放电，但也可可逆性拮抗巴氯芬的这一作用。然而，去氯法氯芬无活性。因此，法氯芬和4-ABPA是新皮质中的GABAB受体拮抗剂，而3-APPA和BPG在皮质GABAB受体上均具有部分激动剂/拮抗剂活性。