2-羟基舒氯芬的（S）-对映体是中枢和外周制剂中活性GABAB受体拮抗剂。

The (S)-enantiomer of 2-hydroxysaclofen is the active GABAB receptor antagonist in central and peripheral preparations.

作者信息

Kerr D I, Ong J, Doolette D J, Schafer K, Prager R H

机构信息

Department of Anaesthesia and Intensive Care, The University of Adelaide, Adelaide, South Australia 5005, Australia.

出版信息

Eur J Pharmacol. 1995 Dec 12;287(2):185-9. doi: 10.1016/0014-2999(95)00641-9.

DOI:10.1016/0014-2999(95)00641-9

PMID:8749034

Abstract

In the guinea-pig isolated ileum, (RS)-(+/-)-baclofen induced a depression of cholinergic twitch contractions, reversibly and competitively antagonised by (S)-2-hydroxysaclofen (pA2 = 5.2 +/- 0.2), but not by (R)-2-hyroxysaclofen. The depression of excitatory field potentials by baclofen ( 5 mu M) in rat CA1 hippocampal slices was antagonised by (S)-2-hydroxysaclofen (100 mu m) (pA2 = 4.3), whilst in rat neocortex, (S)-2-hyroxysaclofen (50-500 mu M) antagonised the baclofen (10 mu M)-induced suppression of spontaneous discharges, the (R)-enantiomer being inactive. These results show that (S)-2-hydroxysaclofen is the active antagonist at central and peripheral GABAB receptors.

摘要

在豚鼠离体回肠中，（RS）-（±）-巴氯芬可引起胆碱能抽搐收缩的抑制，（S）-2-羟基巴氯芬可对其产生可逆性竞争性拮抗作用（pA2 = 5.2±0.2），而（R）-2-羟基巴氯芬则无此作用。在大鼠CA1海马切片中，巴氯芬（5μM）引起的兴奋性场电位抑制可被（S）-2-羟基巴氯芬（100μM）拮抗（pA2 = 4.3），而在大鼠新皮层中，（S）-2-羟基巴氯芬（50 - 500μM）可拮抗巴氯芬（10μM）引起的自发放电抑制，（R）-对映体则无活性。这些结果表明，（S）-2-羟基巴氯芬是中枢和外周GABAB受体的活性拮抗剂。