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The (S)-enantiomer of 2-hydroxysaclofen Is the Active GABAB Receptor Antagonist in Central and Peripheral Preparations

The (S)-enantiomer of 2-hydroxysaclofen Is the Active GABAB Receptor Antagonist in Central and Peripheral Preparations

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

Eur J Pharmacol. 1995 Dec 12;287(2):185-9.

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP117354640	2-Hydroxysaclofen		117354-64-0	Price

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