Antagonism at GABAB receptors by saclofen and related sulphonic analogues of baclofen and GABA.

Abstract:

:Saclofen (the direct sulphonic analogue of baclofen) is a competitive antagonist of baclofen at GABAB receptors in guinea pig ileum and rat cortical slices (estimated pA2 = 5.3), at least twice as potent as 2-hydroxy-saclofen (pA2 = 5). A series of related sulphonic analogues also antagonised baclofen in the guinea pig ileum, including 2-hydroxy-saclofen amide (pA2 = 3.3), 3-amino-2-hydroxy-2-phenyl-propylsulphonic acid (pA2 = 3.5), 3-amino-2-(benzo-(b)-furan-2-yl)-propylsulphonic acid (pA2 = 4.3), and 3-amino-2-(4-chlorophenyl)-prop-1-enesulphonic acid (pA2 = 2.5-3), but none were more active than saclofen which is the most potent specific GABAB antagonist yet found.

journal_name

Neurosci Lett

journal_title

Neuroscience letters

authors

Kerr DI,Ong J,Johnston GA,Abbenante J,Prager RH

doi

10.1016/0304-3940(89)90824-0

subject

Has Abstract

pub_date

1989-12-15 00:00:00

pages

239-44

issue

1-3

eissn

0304-3940

issn

1872-7972

pii

0304-3940(89)90824-0

journal_volume

107

pub_type

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