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 Lettjournal_title
Neuroscience lettersauthors
Kerr DI,Ong J,Johnston GA,Abbenante J,Prager RHdoi
10.1016/0304-3940(89)90824-0subject
Has Abstractpub_date
1989-12-15 00:00:00pages
239-44issue
1-3eissn
0304-3940issn
1872-7972pii
0304-3940(89)90824-0journal_volume
107pub_type
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