Affordable Access

Thioether analogues of baclofen, phaclofen and saclofen.

Authors
  • Allan, R D
  • Drew, C A
  • Ong, J
  • Tran, H W
Type
Published Article
Journal
Neuroscience Letters
Publisher
Elsevier
Publication Date
May 04, 1990
Volume
112
Issue
2-3
Pages
223–228
Identifiers
PMID: 2163039
Source
Medline
License
Unknown

Abstract

Analogues of baclofen, phaclofen and saclofen, incorporating a sulfur atom within the methylene chain, have been tested against responses induced by baclofen for activity at gamma-aminobutyric acid-B (GABAB) receptor sites, using a number of preparations including the guinea-pig isolated ileum and vas deferens, rat brain cortical slices and displacement of (-)-[3H]baclofen in rat cerebellar membranes. Results indicate that 2-([2-amino-1-(4-chlorophenyl)ethyl]thio)ethanephosphonic acid 2d is the most active of the new compounds. 2d is some 2-5 times weaker than phaclofen as a GABAB antagonist and approximately half as potent as phaclofen as an inhibitor of GABAB binding.

Report this publication

Statistics

Seen <100 times