Add time:08/30/2019         Source:sciencedirect.com

Analogues of baclofen, PHACLOFEN (cas 114012-12-3) and saclofen, incorporating a sulfur atom within the methylene chain, have been tested against responses induced by baclofen for activity at γ-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.

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