Biological activity of 3-aminopropyl (methyl) phosphinic acid, a potent and selective GABAB agonist with CNS activity

Add time:08/07/2019    Source:sciencedirect.com

The GABAB receptor affinity of a number of GABA analogues, where the carboxylic acid group has been replaced with a range of acidic moieties, were determined. The phosphinic acid analogue (1) was identified as a potent selective GABAB ligand which is CNS penetrating and 10-fold more active than baclofen (2).

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