A partial agonist of GABAB receptors
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3-Aminopropylphosphonic acid (3-APPA) is a phosphonic analog of GABA that acts as a partial agonist of GABAB receptors (IC50 = 1.5 μM in a radioligand binding assay). It induces relaxation in unstimulated isolated guinea pig ileum longitudinal muscle and reverses GABA- and baclofen-induced inhibition of twitch responses in isolated guinea pig ileum longitudinal muscle. 3-APPA (5 mg/kg) completely inhibits GABA- and baclofen-induced inhibition of vagally stimulated bronchospasms in guinea pigs. It also reverses the antitussive effect of baclofen in cats when administered at a dose of 3 mg/kg.
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