Phosphinic acid analogues of GABA are antagonists at the GABAB receptor in the rat anococcygeus
Open Access
- 1 January 1991
- journal article
- Published by Wiley in British Journal of Pharmacology
- Vol. 102 (1) , 5-6
- https://doi.org/10.1111/j.1476-5381.1991.tb12121.x
Abstract
CGP 35348 (3-aminopropyl(diethoxymethyl)phosphinic acid) and 3-aminopropyl(n-hexyl)phosphinic acid (3-APHPA) were tested in the rat anococcygeus muscle against CGP 27492 (3-aminopropylphosphinic acid), a selective GABAB agonist, for their antagonist activity. Their antagonist potency was compared with that of 2-hydroxysaclofen. The pA2 values for CGP 35348, 3-APHPA and 2-hydroxysaclofen were 5.38, 4.86, 4.45 respectively in the rat anococcygeus muscle. These results confirm the previous reports of GABAB antagonist activity for these compounds and show a marginal improvement in potency over 2-hydroxysaclofen.Keywords
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