Literature DB >> 1646062

Phosphinic acid analogues of GABA are antagonists at the GABAB receptor in the rat anococcygeus.

J M Hills1, A J Sellers, J Mistry, M Broekman, W Howson.   

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.

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Year:  1991        PMID： 1646062      PMCID： PMC1917890          DOI： 10.1111/j.1476-5381.1991.tb12121.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN： 0007-1188            Impact factor:   8.739


  6 in total

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Authors:  N Bowery
Journal:  Trends Pharmacol Sci       Date:  1989-10       Impact factor: 14.819

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Authors:  D I Kerr; J Ong; R H Prager; B D Gynther; D R Curtis
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4.  2-Hydroxy-saclofen: an improved antagonist at central and peripheral GABAB receptors.

Authors:  D I Kerr; J Ong; G A Johnston; J Abbenante; R H Prager
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5.  Baclofen antagonism by 2-hydroxy-saclofen in the cat spinal cord.

Authors:  D R Curtis; B D Gynther; D T Beattie; D I Kerr; R H Prager
Journal:  Neurosci Lett       Date:  1988-09-23       Impact factor: 3.046

6.  3-Aminopropylphosphinic acid--a potent, selective GABAB receptor agonist in the guinea-pig ileum and rat anococcygeus muscle.

Authors:  J M Hills; R A Dingsdale; M E Parsons; R E Dolle; W Howson
Journal:  Br J Pharmacol       Date:  1989-08       Impact factor: 8.739
  6 in total
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