Phosphinic acid analogues of GABA are antagonists at the GABAB receptor in the rat anococcygeus
Phosphinic acid analogues of GABA are antagonists at the GABAB receptor in the rat anococcygeus
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GABA 的次膦酸类似物是大鼠尾骨 GABAB 受体的拮抗剂
DOI：
10.1111/j.1476-5381.1991.tb12121.x
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发表时间：
1991
影响因子：
7.3
通讯作者：
W. Howson
中科院分区：
文献类型：
--
作者：
J. Hills;A. J. Sellers;J. Mistry;M. Broekman;W. Howson
用GABAB激动剂CGp 35348(3-氨丙基(二乙氧甲基)膦酸)和3-氨基丙基(n-己基)膦酸(3-APHPA)在大鼠肛尾肌进行拮抗作用。比较了它们与2-羟基氯芬的拮抗效力。Cgp 35348、3-APHPA和2-羟基糖胺在大鼠肛尾肌的PA2值分别为5.38、4.86和4.45。这些结果证实了以前关于这些化合物的GABAB拮抗剂活性的报道，并显示出比2-羟基糖芬的效力略有提高。
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.