ANTAGONISM AT GABAB-RECEPTORS BY SACLOFEN AND RELATED SULFONIC ANALOGS OF BACLOFEN AND GABA
ANTAGONISM AT GABAB-RECEPTORS BY SACLOFEN AND RELATED SULFONIC ANALOGS OF BACLOFEN AND GABA
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DOI：
10.1016/0304-3940(89)90824-0
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发表时间：
1989-12-15
影响因子：
2.5
通讯作者：
PRAGER, RH
中科院分区：
文献类型：
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作者：
KERR, DIB;ONG, J;PRAGER, RH
沙氯芬（巴氯芬的直接磺酸类似物）是巴氯芬在豚鼠回肠和大鼠皮质片中GABAB受体上的竞争性拮抗剂（估计pA2 = 5.3），至少是2-羟基沙氯芬（pA2 = 5）的两倍。一系列相关的磺胺类似物也在豚鼠回肠中拮抗巴氯芬，包括2-羟基-saclofen酰胺（pA2 = 3.3）、3-氨基-2-羟基-2-苯基-丙基磺酸（pA2 = 3.5）、3-氨基-2-（苯并-(b)-呋喃-2-基）-丙基磺酸（pA2 = 4.3）和3-氨基-2-（4-氯苯基）-丙-1-烯磺酸（pA2 = 2.5-3），但没有一种比saclofen更有效，saclofen是目前发现的最有效的GABAB特异性拮抗剂。
Saclofen (the direct sulphonic analogue of baclofen) is a competitive antagonist of baclofen at GABAB receptors in guinea pig ileum and rat cortical slices (estimated pA2 = 5.3), at least twice as potent as 2-hydroxy-saclofen (pA2 = 5). A series of related sulphonic analogues also antagonised baclofen in the guinea pig ileum, including 2-hydroxy-saclofen amide (pA2 = 3.3), 3-amino-2-hydroxy-2-phenyl-propylsulphonic acid (pA2 = 3.5), 3-amino-2-(benzo-(b)-furan-2-yl)-propylsulphonic acid (pA2 = 4.3), and 3-amino-2-(4-chlorophenyl)-prop-1-enesulphonic acid (pA2 = 2.5-3), but none were more active than saclofen which is the most potent specific GABAB antagonist yet found.