Sawynok J
Neuropharmacology. 1986 Jul;25(7):795-8. doi: 10.1016/0028-3908(86)90098-5.
Following intrathecal injection, pretreatment with both D-baclofen and 5-aminovaleric acid (5-AV) inhibited the antinociceptive effect of L-baclofen, but homotaurine (3-aminopropane sulphonic acid, APS) was inactive as an antagonist (rank order D-baclofen greater than 5-AV greater than APS = 0). In an established GABAB system, the electrically stimulated guinea pig longitudinal muscle myenteric plexus preparation, APS and 5-AV but not D-baclofen reduced the inhibitory effect of L-baclofen (APS = 5-AV greater than D-baclofen = 0). Receptors with which baclofen interacts in the spinal cord to produce antinociception differ from GABAB receptors with respect to the rank order of potency of antagonists as well as close structural analogs, and these criteria could be used for characterization of such receptors.
鞘内注射后，D-巴氯芬和5-氨基戊酸（5-AV）预处理均抑制了L-巴氯芬的镇痛作用，但高牛磺酸（3-氨基丙烷磺酸，APS）作为拮抗剂无活性（效力顺序为D-巴氯芬大于5-AV大于APS = 0）。在已建立的GABAB系统，即电刺激豚鼠纵肌肠肌丛标本中，APS和5-AV而非D-巴氯芬降低了L-巴氯芬的抑制作用（APS = 5-AV大于D-巴氯芬 = 0）。巴氯芬在脊髓中相互作用产生镇痛作用的受体，在拮抗剂以及结构类似物的效力顺序方面不同于GABAB受体，这些标准可用于此类受体的表征。
