Hasuo H, Gallagher J P
Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77550.
Neurosci Lett. 1988 Mar 21;86(1):77-81. doi: 10.1016/0304-3940(88)90186-3.
Phaclofen has recently been described as an antagonist to baclofen at both peripheral and central receptors. We have applied phaclofen in known concentrations to an isolated rat brain slice preparation containing the septal nuclei. Our data demonstrate that phaclofen antagonizes responses to exogenously applied baclofen in a competitive manner. On the other hand, phaclofen is not as effective in antagonizing competitively the synaptically mediated late hyperpolarizing response (LHP) recorded from the same or similar dorsolateral septal nucleus (DLSN) neurons from which baclofen responses were recorded. Our data support the usefulness of phaclofen as a competitive antagonist of baclofen, and suggest that when larger stimulus intensities are applied, the LHP in the dorsolateral septum of the rat may be mediated by a transmitter in addition to gamma-aminobutyric acid (GABA).
最近有研究表明,巴氯芬在外周和中枢受体上都有拮抗剂,即法氯芬。我们将已知浓度的法氯芬应用于含有隔核的离体大鼠脑片标本。我们的数据表明,法氯芬以竞争性方式拮抗外源性应用巴氯芬的反应。另一方面,法氯芬在竞争性拮抗从记录巴氯芬反应的相同或相似背外侧隔核(DLSN)神经元记录的突触介导的晚期超极化反应(LHP)方面效果不佳。我们的数据支持法氯芬作为巴氯芬竞争性拮抗剂的有效性,并表明当施加更大的刺激强度时,大鼠背外侧隔区的LHP可能除了γ-氨基丁酸(GABA)之外还由一种神经递质介导。