Tanabe M, Kaneko T
Neuroscience Research Laboratories, Sankyo Co. Ltd., Tokyo, Japan.
Eur J Pharmacol. 1996 Oct 17;313(3):187-9. doi: 10.1016/0014-2999(96)00634-6.
We studied the modulatory effect of (R)-4-chloro-2-(2-hydroxy-3-morpholinopropyl)-5-phenyl-4-isoxaz olin-3-one hydrochloride (CS-722), a centrally acting muscle relaxant, on synaptic transmission in the ventral horn neurons of neonatal rat lumbar spinal cord in slices using whole cell recording techniques. Pharmacologically isolated excitatory or inhibitory postsynaptic currents (EPSCs and IPSCs) were evoked by stimulating neighboring neurons. CS-722 preferentially enhanced IPSCs with little effects on EPSCs. Moreover, CS-722 reduced paired pulse facilitation of gamma-aminobutyric acid (GABA)-mediated IPSCs, suggesting its action on the presynaptic terminal. Preferential facilitatory effects on inhibitory synaptic transmission seem to be one of the mechanisms underlying muscle relaxation of this compound.
我们使用全细胞记录技术,研究了中枢性肌肉松弛剂(R)-4-氯-2-(2-羟基-3-吗啉基丙基)-5-苯基-4-异恶唑啉-3-酮盐酸盐(CS-722)对新生大鼠腰脊髓腹角神经元切片中突触传递的调节作用。通过刺激相邻神经元诱发药理学分离的兴奋性或抑制性突触后电流(EPSC和IPSC)。CS-722优先增强IPSC,对EPSC影响很小。此外,CS-722降低了γ-氨基丁酸(GABA)介导的IPSC的双脉冲易化,提示其作用于突触前终末。对抑制性突触传递的优先易化作用似乎是该化合物肌肉松弛作用的潜在机制之一。