Pharmacological studies on 6-amino-2-fluoromethyl-3-(O-tolyl)-4(3H)-quinazolinone (afloqualone), a new centrally acting muscle relaxant. (II) Effects on the spinal reflex potential and the rigidity.
Pharmacological studies on 6-amino-2-fluoromethyl-3-(O-tolyl)-4(3H)-quinazolinone (afloqualone), a new centrally acting muscle relaxant. (II) Effects on the spinal reflex potential and the rigidity.
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6-氨基-2-氟甲基-3-(O-甲苯基)-4(3H)-喹唑啉酮（afloqualone）的药理学研究，一种新型中枢作用肌肉松弛剂。
DOI：
10.1254/jjp.32.427
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发表时间：
1982
期刊：
影响因子：
--
通讯作者：
R. Ishida
中科院分区：
文献类型：
--
作者：
T. Ochiai;R. Ishida
在实验动物中研究了阿氟喹酮对单突触反射 (MSR) 和多突触反射 (PSR) 电位以及 α 和 γ 刚性的影响。尽管如前一篇论文报道的那样，阿氟喹酮对猫的髌骨反射没有抑制作用，但阿氟喹酮剂量依赖性地抑制脊椎猫的 MSR 和 PSR 电位。 Afloqualone 与 tolperisone 一样，比 MSR 电位更选择性地抑制 PSR 电位，而巴氯芬以相反的顺序抑制它们。然而，阿氟喹酮的 PSR 潜力选择性高于甲苯哌丙酮。在大鼠和猫中，口服给药时，阿氟喹酮剂量依赖性地放松α-和γ-刚性。以及静脉注射其对α-刚性的50%抑制剂量是对γ-刚性的1.5-2倍。托哌酮还放松了静脉注射中的这两种刚性。给药，但口服给药时效果甚微。只有美菲新可以缓解猫缺血后的脊柱僵硬。这些结果表明，与除巴氯芬之外的其他众所周知的中枢作用肌肉松弛剂一样，阿氟喹酮对多突触通路的抑制比对脊髓的单突触通路的抑制更强烈，对伽玛系统的抑制比对α系统的抑制更强烈。
Effects of afloqualone on mono- (MSR) and poly-synaptic reflex (PSR) potentials and alpha- and gamma-rigidities were studied in experimental animals. Afloqualone dose dependently inhibited both MSR and PSR potentials in spinalized cats though afloqualone had no inhibitory effect on the patellar reflex in cats as reported in the previous paper. Afloqualone, like tolperisone, more selectively inhibited the PSR potential than MSR potential, whereas baclofen inhibited them in reverse order. However, the selectivity towards the PSR potential was higher with afloqualone than with tolperisone. In rats and cats, afloqualone dose dependently relaxed both alpha- and gamma-rigidity when administered p.o. as well as i.v. Its 50% inhibitory dose for alpha-rigidity was 1.5-2 times larger than that for gamma-rigidity. Tolperisone also relaxed both rigidities in i.v. administration, but had little effect when given p.o. Only mephenesin relaxed the post-ischaemic spinal rigidity in cats. These results suggest that afloqualone, like other well known centrally acting muscle relaxants except for baclofen, more strongly inhibits the polysynaptic pathway than the mono-synaptic pathway of the spinal cord as well as more strongly the gamma-system than the alpha-system.