Gardocki J F, Hageman W E, Pruss T P
Arch Int Pharmacodyn Ther. 1978 Jun;233(2):326-42.
The pharmacological profile of a new centrally acting skeletal muscle relaxant, xilobam, is described and compared to that of existing skeletal muscle relaxants. The potencyof xilobam, administered intravenously, is approximately ten times that of methocarbamol in the linguomandibular assay in the cat. When evaluated in the strychnin assay in the mouse, the potency of xilobam is approximately seven times that of chlorzoxazone and eleven tomes that of methocarbamol and five times that of metaxalone. In contrast to methocarbamol, xilobam exhibits little or no sedative activity and appears devoid of antianxiety properties. When administered to non-anesthetized dogs, xilobam and other centrally acting muscle relaxants, such as chlorzoxazone and methocarbamol, increased arterial pressure and heart rate. Mydraiasis, vocalization and muscle rigidity were concomitantly observed. These effects appear to be centrally induced. It is concluded that xilobam appears to be a potent centrally acting muscle relaxant which should not be sedating or anxiolytic in man.
本文描述了一种新型中枢性骨骼肌松弛剂希洛巴胺的药理学特征，并与现有的骨骼肌松弛剂进行了比较。在猫的舌下颌试验中，静脉注射希洛巴胺的效力约为美索巴莫的十倍。在小鼠的士的宁试验中评估时，希洛巴胺的效力约为氯唑沙宗的七倍、美索巴莫的十一倍和美他沙酮的五倍。与美索巴莫不同，希洛巴胺几乎没有或没有镇静活性，且似乎没有抗焦虑特性。给未麻醉的狗给药时，希洛巴胺和其他中枢性肌肉松弛剂，如氯唑沙宗和美索巴莫，会升高动脉血压和心率。同时观察到瞳孔散大、发声和肌肉僵硬。这些效应似乎是由中枢诱导的。结论是，希洛巴胺似乎是一种强效的中枢性肌肉松弛剂，对人不应有镇静或抗焦虑作用。
