Uesaka I, Kubo S, Matsubara I, Kasé Y
Arzneimittelforschung. 1977 Jul;27(7):1439-45.
Pharmacological effects of o-chloro-alpha-[(tert.-butylamino)methyl]benzylalcohol hydrochloride (C-78) on the nervous systems and miscellaneous organs were studied. 1. Through a low dosage of C-78 had little influence on the central nervous system, a high dosage of C-78 had a little slow-waving effect on the spontaneous EEG in rabbits, inhibitory action of the convulsion caused by pentetrazol or electroshock in mice and anti-pyrogenic action in rabbits. C-78 also dose-dependently inhibited the increase of motility caused by amphetamine in mice. 2. Only high concentrations of C78 had a local anesthetic action on the cornea and the skin of the back in guinea pigs. 3. C-78 significantly increased non-esterified fatty acids (NEFA) and glucose contents of blood in rabbits, but these actions were inhibited by propranolol. Another, high dosage of C-78 had anti-ulcer and anti-inflammatory action. From the results of the previous experiments and this study, it was concluded that C-78 is a new beta 2-receptor stimulating drug where beta 2-receptor selectivity is greater than that of isoproterenol, salbutamol and clorprenaline.
研究了盐酸邻氯-α-[(叔丁氨基)甲基]苄醇(C-78)对神经系统和其他器官的药理作用。1. 低剂量的C-78对中枢神经系统影响不大,高剂量的C-78对兔自发脑电图有轻微的慢波作用,对小鼠戊四氮或电休克所致惊厥有抑制作用,对兔有解热作用。C-78还剂量依赖性地抑制小鼠中由苯丙胺引起的运动增加。2. 仅高浓度的C78对豚鼠角膜和背部皮肤有局部麻醉作用。3. C-78显著增加兔血液中非酯化脂肪酸(NEFA)和葡萄糖含量,但这些作用被普萘洛尔抑制。此外,高剂量的C-78有抗溃疡和抗炎作用。根据先前实验和本研究的结果,得出结论:C-78是一种新型β2受体激动剂,其对β2受体的选择性大于异丙肾上腺素、沙丁胺醇和氯丙那林。