Goldschmidt P L, Frances H, Simon P
Pharmacol Biochem Behav. 1984 Aug;21(2):177-80. doi: 10.1016/0091-3057(84)90210-7.
The effects of 3 beta-adrenergic agonists (clenbuterol, isoproterenol and salbutamol) on the spontaneous motor activity of mice were studied. The present research indicated that motor activity was significantly decreased 30 minutes after IP injection of either clenbuterol (0.06 mg/kg), isoproterenol (0.5 mg/kg) or salbutamol (2 mg/kg). Hypomotility induced by clenbuterol was also significantly antagonized by propranolol in doses ranging from 1 to 8 mg/kg and by penbutolol in doses from 0.03 to 0.5 mg/kg. However, practolol, which does not cross the blood brain barrier, did not antagonize the effect of clenbuterol. Therefore, it may be hypothesized that beta adrenergic agonists decrease motor activity by a central mechanism. It was also found that tachyphylaxis or resistance to treatment, observed in cardiovascular and bronchopulmonary systems with beta-adrenergic agonists, developed after 7 injections of clenbuterol (0.25 mg/kg IP, twice daily) in the behavioral model of spontaneous motor activity in mice.
研究了3种β-肾上腺素能激动剂(克伦特罗、异丙肾上腺素和沙丁胺醇)对小鼠自发运动活性的影响。本研究表明,腹腔注射克伦特罗(0.06mg/kg)、异丙肾上腺素(0.5mg/kg)或沙丁胺醇(2mg/kg)30分钟后,运动活性显著降低。普萘洛尔剂量为1至8mg/kg以及喷布洛尔剂量为0.03至0.5mg/kg时,也能显著拮抗克伦特罗诱导的运动减弱。然而,不能透过血脑屏障的醋氨心安不能拮抗克伦特罗的作用。因此,可以推测β-肾上腺素能激动剂通过中枢机制降低运动活性。还发现在小鼠自发运动活性的行为模型中,连续7次注射克伦特罗(0.25mg/kg腹腔注射,每日两次)后,出现了β-肾上腺素能激动剂在心血管和支气管肺系统中所观察到的快速减敏或耐药现象。