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介导沙丁胺醇代谢作用的β-肾上腺素能受体亚型的特征分析。

Characterization of beta-adrenoceptor subtype mediating the metabolic actions of salbutamol.

作者信息

Berend N, Marlin G E

出版信息

Br J Clin Pharmacol. 1978 Mar;5(3):207-11. doi: 10.1111/j.1365-2125.1978.tb01625.x.

Abstract
  1. The following four intravenous treatments were administered in a balanced, randomized, Latin square design to four healthy volunteers: (1) saline injection (10 min); salbutamol infusion (0.15 microgram kg-1 min-1 for 60 min) (sS), (2) propranolol injection (0.3 mg kg-1 for 10 min); salbutamol infusion (pS), (3) practolol injection (2 mg kg-1 for 10 min); salbutamol infusion (PS) and (4) saline injection; saline infusion (ss). 2. Heart rate was recorded and venous blood taken for estimation of insulin, glucose and potassium before and after each injection (0 and 12-15 min) and at various times during the infusion (30,45,60 and 75 min). 3. The mean, peak % heart rate changes from baseline, control were +65.8%, +23.0%, -10.9% and -12.1%, the mean, peak % glucose changes, +61.0%, +7.1%, +3.6% and +6.9%, and the mean, peak % insulin changes, +298%, +28%, -28% and -43% during the infusions for sS, PS, ss and pS respectively. 4. The mean serum potassium levels before the injections and at the completion of the infusions were 3.98 and 3.08 4.03 and 3.63, 4.07 and 4.15, and 4.03 and 4.13 meq/l for sS, PS, ss and pS respectively. 5. Propanolol completely abolished the cardiac and metabolic responses of salbutamol. 6. Practolol produced only partial cardiac beta-adrenoceptor blockade, but completely inhibited the metabolic actions of salbutamol.
摘要
  1. 采用平衡、随机、拉丁方设计,对四名健康志愿者进行了以下四种静脉治疗:(1) 注射生理盐水(10分钟);输注沙丁胺醇(0.15微克/千克/分钟,持续60分钟)(sS),(2) 注射普萘洛尔(0.3毫克/千克,持续10分钟);输注沙丁胺醇(pS),(3) 注射醋氨心安(2毫克/千克,持续10分钟);输注沙丁胺醇(PS),以及(4) 注射生理盐水;输注生理盐水(ss)。2. 在每次注射前及注射后(0和12 - 15分钟)以及输注期间的不同时间点(30、45、60和75分钟)记录心率,并采集静脉血以测定胰岛素、葡萄糖和钾。3. 在输注期间,sS、PS、ss和pS的平均心率从基线变化的峰值百分比分别为+65.8%、+23.0%、 - 10.9%和 - 12.1%,平均血糖变化的峰值百分比分别为+61.0%、+7.1%、+3.6%和+6.9%,平均胰岛素变化的峰值百分比分别为+298%、+28%、 - 28%和 - 43%。4. sS、PS、ss和pS在注射前及输注结束时的平均血清钾水平分别为3.98和3.08、4.03和3.63、4.07和4.15以及4.03和4.13毫当量/升。5. 普萘洛尔完全消除了沙丁胺醇的心脏和代谢反应。6. 醋氨心安仅产生部分心脏β - 肾上腺素能受体阻滞,但完全抑制了沙丁胺醇的代谢作用。

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