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罗 31-1118、氟索洛尔和吲哚洛尔在人体中的部分激动剂活性评估。

An assessment of the partial agonist activity of Ro 31-1118, flusoxolol and pindolol in man.

作者信息

McCaffrey P M, Riddell J G, Shanks R G

机构信息

Department of Therapeutics and Pharmacology, Queen's University of Belfast.

出版信息

Br J Clin Pharmacol. 1987 Nov;24(5):571-80. doi: 10.1111/j.1365-2125.1987.tb03215.x.

DOI:10.1111/j.1365-2125.1987.tb03215.x
PMID:2893634
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1386328/
Abstract
  1. The effects of single oral doses of three beta-adrenoceptor partial agonists (Ro 31-1118, flusoxolol and pindolol), two beta-adrenoceptor antagonists (propranolol and atenolol), two beta-adrenoceptor agonists (salbutamol and prenalterol) and placebo on sleeping heart rate, quality of sleep, supine heart rate, exercise heart rate, blood pressure, forearm blood flow and finger tremor were studied in eight healthy male volunteers. 2. Sleeping heart rate was increased by Ro 31-1118, flusoxolol, pindolol, salbutamol and prenalterol and decreased by propranolol and atenolol. 3. None of the drugs studied affected quality of sleep. 4. Supine heart rate was increased by flusoxolol, prenalterol and salbutamol, unaffected by Ro 31-1118 and pindolol and reduced by propranolol and atenolol. 5. Exercise heart rate was reduced by both beta-adrenoceptor antagonists and the three partial agonists and unaffected by salbutamol and prenalterol. 6. Systolic blood pressure was increased by Ro 31-1118, flusoxolol, salbutamol and prenalterol, unaffected by pindolol and reduced by propranolol and atenolol. Diastolic blood pressure was reduced by salbutamol and prenalterol. 7. Forearm blood flow was increased by Ro 31-1118, salbutamol and prenalterol, unchanged by pindolol and flusoxolol and decreased by atenolol and propranolol. 8. Finger tremor was increased by Ro 31-1118, flusoxolol, pindolol, salbutamol, and prenalterol. 9. beta-adrenoceptor partial agonists have different effects on the cardiovascular system and finger tremor to beta-adrenoceptor antagonists. 10. While Ro 31-1118 and flusoxolol are antagonists mainly at the beta 1-adrenoceptor they have agonist activity at both beta 1- and beta 2 adrenoceptors. 11. While pindolol is a non-selective antagonist its agonist activity is mainly at the beta 2-adrenoceptor.
摘要
  1. 研究了单次口服三种β-肾上腺素能受体部分激动剂(Ro 31-1118、氟索洛尔和吲哚洛尔)、两种β-肾上腺素能受体拮抗剂(普萘洛尔和阿替洛尔)、两种β-肾上腺素能受体激动剂(沙丁胺醇和普瑞特罗)以及安慰剂对8名健康男性志愿者的睡眠心率、睡眠质量、仰卧心率、运动心率、血压、前臂血流量和手指震颤的影响。2. Ro 31-1118、氟索洛尔、吲哚洛尔、沙丁胺醇和普瑞特罗可使睡眠心率升高,普萘洛尔和阿替洛尔则使其降低。3. 所研究的药物均未影响睡眠质量。4. 氟索洛尔、普瑞特罗和沙丁胺醇可使仰卧心率升高,Ro 31-1118和吲哚洛尔对其无影响,普萘洛尔和阿替洛尔则使其降低。5. β-肾上腺素能受体拮抗剂和三种部分激动剂均可使运动心率降低,沙丁胺醇和普瑞特罗对其无影响。6. Ro 31-1118、氟索洛尔、沙丁胺醇和普瑞特罗可使收缩压升高,吲哚洛尔对其无影响,普萘洛尔和阿替洛尔则使其降低。沙丁胺醇和普瑞特罗可使舒张压降低。7. Ro 31-1118、沙丁胺醇和普瑞特罗可使前臂血流量增加,吲哚洛尔和氟索洛尔对其无影响,阿替洛尔和普萘洛尔则使其降低。8. Ro 31-1118、氟索洛尔、吲哚洛尔、沙丁胺醇和普瑞特罗可使手指震颤增加。9. β-肾上腺素能受体部分激动剂对心血管系统和手指震颤的作用与β-肾上腺素能受体拮抗剂不同。10. 虽然Ro 31-1118和氟索洛尔主要是β1-肾上腺素能受体拮抗剂,但它们在β1-和β2-肾上腺素能受体上均具有激动剂活性。11. 虽然吲哚洛尔是一种非选择性拮抗剂,但其激动剂活性主要在β2-肾上腺素能受体上。

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