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托美索酯,一种通过对血管平滑肌产生直接舒张作用来降低血压的药物。

Tolmesoxide, a drug that lowers blood pressure by a direct relaxant effect on vascular smooth muscle.

作者信息

Doxey J C

出版信息

Br J Pharmacol. 1978 May;63(1):111-8. doi: 10.1111/j.1476-5381.1978.tb07780.x.

Abstract

1 The blood pressure of conscious, deoxycorticosterone acetate (DOCA) hypertensive and 1 kidney Goldblatt hypertensive rats and renal hypertensive and normotensive cats was reduced by tolmesoxide (4,5-dimethoxy-o-tolyl methyl sulphoxide). 2 Tachycardia accompanied the hypotension. In rats the increase in heart rate was abolished by concurrent administration of propranolol. Tachycardia did not occur in pithed rats. 3 Vascoconstriction induced by sympathetic stimulation, noradrenaline, tyramine, angiotensin or vasporessin was antagonized by tolmesoxide. 4 The antagonism of vasoconstrictor responses produced by tolmesoxide was unaffected by beta-adrenoceptor, muscarinic or histamine antagonists. 5 It is concluded that the lowering of pressure produced by tolmesoxide results from a defect relaxant effect on vascular smooth muscle.

摘要
  1. 甲苯磺氧化物(4,5-二甲氧基-邻甲苯基甲基亚砜)可降低清醒的、醋酸脱氧皮质酮(DOCA)高血压大鼠、单肾 Goldblatt 高血压大鼠以及肾性高血压和正常血压猫的血压。2. 低血压伴有心动过速。在大鼠中,同时给予普萘洛尔可消除心率的增加。在脊髓损毁的大鼠中未出现心动过速。3. 甲苯磺氧化物可拮抗交感神经刺激、去甲肾上腺素、酪胺、血管紧张素或血管加压素诱导的血管收缩。4. 甲苯磺氧化物对血管收缩反应的拮抗作用不受β-肾上腺素能受体、毒蕈碱或组胺拮抗剂的影响。5. 得出的结论是,甲苯磺氧化物产生的降压作用源于其对血管平滑肌的舒张作用缺陷。
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f74c/1668277/c8cbe6296d24/brjpharm00432-0110-a.jpg

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