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利多卡因的苄基氨基甲酰类似物:血管减压作用机制

Benzyl carbamyl analogue of lignocaine: vasodepressor mechanism of action.

作者信息

Chiang Y L, Freeman J J, Sowell J W, Kosh J W

出版信息

Clin Exp Pharmacol Physiol. 1982 Nov-Dec;9(6):645-55. doi: 10.1111/j.1440-1681.1982.tb00836.x.

DOI:10.1111/j.1440-1681.1982.tb00836.x
PMID:7166009
Abstract
  1. The benzyl carbamyl analogue of lignocaine [2-(diethylaminoacetamido)-3-carbamyl-4-methyl-5-benzylpyrrole] at an intravenous dose of 4 mg/kg caused a blood pressure decrease of 54 mmHg. 2. A greater hypotensive effect was observed in hypertensive compared to normotensive animals. Anaesthesia magnified the vasodepressor effect in both groups. 3. The analogue did not possess centrally-mediated effects on blood pressure but exerted its hypotensive effect via a peripheral mechanism. 4. The analogue produced a relaxant effect on intestinal and vascular smooth muscle while exerting minimal effects on muscarinic, sympathetic, or ganglionic nicotinic receptors. 5. The analogue exhibited less cardiac depressant action on left ventricular rate (dp/dt) and force of contraction than lignocaine. 6. Lethal effects for the analogue were first observed at 16 mg/kg following intravenous administration and at 500 mg/kg following intraperitoneal administration. 7. In conclusion, the benzyl carbamyl analogue exhibited direct vascular smooth muscle relaxant activity with less cardiac or CNS side effects than lignocaine.
摘要
  1. 利多卡因的苄基氨基甲酰类似物[2-(二乙氨基乙酰胺基)-3-氨基甲酰基-4-甲基-5-苄基吡咯]静脉注射剂量为4mg/kg时,可使血压下降54mmHg。2. 与血压正常的动物相比,高血压动物的降压作用更明显。麻醉使两组的血管减压作用均增强。3. 该类似物对血压无中枢介导作用,其降压作用是通过外周机制实现的。4. 该类似物对肠道和血管平滑肌有舒张作用,而对毒蕈碱、交感神经或神经节烟碱受体的作用极小。5. 该类似物对左心室速率(dp/dt)和收缩力的心脏抑制作用比利多卡因小。6. 静脉注射后,该类似物在16mg/kg时首次出现致死效应,腹腔注射后在500mg/kg时出现致死效应。7. 总之,苄基氨基甲酰类似物具有直接的血管平滑肌舒张活性,与利多卡因相比,心脏或中枢神经系统副作用较小。

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