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夸唑定(MJ - 1988)的心血管药理学,特别涉及对心肌血流量和代谢产热的影响。

Cardiovascular pharmacology of quazodine (MJ-1988), with particular reference to effects of myocardial blood flow and metabolic heat production.

作者信息

Parratt J R, Winslow E

出版信息

Br J Pharmacol. 1971 Jun;42(2):193-204. doi: 10.1111/j.1476-5381.1971.tb07100.x.

Abstract
  1. The effects of intravenous infusions of quazodine (6,7-dimethoxy-4-ethylquinazoline; MJ-1988) on myocardial blood flow, myocardial metabolic heat production and on general haemodynamics have been studied in cats anaesthetized with sodium pentobarbitone.2. Quazodine (0.25 and 0.5 (mg/kg)/min for 10 min) decreased diastolic blood pressure, peripheral vascular resistance, systolic ejection time and left ventricular end-diastolic pressure. Heart rate, cardiac effort, output and external work and left ventricular dP/dt were markedly increased. These changes are indicative of increased myocardial contractility and peripheral vasodilatation.3. In a dose of (1.0 mg/kg)/min, quazodine had a more marked hypotensive effect, systolic pressure being significantly reduced, and had less effect on left ventricular dP/dt and cardiac effort. Calculated external cardiac work was slightly reduced and there were very occasional nodal arrhythmias.4. Changes in heart rate, aortic dP/dt and diastolic blood pressure induced by quazodine were unaffected by the previous administration of the beta-adrenoceptor blocking agent alprenolol in a dose (1.0 mg/kg) which abolished the effects of isoprenaline.5. In all doses, quazodine markedly increased local blood flow (by 70-540%) around an implanted myocardial heated thermocouple recorder. ;Corrected temperature', an index of local myocardial metabolic heat production, was almost unchanged and it is suggested that increased myocardial contractility, occurring with unchanged metabolic heat production and oxygen consumption, probably results from a concomitant decrease in intramural wall tension.
摘要
  1. 已在戊巴比妥钠麻醉的猫身上研究了静脉输注喹唑定(6,7 - 二甲氧基 - 4 - 乙基喹唑啉;MJ - 1988)对心肌血流量、心肌代谢产热以及全身血流动力学的影响。

  2. 喹唑定(0.25和0.5(毫克/千克)/分钟,持续10分钟)可降低舒张压、外周血管阻力、收缩期射血时间和左心室舒张末期压力。心率、心脏作功、输出量、外功以及左心室dP/dt均显著增加。这些变化表明心肌收缩力增强和外周血管扩张。

  3. 以(1.0毫克/千克)/分钟的剂量给药时,喹唑定具有更显著的降压作用,收缩压显著降低,对左心室dP/dt和心脏作功的影响较小。计算得出的心脏外功略有降低,偶尔会出现结性心律失常。

  4. 喹唑定引起的心率、主动脉dP/dt和舒张压变化不受先前给予剂量为(1.0毫克/千克)的β - 肾上腺素能受体阻滞剂阿普洛尔的影响,该剂量的阿普洛尔可消除异丙肾上腺素的作用。

  5. 在所有剂量下,喹唑定均可使植入心肌的热偶记录器周围的局部血流量显著增加(增加70 - 540%)。“校正温度”是局部心肌代谢产热的指标,几乎未发生变化,提示在代谢产热和耗氧量不变的情况下心肌收缩力增强,可能是由于壁内张力同时降低所致。

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本文引用的文献

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Thermal-dilution technics.热稀释技术。
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PHARMACOLOGIC APPROACH TO THE TREATMENT OF SHOCK.
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A method for the calculation of areas under indicator-dilution curves.
J Appl Physiol. 1966 Mar;21(2):695-9. doi: 10.1152/jappl.1966.21.2.695.

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