陈维洲, 丁光生. 四种苯骈二氧六环化合物的腎上腺素能阻断作用J. 药学学报, 1963, 10(2): 105-110.
引用本文: 陈维洲, 丁光生. 四种苯骈二氧六环化合物的腎上腺素能阻断作用J. 药学学报, 1963, 10(2): 105-110.
CHEN WEI-ZHOU AND TING KUANG-SHENG, . ADRENERGIC BLOCKING EFFECTS OF 4 BENZODIOXANESJ. Acta Pharmaceutica Sinica, 1963, 10(2): 105-110.
Citation: CHEN WEI-ZHOU AND TING KUANG-SHENG, . ADRENERGIC BLOCKING EFFECTS OF 4 BENZODIOXANESJ. Acta Pharmaceutica Sinica, 1963, 10(2): 105-110.

四种苯骈二氧六环化合物的腎上腺素能阻断作用

ADRENERGIC BLOCKING EFFECTS OF 4 BENZODIOXANES

  • 摘要: 四种苯駢二氧六环化合物的結构式为: 小白鼠腹腔注射BD-3,933F,BD-1和BD-5的LD50分別为0.1,0.20,0.26和0.22克/公斤,BD-3和933F組死亡多在1—3小时內,而BD-1和BD-5組死亡多在1—3天內。BD-5在小鼠能显著減低腎上腺素的毒性,而其他3药则不能。麻醉大白鼠和猫靜脉注射4药后均可引起降压,但4药间差异均不显著。BD-3,933F和BD-1使麻醉猫靜脉注射腎上腺素的升压引起反轉作用,而BD-5仅具抑制作用。对酪胺及去甲腎上腺素的升压,4药均可抑制。麻醉猫靜脉注射10毫克/公斤的933F有增血糖作用,BD-5注射20毫克/公斤才增高血糖。933F和BD-5对腎上腺素所引起的血糖及乳酸均无明显的抑制作用。因为BD-5同时阻断收縮和舒张血管的作用,但不引起腎上腺素的反轉作用,因此在治疗血管痙攣性疾患中可能比933F效果更好。

     

    Abstract: The structural formulae of the 4 benzodioxanes are: The intraperitoneal LD50's of BD-3, 933F, BD-1, and BD-5 in mice were 0.16,0.20, 0.26, and 0.22 g/kg respectively. Deaths of the animals occurred mostly in 1—3 hours for the BD-3 and 933F groups, while those for the BD-1 and BD-5 groups occurred mostly in 1—3 days. BD-5 markedly decreased the toxicity of intraperitoneal epinephrine in mice, whereas the other 3 compounds did not. Intravenous injections of these 4 drugs in anaesthetized rats and cats all produced a fall of blood pressure, but the differences among the hypotensive potencies were nonsignificant. BD-3, 933F, and BD-1 resulted in a reversal of the epinephrine hypertension in anaesthetized cats, while BD-5 yielded merely an inhibition. All these 4 compounds inhibited the pressor effects of tyramine and norepinephrine. Intravenous administration of 10 mg/kg of 933F in anaesthetized cats raised the blood glucose level, but BD-5 did so only at the dosage of 20mg/kg. BD-5 and 933F did not significantly inhibit the epinephrine-induced hyperglycemia and hyperlactacidemia. Since BD-5 blocked both vasoconstrictor and dilator responses and did not cause epinephrine reversal, it might be better than 933F in treating vasospastic diseases. Clinical trial is recommended.

     

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