Coupland N J, Bailey J E, Wilson S J, Potter W Z, Nutt D J
Psychopharmacology Unit, School of Medical Sciences, University of Bristol, England.
Clin Pharmacol Ther. 1994 Oct;56(4):420-9. doi: 10.1038/clpt.1994.156.
Ethoxyidazoxan, a potent and highly selective alpha 2-adrenergic receptor antagonist, was administered intravenously to six healthy male volunteers in a double-blind, placebo-controlled, dose-rising design. Doses of 6 micrograms/kg and 8 micrograms/kg infused intravenously over 30 minutes produced significant elevations of plasma norepinephrine and body temperature and inhibited norepinephrine-induced platelet aggregation. Central activity was shown by reversal of the slowing of saccadic eye movements and an increase in saccade peak velocity at the higher dose. Modest increases in blood pressure were produced without change in heart rate. Ethoxyidazoxan was well tolerated, with slight changes in subjective alertness and sedation.
依托昔唑啉是一种强效且高度选择性的α2-肾上腺素能受体拮抗剂，采用双盲、安慰剂对照、剂量递增设计，对6名健康男性志愿者进行静脉给药。静脉输注30分钟，剂量为6微克/千克和8微克/千克时，可使血浆去甲肾上腺素和体温显著升高，并抑制去甲肾上腺素诱导的血小板聚集。在较高剂量下，眼跳减慢得到逆转，眼跳峰值速度增加，表明有中枢活性。血压有适度升高，但心率无变化。依托昔唑啉耐受性良好，主观警觉性和镇静状态有轻微变化。
