Palluk R, Hoefke W, Gaida W
Arzneimittelforschung. 1985;35(1A):395-401.
The effects of the selective alpha 1-and alpha 2-adrenergic agonists phenylephrine and B-HT 920 (2-amino-6-allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine) and the respective antagonists prazosin and yohimbine on smooth muscle activity of isolated rat aorta, rabbit vena cava inferior and rabbit vena ischiadica have been investigated. In addition, the influence of angiotensin II on the effects of these agonists and antagonists was evaluated. Among the two agonists phenylephrine was the most potent in the rat aorta and B-HT 920 in the two venous vessels. Prazosin and yohimbine revealed a competitive antagonism against both agonists in all three vessels. No differentiation between alpha 1- and alpha 2-adrenoceptor mediated responses was seen in rat aorta and rabbit vena ischiadica. In the rabbit vena cava, prazosin was more potent against phenylephrine than against B-HT 920 whilst yohimbine was more potent against B-HT 920 than against phenylephrine, thus pointing to the existence of functional alpha 1- and alpha 2-adrenoceptors. Angiotensin II (5 X 10(-9) mol/l) induced sustained contractions in rat aorta and transient contractions of different relative magnitude in the veins. Angiotensin II pretreatment increased the potency of phenylephrine in all vessels with no influence on maximum contraction. B-HT 920 potency was increased in the vein preparations; maximum contractions were increased in rat aorta, decreased in rabbit vena cava and not influenced in rabbit vena ischiadica.(ABSTRACT TRUNCATED AT 250 WORDS)
研究了选择性α1和α2肾上腺素能激动剂去氧肾上腺素和B-HT 920(2-氨基-6-烯丙基-5,6,7,8-四氢-4H-噻唑并[4,5-d]氮杂卓)以及相应的拮抗剂哌唑嗪和育亨宾对离体大鼠主动脉、兔下腔静脉和兔坐骨神经静脉平滑肌活性的影响。此外,还评估了血管紧张素II对这些激动剂和拮抗剂作用的影响。在这两种激动剂中,去氧肾上腺素对大鼠主动脉作用最强,而B-HT 920对两条静脉血管作用最强。哌唑嗪和育亨宾在所有三种血管中均显示出对两种激动剂的竞争性拮抗作用。在大鼠主动脉和兔坐骨神经静脉中,未观察到α1和α2肾上腺素能受体介导反应的差异。在兔下腔静脉中,哌唑嗪对去氧肾上腺素的作用比对B-HT 920更强,而育亨宾对B-HT 920的作用比对去氧肾上腺素更强,因此表明存在功能性α1和α2肾上腺素能受体。血管紧张素II(5×10−9mol/L)在大鼠主动脉中诱导持续收缩,在静脉中诱导不同相对强度的短暂收缩。血管紧张素II预处理增加了所有血管中去氧肾上腺素的效力,对最大收缩无影响。B-HT 920在静脉制剂中的效力增加;大鼠主动脉中的最大收缩增加,兔下腔静脉中的最大收缩减少,兔坐骨神经静脉中的最大收缩不受影响。(摘要截短于250字)