摄取1对犬隐静脉中α-肾上腺素能受体拮抗剂效价的影响。
The effects of uptake1 on alpha-adrenoceptor antagonist potency in dog saphenous vein.
作者信息
Humphrey P P
出版信息
Br J Pharmacol. 1978 Aug;63(4):665-9. doi: 10.1111/j.1476-5381.1978.tb17280.x.
Abstract
1 The effects of alpha-adrenoceptor antagonists on contractile responses to noradrenaline and methoxamine were examined in isolated saphenous vein strips of the dog. 2 Phentolamine, labetalol and thymoxamine antagonized responses to methoxamine to a greater extent than responses to noradrenaline. 3 Cocaine (3.0 x 10(-5) mol/l) increased the potency of noradrenaline by about eight fold, but had little or no effect on the potency of methoxamine. 4 In the presence of cocaine (3.0 x 10(-5) mol/l) the potency of the antagonists against noradrenaline was increased such that the pA2 values were then similar to those obtained against methoxamine. 5 It is concluded that the lower potency of phentolamine, labetalol and thymoxamine as antagonists of noradrenaline than of methoxamine is due to the presence of an avid saturable uptake1 process in the saphenous vein.
摘要
- 在犬的离体隐静脉条上研究了α-肾上腺素能受体拮抗剂对去甲肾上腺素和甲氧明收缩反应的影响。2. 酚妥拉明、拉贝洛尔和噻吗洛尔对甲氧明反应的拮抗作用比对去甲肾上腺素反应的拮抗作用更强。3. 可卡因（3.0×10⁻⁵mol/L）使去甲肾上腺素的效价增加约8倍，但对甲氧明的效价几乎没有影响。4. 在可卡因（3.0×10⁻⁵mol/L）存在的情况下，拮抗剂对去甲肾上腺素的效价增加，使得pA2值与对甲氧明获得的值相似。5. 得出结论，酚妥拉明、拉贝洛尔和噻吗洛尔作为去甲肾上腺素拮抗剂的效价比作为甲氧明拮抗剂的效价低，是由于隐静脉中存在一种 avid 可饱和摄取1过程。
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