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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本文引用的文献
1
Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.
2
The inhibition of noradrenaline uptake by drugs.药物对去甲肾上腺素摄取的抑制作用。
Adv Drug Res. 1965;2:1-46.
3
Mechanism of cocaine potentiation of responses to amines.可卡因增强对胺类反应的机制。
Br J Pharmacol. 1969 Mar;35(3):428-39. doi: 10.1111/j.1476-5381.1969.tb08284.x.
4
5
The pharmacological differentiation of adrenergic receptors.肾上腺素能受体的药理学分化
Ann N Y Acad Sci. 1967 Feb 10;139(3):553-70. doi: 10.1111/j.1749-6632.1967.tb41229.x.
6
Steric aspects of adrenergic drugs. 18. -Adrenergic receptors of mammalian aorta.肾上腺素能药物的空间因素。18. 哺乳动物主动脉的α-肾上腺素能受体。
Eur J Pharmacol. 1972 Jul;19(1):79-87. doi: 10.1016/0014-2999(72)90079-9.
7
A quantitative study of alpha adrenergic receptors in the spleen and aorta of the rabbit.兔脾脏和主动脉中α肾上腺素能受体的定量研究。
J Pharmacol Exp Ther. 1972 Feb;180(2):317-25.
8
Receptors for noradrenaline and histamine in the rabbit's posterior vena cava.家兔后腔静脉中去甲肾上腺素和组胺的受体
Br J Pharmacol Chemother. 1968 Jan;32(1):87-95. doi: 10.1111/j.1476-5381.1968.tb00432.x.
9
Competitive blockade of adrenergic alpha-receptors and histamine receptors by thymoxamine.噻吗心安对肾上腺素能α受体和组胺受体的竞争性阻断作用。
J Pharm Pharmacol. 1965 Jul;17(7):449-58. doi: 10.1111/j.2042-7158.1965.tb07701.x.
10
On the question of subclassification of -adrenoceptors.关于β-肾上腺素能受体的亚分类问题。
J Pharm Pharmacol. 1973 Mar;25(3):263-4. doi: 10.1111/j.2042-7158.1973.tb10638.x.
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