酚妥拉明对生物胺及神经腺接头处递质反应的竞争性拮抗作用。
Competitive antagonism by phentolamine of responses to biogenic amines and the transmitter at a neuroglandular junction.
作者信息
Bowser-Riley F, House C R, Smith R K
出版信息
J Physiol. 1978 Jun;279:473-89. doi: 10.1113/jphysiol.1978.sp012357.
Abstract
- A quantitative study has been made of phentolamine's inhibition of the electrical and secretory responses of the isolated salivary glands of Nauphoeta cinerea Olivier to nerve stimulation and bath applications of agonists. 2. The results suggested that phentolamine is a competitive antagonist having an affinity constant of about 1 micrometer-1 for the receptors for dopamine, noradrenaline, adrenaline and the neurotransmitter. 3. Phentolamine also inhibited responses to 5-hydroxytryptamine in a manner seemingly more complex than competitive antagonism. Attempts to estimate the affinity constant gave values of about 0.08 and 0.015 microgram-1 for inhibition of the secretory and electrical responses respectively. 4. This investigation showed that phentolamine discriminates between two kinds of receptor in this gland, one binding 5-hydroxytryptamine and the other combining with catecholamines and the neurotransmitter.
摘要
- 已经对酚妥拉明抑制烟草甲（Nauphoeta cinerea Olivier）离体唾液腺对神经刺激和激动剂浴应用的电反应和分泌反应进行了定量研究。2. 结果表明，酚妥拉明是一种竞争性拮抗剂，对多巴胺、去甲肾上腺素、肾上腺素和神经递质的受体具有约1微摩尔-1的亲和常数。3. 酚妥拉明对5-羟色胺反应的抑制方式似乎比竞争性拮抗作用更复杂。估计亲和常数的尝试分别得出抑制分泌反应和电反应的约0.08和0.015微克-1的值。4. 这项研究表明，酚妥拉明在该腺体中区分两种受体，一种结合5-羟色胺，另一种与儿茶酚胺和神经递质结合。
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