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Selectivity of blocking agents for pre-and postsynaptic alpha-adrenoceptors.

作者信息

Doxey J C, Smith C F, Walker J M

出版信息

Br J Pharmacol. 1977 May;60(1):91-6. doi: 10.1111/j.1476-5381.1977.tb16752.x.

DOI:10.1111/j.1476-5381.1977.tb16752.x
PMID:18248
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1667189/
Abstract
  1. Low frequency (0.1 Hz) electrical stimulation of the rat isolated vas deferens produced regular contractions that were inhibited by low concentrations of clonidine. 2. The inhibition of the vas deferens produced by clonidine was presynaptic in origin and involved alpha-adrenoceptors. 3. Presynaptic alpha-adrenoceptor antagonist activity was assessed by studying the effects of increasing concentrations of the antagonists on cumulative clonidine dose-response curves on the stimulated vas deferens. 4. Postsynaptic alpha-adrenoceptor antagonist activity was assessed by comparison of control cumulative noradrenaline dose-response curves with those in the presence of increasing concentrations of antagonists in the rat anococcygeus muscle. 5. The results indicate that yohimbine and phentolamine are more potent in blocking presynaptic than postsynaptic alpha-adrenoceptors. Phenoxybenzamine and prazosin block postsynaptic alpha-adrenoceptors preferentially. 6. The findings support the view that presynaptic and postsynaptic alpha-adrenoceptors differ in their sensitivity to alpha-adrenoceptor antagonists.
摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0847/1667189/7d4a1e002da7/brjpharm00444-0095-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0847/1667189/cb1b4f4ad573/brjpharm00444-0094-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0847/1667189/4feb4835c9ad/brjpharm00444-0094-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0847/1667189/7d4a1e002da7/brjpharm00444-0095-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0847/1667189/cb1b4f4ad573/brjpharm00444-0094-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0847/1667189/4feb4835c9ad/brjpharm00444-0094-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0847/1667189/7d4a1e002da7/brjpharm00444-0095-a.jpg

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Selectivity of blocking agents for pre-and postsynaptic alpha-adrenoceptors.
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本文引用的文献

1
Cumulative dose-response curves. II. Technique for the making of dose-response curves in isolated organs and the evaluation of drug parameters.累积剂量-反应曲线。II. 离体器官中剂量-反应曲线的制作技术及药物参数的评估
Arch Int Pharmacodyn Ther. 1963;143:299-330.
2
Dual site of action of phenoxybenzamine in the cat's spleen; blockade of alpha-adrenergic receptors and inhibition of re-uptake of neurally released norepinephrine.酚苄明在猫脾脏中的双重作用位点;α-肾上腺素能受体阻断和对神经释放去甲肾上腺素再摄取的抑制。
Experientia. 1964 May 15;20(5):272-3. doi: 10.1007/BF02151802.
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The rat anococcygeus; a new, densely innervated smooth muscle preparation.
芒果(漆树科)叶的分级提取物和分离出的纯化合物对小鼠新奇诱导的竖毛和理毛行为的影响。
Afr J Tradit Complement Altern Med. 2013 Aug 12;10(5):244-55. doi: 10.4314/ajtcam.v10i5.5. eCollection 2013.
4
The effect of intrathecal mu, delta, kappa, and alpha-2 agonists on thermal hyperalgesia induced by mild burn on hind paw in rats.鞘内给予 μ、δ、κ 和 α-2 激动剂对大鼠后足底轻度烧伤诱导的热痛觉过敏的影响。
J Anesth. 2011 Dec;25(6):884-91. doi: 10.1007/s00540-011-1240-2. Epub 2011 Oct 9.
5
Post-junctional alpha-adrenoceptors and basal limb vascular tone in healthy men.健康男性的节后α-肾上腺素能受体与基础肢体血管张力
J Physiol. 2002 May 1;540(Pt 3):1103-10. doi: 10.1113/jphysiol.2001.015297.
6
Reductions in basal limb blood flow and vascular conductance with human ageing: role for augmented alpha-adrenergic vasoconstriction.随着人类衰老,基础肢体血流量和血管传导性降低:α-肾上腺素能血管收缩增强的作用。
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5
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J Physiol. 1974 Mar;237(3):505-19. doi: 10.1113/jphysiol.1974.sp010495.
8
Comparison of the effects of clonidine on pre- and postsynaptic adrenoceptors in the rabbit pulmonary artery. Alpha-sympathomimetic inhibition of Neurogenic vasoconstriction.可乐定对兔肺动脉突触前和突触后肾上腺素能受体作用的比较。神经源性血管收缩的α-拟交感神经抑制作用。
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9
Cardiovascular effects of prazosin in normotensive and genetically hypertensive rats.哌唑嗪对正常血压和遗传性高血压大鼠的心血管效应。
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10
Pre- and postsynaptic components in effect of drugs with alpha adrenoceptor affinity.具有α肾上腺素能受体亲和力的药物作用中的突触前和突触后成分。
Nature. 1975 Apr 3;254(5499):440-1. doi: 10.1038/254440a0.