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哌罗克生和2-(2-咪唑啉基)-1,4-苯并二恶烷(170 150)对大鼠突触前和突触后受体的比较研究

[Comparative study of piperoxan and 2-(2-imidazolinyl)-1, 4-benzodioxane (170 150) on pre- and postsynaptic receptors in the rat].

作者信息

Mouillé P, Dabiré H, Fournier B, Schmitt H

出版信息

J Pharmacol. 1982 Jul-Sep;13(3):389-97.

PMID:6290793
Abstract
  1. 170 150 (imidazolinyl-2)-2-benzodioxane 1-4), as does piperoxan, competitively antagonizes the hypertension induced by clonidine in the pithed rat. Piperoxan appears slightly less potent than 170 150 in this preparation as shown by the comparison of the apparent pA10 values: 5.3 for piperoxan versus 5.4 for 170 150. 2. The two drugs antagonize the reduction of the electrically-induced tachycardia produced by clonidine. 170 150 appears to be 3-fold more potent than piperoxan in this preparation. 3. These results are compatible with a blockade of alpha 2-pre and postsynaptic adrenoceptors of the rat by piperoxan and 170 150 appears to be 3-fold more potent than piperoxan in this preparation. 3. These results are compatible with a blockade of alpha 2-pre and postsynaptic adrenoceptors of the rat by piperoxan and 170 150 and they are in agreement with our previous results which indicate that compound 170 150 shows a preferential affinity for alpha 2-adrenoceptors.
摘要
  1. 170 150(咪唑啉基-2)-2-苯并二恶烷1-4)与哌罗克生一样,能竞争性拮抗去脑大鼠中可乐定诱导的高血压。在该制剂中,哌罗克生的效力似乎略低于170 150,表观pA10值的比较表明:哌罗克生为5.3,而170 150为5.4。2. 这两种药物能拮抗可乐定引起的电诱导心动过速的减慢。在该制剂中,170 150的效力似乎比哌罗克生强3倍。3. 这些结果与哌罗克生对大鼠α2-突触前和突触后肾上腺素能受体的阻断作用相符,且在该制剂中170 150的效力似乎比哌罗克生强3倍。3. 这些结果与哌罗克生和170 150对大鼠α2-突触前和突触后肾上腺素能受体的阻断作用相符,并且与我们之前的结果一致,即化合物170 150对α2-肾上腺素能受体表现出优先亲和力。

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