新型氟哌啶醇类似物的合成及其与大鼠腮腺切片和人血小板膜中α-肾上腺素能受体相互作用的表征。
Synthesis of new haloperidol analogues and characterization of their interactions with alpha-adrenoceptors in rat parotid slices and human platelet membranes.
作者信息
Atlas D, Friedman Z, Litvin Y, Steer M L
出版信息
Br J Pharmacol. 1982 Jan;75(1):213-7. doi: 10.1111/j.1476-5381.1982.tb08775.x.
Abstract
1 The synthesis of several butyrophenone analogues of haloperidol is described. 2 The effects of these compounds on alpha-adrenoceptors were evaluated by examining their ability to reduce alpha 1-stimulated K+ release from rat parotid slices and to displace [3H]-phentolamine from human platelet membrane alpha 2-adrenoceptors. 3 The affinity of haloperidol and its analogues for alpha 1-receptors was found to be 1 to 2 orders of magnitude greater than that for alpha 2-adrenoceptors. These observations suggest that most of the alpha-adrenoceptor activity of butyrophenones results from their interaction with alpha 1-adrenoceptors. 4 The relatively high affinity of the butyrophenones for alpha 1-adrenoceptors suggests that they may be useful as probes in studies of alpha 1-adrenoceptors in these and other tissues.
摘要
- 描述了几种氟哌啶醇丁酰苯类似物的合成。2. 通过检测这些化合物降低大鼠腮腺切片中α1刺激的钾离子释放以及从人血小板膜α2肾上腺素能受体上置换[3H] - 酚妥拉明的能力，评估了它们对α肾上腺素能受体的作用。3. 发现氟哌啶醇及其类似物对α1受体的亲和力比对α2肾上腺素能受体的亲和力大1至2个数量级。这些观察结果表明，丁酰苯类药物的大多数α肾上腺素能受体活性源于它们与α1肾上腺素能受体的相互作用。4. 丁酰苯类药物对α1肾上腺素能受体的相对高亲和力表明，它们可能作为研究这些组织和其他组织中α1肾上腺素能受体的有用探针。
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Synthesis of new haloperidol analogues and characterization of their interactions with alpha-adrenoceptors in rat parotid slices and human platelet membranes.新型氟哌啶醇类似物的合成及其与大鼠腮腺切片和人血小板膜中α-肾上腺素能受体相互作用的表征。
Br J Pharmacol. 1982 Jan;75(1):213-7. doi: 10.1111/j.1476-5381.1982.tb08775.x.
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