[3H] -可乐定与豚鼠肾膜中α-肾上腺素能受体结合的特性。
The characteristics of [3H]-clonidine binding to an alpha-adrenoceptor in membranes from guinea-pig kidney.
作者信息
Jarrott B, Louis W J, Summers R J
出版信息
Br J Pharmacol. 1979 Apr;65(4):663-70. doi: 10.1111/j.1476-5381.1979.tb07879.x.
Abstract
- [3H]-clonidine binds to membranes prepared from guinea-pig kidney. 2. At 25 degrees C the binding is rapid and saturable. 3. Scatchard analysis of the binding data showed that the Kd for [3H]-clonidine binding in kidney membranes is 8.54 nM and the density of binding sites 12.5 pmol/g wet wt. tissue. 4. Hill plots of the binding data showed that there were no cooperative site interactions associated with binding. 5. [3H]-clonidine binding could be displaced by drugs, the most potent being drugs with a high affinity for the alpha-adrenoceptor. The neuroleptic drugs (+)-butaclamol, cis-clopenthixol and cis-flupenthixol at high concentration also displaced [3H]-clonidine binding. 6. Drugs acting as agonists or antagonists of beta-adrenoceptors, histamine receptors, acetylcholine receptors as well as prostaglandins E1, E2, F1alpha and F2alpha, angiotensin II, arginine vasopressin, naloxone, nalorphine and pargyline had little effect on binding. 7. It is likely that the binding site labelled by [3H]-clonidine in guinea-pig kidney membranes is an alpha-adrenoceptor similar in some pharmacological aspects to an alpha2-adrenoceptor.
摘要
- [3H]-可乐定与豚鼠肾制备的膜结合。2. 在25摄氏度时，结合迅速且具有饱和性。3. 对结合数据进行Scatchard分析表明，肾膜中[3H]-可乐定结合的解离常数（Kd）为8.54纳摩尔，结合位点密度为12.5皮摩尔/克湿重组织。4. 结合数据的希尔图显示，结合过程不存在协同位点相互作用。5. [3H]-可乐定结合可被药物取代，最有效的是对α-肾上腺素能受体具有高亲和力的药物。高浓度的抗精神病药物(+)-丁酰苯、顺式氯普噻吨和顺式氟奋乃静也能取代[3H]-可乐定的结合。6. 作为β-肾上腺素能受体、组胺受体、乙酰胆碱受体激动剂或拮抗剂的药物，以及前列腺素E1、E2、F1α和F2α、血管紧张素II、精氨酸加压素、纳洛酮、纳洛芬和帕吉林对结合几乎没有影响。7. 豚鼠肾膜中被[3H]-可乐定标记的结合位点很可能是一种α-肾上腺素能受体，在某些药理学方面与α2-肾上腺素能受体相似。
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