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Physiology and pathophysiology of drug receptor mechanisms

药物受体机制的生理学和病理生理学

基本信息

批准号：
01304028
负责人：
KURIYAMA Kinya
金额：
$ 4.61万
依托单位：
Kyoto Prefectural University of Medicine
依托单位国家：
日本
项目类别：
Grant-in-Aid for Co-operative Research (A)
财政年份：
1989
资助国家：
日本
起止时间：
1989 至 1991
项目状态：
已结题

项目摘要

Physiological and pathophysiological roles of drug receptors in various organs were investigated in this research group and the following results and conclusions were obtained. 1) Continuous exposure of primary cultured neurons to muscarinic agonists and/or antagonists induced down- and/or up-regulation of the receptor and these changes were accompanied with those in second messenger systems coupled with the receptor. 2) The membrane stabilizing effect was essential for the protecting effect of various drugs on cardiac myopathy induced by cardiac ischemia. 3) The proliferation of vascular endotherial cells, which plays an important role in the progession of arteriosclerosis, was associated with the stimulation of alpha_1-adrenoceptor by cathecholamines. 4) The development of functional tolerance to morphine was prevented by the concomitant administrations of adrenergic blockers, k-opioid receptor agonist and calcium channel blockers. 5) Potassium channel opener selectively inhibited IP_3 -induced CA^<++> release in the heart. 6) Central dopamine D_1 receptor was operated when the excess of dopamine release was induced. 7) The function of adrenergic receptors in vascular smooth muscle showed a decrease with the progression of aging, while cholinergic receptors in this tissue were not affected significantly by aging. 8) The bata-receptors in the coronary artery were mostly beta_1 type. 9) The dilatation of cerebral arteries was mediated by the increase of cGMP caused by the activation of guanylate cyclase with NO. 10) Endothelin inhibited ganglionic transmission by ganglionic stimulation of thromboxane A_2 production as well as postganglionic activation of Ca^<++> dependent K^+channel. 11) The hypothalamus possessed both subsaince P and opioid receptors which are involved in the regulation of urinary outflow.

本课题组研究了药物受体在各器官中的生理和病理生理作用，并获得了以下结果和结论。1)原代培养的神经元连续暴露于毒蕈碱激动剂和/或拮抗剂诱导的受体的下调和/或上调，这些变化伴随着与受体偶联的第二信使系统。2)膜稳定作用是各种药物对心肌缺血所致心肌病变保护作用的基础。3)血管内皮细胞的增殖在动脉粥样硬化的发生发展中起重要作用，其增殖与胆碱能刺激α_1-肾上腺素能受体有关。4)同时给予肾上腺素能受体阻滞剂、K-阿片受体激动剂和钙通道阻滞剂可防止对吗啡的功能性耐受。5)钾通道开放剂选择性地抑制IP_3诱导的心肌CA^++释放。6)当多巴胺释放过量时，中枢多巴胺D_1受体起作用。7)血管平滑肌中肾上腺素能受体的功能随增龄而下降，而胆碱能受体的功能则不受增龄的影响。8)冠状动脉β受体以β_1型为主。9)NO激活鸟苷酸环化酶引起cGMP增加，从而引起脑动脉扩张。10）内皮素通过刺激神经节血栓素A_2的产生和节后Ca^++依赖性K^+通道的激活抑制神经节传递。11)下丘脑具有参与尿流出调节的P物质受体和阿片受体。