论文部分内容阅读
许多精神药物和心血管药物都是通过影响突触机制显示疗效。但由于药物作用的分子机制仍未阐明,至今这些领域中的新药筛选方案尚未能与神经递质的基础研究紧密相联,因而,在许多方面,还不能通过体外生化活性的检测来建立鉴定新药的系统方法。药物可通过多种途径影响神经递质系统,如可干扰递质的合成或降解的酶,改变递质的贮存或释放、或在受体位点上拟似或阻滞递质的作用。许多精神药物和心血管药物作用于受体。因此采用分子策略来发现新药需要简便的生化检测方法以识别受体位点。如在电器官中烟碱(N)-胆碱受体的成功鉴定是由于发现了极强的毒素,如[~(125)I]-α-银环蛇毒素和密度高达膜蛋白20%的N-胆碱受体。仅占脑或心脏重量百万分之一的阿片受体已能成功地用简
Many psychotropic and cardiovascular drugs show efficacy by affecting synaptic mechanisms. However, as the molecular mechanism of drug action has not been elucidated yet, new drug screening programs in these fields so far have not been closely linked to the basic research of neurotransmitters and, in many ways, the identification of in vitro biochemical activity can not be established Systematic approach to new drugs. Drugs can affect neurotransmitter systems in a number of ways, such as enzymes that interfere with the synthesis or degradation of the transmitter, alter the storage or release of the transmitter, or mimic or block the transmitter at the receptor site. Many psychotropic and cardiovascular drugs act on receptors. Therefore, the use of molecular strategies to find new drugs need a simple biochemical detection method to identify receptor sites. Successful identification of nicotinic (N) -cholinergic receptors in electrical organs is due to the discovery of extremely strong toxins such as [~ (125) I] -alpha-bungarotoxin and up to 20% N-choline receptors. Opioid receptors, which account for only one part of the brain or heart, have been successfully used