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不久前用选择性毒蕈碱受体拮抗剂pi-renzepine证实了Birdsall等为解释胆硷能激动剂与脑受体结合异常而首先提出的毒蕈碱受体亚型的假说。在接受毒蕈碱受体不均一性这一概念许多年之前就开始了选择性拮抗剂的寻找。科学家认识到毒蕈碱受体可引起很多种生物功能,便寻找能分别影响这些功能的药物。因为外周毒蕈碱受体能控制胃分泌和平滑肌收缩,所以主要目标是寻找选择性抑制分泌的抗溃疡药物和选择性平滑肌解痉药。近30年来已合成了数以千计的化合物,但最近才发现了选择性毒蕈碱拮抗剂pirenzepine,并用于人体治疗。
The hypothesis that Birdsall et al. First proposed the muscarinic receptor subtypes to explain the abnormal binding of cholinergic agonists to brain receptors was recently confirmed by the selective muscarinic receptor antagonist pi-renzepine. The search for selective antagonists began many years ago when it came to accepting the concept of muscarinic receptor heterogeneity. Recognizing that muscarinic receptors cause many biological functions, scientists are looking for drugs that affect these functions separately. Since peripheral muscarinic receptors control gastric secretion and smooth muscle contraction, the main goal is to find anti-ulcer drugs that selectively inhibit secretion and selective antispasmodics. Thousands of compounds have been synthesized in the last 30 years, but the selective muscarinic antagonist pirenzepine was recently discovered and used in human therapy.