摘要
采用放射性配体－受体结合实验，研究了３－（２－羟基－２－环戊基－２－苯基－乙氧基）奎宁环烷（ＰＣＨＥＱ）及其４个光学异构体对豚鼠心脏，小肠纵肌，颌下腺和猪虹膜中的Ｍ受体的作用．结果表明，４种组织中的Ｍ受体对ＰＣＨＥＱ及其异构体表现出相似的立体选择性．ＰＣＨＥＱ及其异构体对４种组织中Ｍ受体的亲和力顺序相同，即ＲＲ′＞ＰＣＨＥＱ＞ＳＲ′＞ＲＳ′＞ＳＳ′．这些化合物对颌下腺中的Ｍ受体的选择性较高，尤以ＳＲ′异构体为显著．
The binding profiles of 3 (2 hydroxy 2 cyclopentyl 2 phenyl ethoxy)quinuclidine (PCHEQ) and its 4 optical isomers to muscarinic acetylcholine receptors (mAChR) on the heart, intestinal muscle and submandibular gland of guinea pig and porcine iris were studied. It was demonstrated that mAChR of the 4 tested tissues had similar stereoselectivity to these compounds. The order of affinity of PCHEQ and its isomers to mAChR in the tested tissues was the same, i.e., RR′>PCHEQ>SR′>RS′>SS′. Among four tested tissues, PCHEQ and its isomers had a relative higher selectivity to mAChR in submandibular glands.
出处
《中国药理学与毒理学杂志》
CAS
CSCD
北大核心
1999年第1期5-8,共4页
Chinese Journal of Pharmacology and Toxicology
关键词
奎宁环烷
光学异构体
毒蕈碱性
受体
receptor
muscarinic
parasympatholytics
stereoisomers
submandibular gland
radioligand assay
