期刊名称:Proceedings of the National Academy of Sciences
印刷版ISSN:0027-8424
电子版ISSN:1091-6490
出版年度:1974
卷号:71
期号:5
页码:1725-1729
DOI:10.1073/pnas.71.5.1725
语种:English
出版社:The National Academy of Sciences of the United States of America
摘要:Binding sites with high affinity and specificity for [3H]quinuclidinyl benzilate (QNB) are present in homogenates of rat brain. The characteristics of the binding sites resemble those of muscarinic cholinergic receptors. Specific binding is saturable with respect to [3H]QNB and tissue concentration and is time-, temperature-, and pH-dependent. The bimolecular rate of association (2.0 x 108 M-1 min-1) and dissociation (1.2 x 10-2 min-1) at 35{degrees} indicate a dissociation constant of 60 pM and a density of 65 pmol/g of brain. Muscarinic antagonists and agonists displace specific [3H]QNB binding, while nicotinic and non-cholinergic drugs possess little affinity for [3H]QNB-binding sites.