Rothman R B, Bykov V, Xue B G, Xu H, De Costa B R, Jacobson A E, Rice K C, Kleinman J E, Brady L S
Clinical Psychopharmacology Section, NIDA Addiction Research Center, Baltimore, MD 21224.
Peptides. 1992 Sep-Oct;13(5):977-87. doi: 10.1016/0196-9781(92)90059-c.
Previous experiments resolved four kappa binding sites in guinea pig brain termed kappa 1a, kappa 1b, and kappa 2b. The present study was undertaken to examine the occurrence of kappa receptor subtypes in rat and human brain. [3H]U69,593 and [3H]bremazocine were used to label kappa 1 and kappa 2 binding sites, respectively, present in brain membranes depleted of mu and delta binding sites by pretreatment with the irreversible ligands, BIT and FIT. Low levels of [3H]U69,593 binding precluded a detailed quantitative study of kappa 1 binding sites in these species. Quantitative examination of [3H]bremazocine binding resolved two kappa 2 binding sites in both rat and human brain whose ligand selectivity patterns differed from that of the guinea pig. These observations suggest that there may be considerable variation in the ligand recognition site of kappa receptor subtypes among mammalian species.
先前的实验在豚鼠脑中确定了四个κ结合位点，分别称为κ1a、κ1b和κ2b。本研究旨在检测大鼠和人脑中κ受体亚型的存在情况。[3H]U69,593和[3H]布马佐辛分别用于标记κ1和κ2结合位点，这些位点存在于通过用不可逆配体BIT和FIT预处理而耗尽μ和δ结合位点的脑膜中。低水平的[3H]U69,593结合使得无法对这些物种中的κ1结合位点进行详细的定量研究。对[3H]布马佐辛结合的定量检测在大鼠和人脑中均确定了两个κ2结合位点，其配体选择性模式与豚鼠不同。这些观察结果表明，哺乳动物物种间κ受体亚型的配体识别位点可能存在相当大的差异。
