(-)PPAP - A NEW AND SELECTIVE LIGAND FOR SIGMA-BINDING SITES

被引:15
作者
GLENNON, RA [1 ]
BATTAGLIA, G [1 ]
SMITH, JD [1 ]
机构
[1] LOYOLA UNIV,DEPT PHARMACOL,MAYWOOD,IL 60153
关键词
Radioligand binding; Sigma receptor;
D O I
10.1016/0091-3057(90)90027-F
中图分类号
B84 [心理学]; C [社会科学总论]; Q98 [人类学];
学科分类号
03 ; 0303 ; 030303 ; 04 ; 0402 ;
摘要
Most agents employed for the investigation of sigma (α) binding sites display relatively low affinity for these sites, bind both at α sites and at either phencyclidine (PCP) sites or dopamine receptors with similar affinity, and/or produce some dopaminergic activity in vivo. We describe a new agent, (-)PPAP or R(-)-N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane hydrochloride, that binds with high affinity and selectivity at α (IC50 = 24 nM) versus either PCP sites (IC50 > 75,000 nM) or D1 and D2 dopamine receptors (IC50 > 5,000 nM). The α affinity of this agent is comparable to that of the standard ligands (+)-3-PPP and DTG. Furthermore, although (-)PPAP is structurally related to amphetamine, it neither produces nor antagonizes amphetamine-like stimulus effect in rats trained to discriminate 1 mg/kg of S(+)amphetamine from saline. © 1990.
引用
收藏
页码:557 / 559
页数:3
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