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(-)PPAP: A new and selective ligand for sigma binding sites

Authors
Journal
Pharmacology Biochemistry and Behavior
0091-3057
Publisher
Elsevier
Publication Date
Volume
37
Issue
3
Identifiers
DOI: 10.1016/0091-3057(90)90027-f
Keywords
  • Sigma Receptor
  • Radioligand Binding

Abstract

Abstract 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 (IC 50 = 24 nM) versus either PCP sites (IC 50 > 75,000 nM) or D1 and D2 dopamine receptors (IC 50 > 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.

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