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Attenuation of Cocaine‐Induced Behaviors by the Sigma Receptor Ligand YZ‐185
Author(s) -
Sage Andrew S.,
Fan KuoHsien,
Lever John R.,
Lever Susan Z.,
Miller Dennis K.
Publication year - 2013
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.27.1_supplement.1098.3
Subject(s) - conditioned place preference , sigma receptor , ligand (biochemistry) , piperazine , chemistry , sigma 1 receptor , receptor , sigma , pharmacology , locomotor activity , stereochemistry , biology , biochemistry , physics , quantum mechanics , agonist
YZ‐185 ( N ‐phenylpropyl‐ N ′‐(3‐methoxyphenethyl)piperazine) is a sigma receptor ligand that binds with greater affinity to the σ1 than to the σ2 sigma receptor subtype (Ki values ≈ 1.4 and 10.2 nM, respectively) in brain. In a dose‐dependent manner and at doses that did not alter basal locomotor activity, YZ‐185 pretreatment attenuated cocaine‐induced hyperactivity in mice. YZ‐185 did not produce conditioned place preference or aversion in mice; however, it attenuated both the induction and expression of conditioned place preference to cocaine. These results indicate a role for sigma receptors in cocaine's locomotor‐activating and conditioned‐rewarding properties and support the use of N ‐phenylpropyl‐ N ′‐substituted piperazine ligands to investigate cocaine's effects.