Short communication
Interactions of erythro-ifenprodil, threo-ifenprodil, erythro-iodoifenprodil, and eliprodil with subtypes of σ receptors

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Abstract

Observations of sigma (σ) receptor heterogeneity have prompted interest in identifying ligands for σ receptor subtypes. Selective ligands for the σ-2 are unavailable, but [3H]ifenprodil labels σ-2 sites. Therefore, isomers and analogues of ifenprodil were compared as potential σ-2 ligands. Threo-ifenprodil and erythro-ifenprodil had high affinity (Ki ⋍ 2 nM) for σ-2 sites; erythro-iodoifenprodil had moderate affinity (Ki ⋍ 46 nM). Threo-ifenprodil, which has less affinity for α1-adrenoceptors than erythro-ifenprodil, was slightly more selective than erythro-ifenprodil for σ-2 sites. These results identify threo-ifenprodil as potentially useful for studies of σ-2 receptors.

Keywords

σ Receptor
Ifenprodil
Eliprodil
Subtype
Receptor binding
Brain, rat

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1

Present address: National Institute of Mental Health, National Center of Neurology and Psychiatry, Japan.