Hashimoto K, London E D
Neuroimaging and Drug Action Section, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA.
Eur J Pharmacol. 1995 Feb 6;273(3):307-10. doi: 10.1016/0014-2999(94)00763-w.
Observations of sigma (sigma) receptor heterogeneity have prompted interest in identifying ligands for sigma receptor subtypes. Selective ligands for the sigma-2 are unavailable, but [3H]ifenprodil labels sigma-2 sites. Therefore, isomers and analogues of ifenprodil were compared as potential sigma-2 ligands. Threo-ifenprodil and erythro-ifenprodil had high affinity (Ki congruent to 2 nM) for sigma-2 sites; erythro-iodoifenprodil had moderate affinity (Ki congruent to 46 nM); eliprodil had lowest affinity (Ki congruent to 630 nM). Threo-ifenprodil, which has less affinity for alpha 1-adrenoceptors than erythro-ifenprodil, was slightly more selective than erythro-ifenprodil for sigma-2 sites. These results identify threo-ifenprodil as potentially useful for studies of sigma-2 receptors.
对σ（西格玛）受体异质性的观察引发了人们对识别σ受体亚型配体的兴趣。目前尚无针对σ-2的选择性配体，但[3H]ifenprodil可标记σ-2位点。因此，比较了ifenprodil的异构体和类似物作为潜在的σ-2配体。苏式ifenprodil和赤式ifenprodil对σ-2位点具有高亲和力（Ki约为2 nM）；赤式碘ifenprodil具有中等亲和力（Ki约为46 nM）；eliprodil的亲和力最低（Ki约为630 nM）。苏式ifenprodil对α1肾上腺素能受体的亲和力低于赤式ifenprodil，对σ-2位点的选择性略高于赤式ifenprodil。这些结果表明苏式ifenprodil可能对σ-2受体的研究有用。
