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538407 
Journal Article 
Novel 2(3H)-benzothiazolones as highly potent and selective sigma-1 receptor ligands 
Yous, S; Wallez, V; Belloir, M; Caignard, DH; McCurdy, CR; Poupaert, JH 
2005 
14 
3 
158-168 
English 
In an effort to produce a new pharmacological probe with high affinity and selectivity for the sigma-1 receptor, we have synthesized a series of original 2(3H)-benzothiazolones utilizing compound 4 [3-(1-piperidinoethyl)-6-propylbenzothiazolin-2-one] as a lead. Receptor binding affinities were determined at sigma-1 and sigma-2 receptors. The best ligand (9, sigma-1 K-i = 0.56 nM, selectivity ratio > 1000) was obtained with an azepine side-chain. When tested on a wide battery of receptors, including 5HT(2A)(h), 5HT(3)(h), alpha(1), alpha(2), beta(1), beta(2), H-1, H-2, opioids, D-1(h), D-2(h), 5HT uptake, and DOPA uptake, compound 9 showed submicromolar affinity only for alpha(2) (Ki = 205 nM) and H-1 (K-i = 311 nM). 
sigma-receptor ligands; antisense strategy; binding-sites; brain; involvement; cocaine; derivatives; modulation; expression; mechanism