Novel 2(3H)-Benzothiazolones as Highly Potent and Selective Sigma-1 Receptor Ligands

Autor:	M Belloir, Wallez, Saïd Yous, Jacques H. Poupaert, D. H. Caignard, Christopher R. McCurdy
Rok vydání:	2005
Předmět:	chemistry.chemical_compound Sigma-1 receptor Chemistry Stereochemistry Organic Chemistry Alpha (ethology) General Pharmacology Toxicology and Pharmaceutics Azepine Receptor Beta (finance) Selectivity Ligand (biochemistry) 5-HT receptor
Zdroj:	Medicinal Chemistry Research. 14:158-168
ISSN:	1554-8120 1054-2523
Popis:	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).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::37e20ce4444070324a2529fb18677b0c https://doi.org/10.1007/s00044-005-0131-1 Zobrazit plný text záznamu Full text from SpringerLink