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  • Title: Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
    Author: Piergentili A, Amantini C, Del Bello F, Giannella M, Mattioli L, Palmery M, Perfumi M, Pigini M, Santoni G, Tucci P, Zotti M, Quaglia W.
    Journal: J Med Chem; 2010 Feb 11; 53(3):1261-9. PubMed ID: 20067271.
    Abstract:
    Conservative chemical modifications of the core structure of the lead spipethiane (1) afforded novel potent sigma(1) ligands. sigma(1) affinity and sigma(1/)sigma(2) selectivity proved to be favored by the introduction of polar functions (oxygen atom or carbonyl group) in position 3 or 4 (4-6) or by the elongation of the distance between the two hydrophobic portions of the molecule with the simultaneous presence of a carbonyl group in position 4 (8 and 9). The observed cytostatic effect against the human breast cancer cell line MCF-7/ADR, highly expressing sigma(1) receptors, and not against MCF-7, as well as the enhancement of morphine analgesia highlighted the sigma(1) antagonist profile of this series of compounds. In particular, due to its high sigma(1) affinity (pK(i) = 10.28) and sigma(1)/sigma(2) selectivity ratio (29510), compound 9 might be a novel valuable tool for sigma receptor characterization and a suitable template for the rational design of potential therapeutically useful sigma(1) antagonists.
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