Transient receptor potential melastatin type-8 (TRPM8) is a transmembrane, non selective Ca2+ permeable cation channel (1), considered as the major sensor for peripheral innocuous cool and its modulation is also responsible for several pathological processes: one of the most investigated effects produced by TRPM8 modulation is the analgesia against chronic and neuropathic pain (2). Notably, both TRPM8 agonists and antagonists exert analgesic effects: in particular, while TRPM8 agonists produce profound analgesia at very low concentrations (2), even greater effects have been reported for TRPM8 antagonists (3). TRPM8 agonists have also been proposed as useful diagnostic and therapeutic tools for the treatment of prostate cancer and benign prostate hyperplasia (4), while TRPM8 antagonists have been investigated for the treatment of overactive and painful bladder syndromes (5). Thus, increasing efforts in the last few years have been dedicated to the design and functional characterization of selective and potent TRPM8 ligands.

N-substituted tryptamines as TRPM8 channel modulators

OSTACOLO, CARMINE;Bertamino, Alessia;
2015-01-01

Abstract

Transient receptor potential melastatin type-8 (TRPM8) is a transmembrane, non selective Ca2+ permeable cation channel (1), considered as the major sensor for peripheral innocuous cool and its modulation is also responsible for several pathological processes: one of the most investigated effects produced by TRPM8 modulation is the analgesia against chronic and neuropathic pain (2). Notably, both TRPM8 agonists and antagonists exert analgesic effects: in particular, while TRPM8 agonists produce profound analgesia at very low concentrations (2), even greater effects have been reported for TRPM8 antagonists (3). TRPM8 agonists have also been proposed as useful diagnostic and therapeutic tools for the treatment of prostate cancer and benign prostate hyperplasia (4), while TRPM8 antagonists have been investigated for the treatment of overactive and painful bladder syndromes (5). Thus, increasing efforts in the last few years have been dedicated to the design and functional characterization of selective and potent TRPM8 ligands.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11386/4812111
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