IN VITRO SCREENING ASSAY FOR THERMONEUTRAL TRPV1 MODULATORS

摘要

The invention relates to an in vitro screening assay based on electrophysiological recording techniques for identifying thermoneutral TRPV1 modulators comprising a) providing a cell expressing TRPV1, optionally in contact with a suitable concentration of a TRPV1 agonist under suitable conditions, b) providing said cell in contact with a suitable concentration of a TRPV1 modulator and optionally in contact with a TRPV1 agonist, if present in step a), under suitable conditions, c) applying a voltage above +100 mV to the cells of a) and of b), d) measuring the respective current of the cells' membranes of a) and b), and e) determining the change of the value of b) compared to the value of a), whereby in the presence of a TRPV1 agonist a residual current of 5 to 50% of b) relative to a) is indicative of a TRPV1 modulator being thermoneutral, and whereby in the absence of a TRPV1 agonist the indication of a TRPV1 modulator being thermoneutral is based on the measurement of the deviation of the current of a) relative to b), whereby a deviation in the range of 50% is indicative of a TRPV1 modulator being thermoneutral, as well as to the use of said screening assay for characterizing the thermogenetic properties of a TRPV1 modulator.