Patent ID: 8158442

Claim:
A method for identifying an antagonist of a bitter taste receptor activity, wherein the bitter taste receptor comprises: (a) a polypeptide comprising the amino acid sequence according to SEQ ID NO: 2; (b) a polypeptide derivative comprising not more than fifteen (15) amino acid residues that are conservatively substituted compared to a polypeptide comprising the amino acid sequence according to SEQ ID NO:2; or (c) a polypeptide comprising an amino acid sequence that is at least 90% identical to the amino acid sequence according to SEQ ID NO:2; wherein said method comprises: (1) contacting the bitter taste receptor or a host cell expressing the bitter taste receptor with a potential antagonist and/or a pharmaceutically acceptable salt thereof having a structure according to formula (I) and/or is a tautomer thereof, wherein; R 1 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkoxyalkyl, heterocycloalkyl, an alicyclic system, aryl, and heteroaryl, optionally substituted; R 2 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkoxyalkyl, heterocycloalkyl, an alicyclic system, aryl, and heteroaryl, optionally substituted; or R 1 and R 2 together form a heterocycloalkyl, an alicyclic system, or heteroaryl; (2) determining whether the potential antagonist inhibits the bitter taste receptor activity; (3) identifying a potential antagonist that reduces the activity of the bitter taste receptor when stimulated by an agonist of the bitter taste receptor, wherein prior, concomitantly and/or after (1), said bitter taste receptor and/or said host cell is contacted with an agonist of the bitter taste receptor.