Patent ID: 11921105
Assignee: nan
Field: Measurement (Instruments)
Classification: CPC C  G | IPC G

Claim 9:
10. A method for identifying at least one positive allosteric modulating compound that enhances the activity of an olfactory receptor in the presence of an agonist of the receptor, comprising
a) providing one or more isolated cells, each cell expressing one mammalian olfactory receptor,
b) exposing the one or more cells to a first compound that activates the olfactory receptor,
c) exposing the one or more cells to one or more test compound, and
d) selecting at least one second compound from the one or more test compounds when the at least one second compound in combination with the first compound has a synergistic effect on the receptor activity as a positive allosteric modulating compound;
wherein the olfactory receptor comprises a polypeptide that
comprises an amino acid sequence having at least 95% sequence identity to SEQ ID NO: 2, 4, 6, or 8; or
is encoded by a nucleic acid molecule comprising a nucleotide sequence having at least 95% sequence identity to SEQ ID NO: 1, 3, 5, or 7, or the reverse complement thereof,
wherein the first compound is an agonist odorant compound of the olfactory receptor,
wherein the first compound is a musk or a floral muguet compound,
wherein the second compound has the structure:, in the form of any one of its stereoisomers or a mixture thereof,
wherein R represents a C3-11 linear alkyl group optionally substituted by a C1-4 alkyl carboxylester group or a hydroxyl group, a C4-11 branched alkyl group optionally substituted by a C1-3 alkoxy group, a C6-12 linear or branched alkenyl or alkadienyl group, a phenyl group substituted by one or two C1-3 alkyl groups, a C5-8 alicyclic alkenyl group or a benzyloxymethyl group, or
wherein the second compound is at least one positive allosteric modulator selected from the group consisting of (E)-dec-2-enal, 2-phenylpropanal; (E)-but-2-enal; 3-methylbenzaldehyde; 3-(1,3-benzodioxol-5-yl)-2-methylpropanal; (+−)-3-(4-methyl-3-penten-1-yl)-3-cyclohexene-1-carbaldehyde, (+−)-4-(4-methyl-3-penten-1-yl)-3-cyclohexene-1-carbaldehyde, and mixtures thereof; heptanal, 4-Propan-2-ylbenzaldehyde; (3R)-3,7-dimethyloct-6-enal; (+)-(3S)-3-[(1R)-4-methyl-3-cyclohexen-1-yl]butanal, (+)-(3R)-3-[(1R)-4-methyl-3-cyclohexen-1-yl]butanal, and mixtures thereof; hexanal; 2,6-dimethylhept-5-enal; benzaldehyde; 2-methyl-3-(4-methylphenyl)propanal; 3,5,6-trimethyl-3-cyclohexene-1-carbaldehyde, 2,4,6-trimethyl-3-cyclohexene-1-carbaldehyde, and mixtures thereof, 4-ethylbenzaldehyde; 6-methoxy-2,6-dimethylheptanal; (E)-non-2-enal; and combinations thereof,
wherein the first compound and the second compound are different compounds, and
wherein the second compound is not an agonist of the receptor.