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    Electrophysiological assays using oocytes that express human enac and the use of phenamil to improve the effect of enac enhancers in assays using membrane potential reporting dyes
    3.
    发明申请
    Electrophysiological assays using oocytes that express human enac and the use of phenamil to improve the effect of enac enhancers in assays using membrane potential reporting dyes 审中-公开

    公开(公告)号：US20170175160A1

    公开(公告)日：2017-06-22

    申请号：US15257517

    申请日：2016-09-06

    Applicant: SENOMYX, INC.

    Inventor： Guy SERVANT ,  Hong CHANG ,  Cyril REDCROW ,  Sumita RAY ,  Imran CLARK ,  Bryan MOYER

    IPC: C12Q1/02 ,  C12N15/85

    CPC classification number: G01N33/6872 ,  C12N15/85 ,  C12N2320/10 ,  C12N2503/02 ,  C12Q1/025 ,  G01N33/5044 ,  G01N2500/10

    Abstract: In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should therebymodulate salty taste in humans.

    SCREENING ASSAYS TO IDENTIFY COMPOUNDS WHICH MODULATE T1R ASSOCIATED TASTE MODALITIES WHICH ELIMINATE FALSE POSITIVES
    6.
    发明申请
    SCREENING ASSAYS TO IDENTIFY COMPOUNDS WHICH MODULATE T1R ASSOCIATED TASTE MODALITIES WHICH ELIMINATE FALSE POSITIVES 审中-公开

    公开(公告)号：US20180106801A1

    公开(公告)日：2018-04-19

    申请号：US15724407

    申请日：2017-10-04

    Applicant: Senomyx, Inc.

    Inventor： Guy SERVANT ,  Nicole Servant

    IPC: G01N33/566

    CPC classification number: G01N33/566 ,  G01N2500/04 ,  G01N2500/10 ,  G01N2500/20

    Abstract: This invention relates to assays which screen for compounds that modulate taste elicited by the T1R2/T1R3 sweet taste receptor which include a novel counter screen to eliminate false positives. In addition, the invention contemplates assays which screen for compounds that modulate taste elicited by the T1R1/T1R3 umami taste receptor which include a novel counter screen to eliminate false positives. Preferably the assays are conducted in high throughput format thereby enabling the screening of many hundreds of different compounds whereby the counter screen significantly improves assay efficiency. Further, the invention relates to the use of the compounds identified in the subject screening assays to modulate T1R associated taste perception.

    BITTER TASTE MODIFIERS INCLUDING SUBSTITUTED 1-BENZYL-3-(1-(ISOXAZOL-4-YLMETHYL)-1H-PYRAZOL-4-YL)IMIDAZOLIDINE-2,4-DIONES AND COMPOSITIONS THEREOF
    8.
    发明申请
    BITTER TASTE MODIFIERS INCLUDING SUBSTITUTED 1-BENZYL-3-(1-(ISOXAZOL-4-YLMETHYL)-1H-PYRAZOL-4-YL)IMIDAZOLIDINE-2,4-DIONES AND COMPOSITIONS THEREOF 审中-公开
    包括取代的1-苄氧基-3-（1-（异辛基-4-甲基苯基）-1H-吡唑-4-基）咪唑烷-2,4-二酮及其组合物的双酚类改性剂

    公开(公告)号：US20160376263A1

    公开(公告)日：2016-12-29

    申请号：US15219573

    申请日：2016-07-26

    Applicant: SENOMYX, INC.

    Inventor： Andrew PATRON ,  Catherine TACHDJIAN ,  Guy SERVANT ,  Tanya DITSCHUN

    IPC: C07D413/14 ,  A23L27/00 ,  A23L27/20 ,  A61K47/22

    CPC classification number: C07D413/14 ,  A23L27/204 ,  A23L27/2054 ,  A23L27/2056 ,  A23L27/86 ,  A61K47/22

    Abstract: The present invention includes compounds and compositions known to modify the perception of bitter taste, and combinations of said compositions and compounds with additional compositions, compounds, and products. Exemplary compositions comprise one or more of the following: cooling agents; inactive drug ingredients; active pharmaceutical ingredients; food additives or foodstuffs; flavorants, or flavor enhancers; food or beverage products; bitter compounds; sweeteners; bitterants; sour flavorants; salty flavorants; umami flavorants; plant or animal products; compounds known to be used in pet care products; compounds known to be used in personal care products; compounds known to be used in home products; pharmaceutical preparations; topical preparations; cannabis-derived or cannabis-related products; compounds known to be used in oral care products; beverages; scents, perfumes, or odorants; compounds known to be used in consumer products; silicone compounds; abrasives; surfactants; warming agents; smoking articles; fats, oils, or emulsions; and/or probiotic bacteria or supplements.

    Abstract translation: 本发明包括已知可以改变苦味感觉的化合物和组合物，以及所述组合物和化合物与另外的组合物，化合物和产品的组合。 示例性组合物包含以下一种或多种：冷却剂; 非活性药物成分; 活性药物成分; 食品添加剂或食品; 调味剂或风味增强剂; 食品或饮料产品; 苦味化合物; 甜味剂 苦涩 酸味香料; 咸味香料; 鲜味香料; 植物或动物产品; 已知用于宠物护理产品的化合物; 已知用于个人护理产品的化合物; 已知用于家庭用品的化合物; 药物制剂; 局部制剂; 大麻衍生或大麻相关产品; 已知用于口腔护理产品的化合物; 饮料; 香水，香水或气味剂; 已知用于消费品的化合物; 有机硅化合物; 研磨剂 表面活性剂 升温剂; 吸烟用品; 脂肪，油或乳液; 和/或益生菌或补品。

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