Redpoint Bio Corporation

Rok Cerne

Robert Bryant

Roy Kyle Palmer

M N Tulu Buber

S Paul Lee

Ivona Bakaj

Karnail S Atwal

F Raymond Salemme

Peihong Zhou

Anita B Atwal, Legal Representative

Gillian Morgan

The present invention is directed to methods of enhancing insulin release, GLP-1 release, and insulin sensitivity, methods of increasing insulin gene expression, methods of decreasing gastric secretion and emptying and glucagons secretion, and methods of inhibiting food intake, and methods of treating diabetes mellitus, insulin resistance syndrome, hyperglycemia, and obesity comprising administering to a subject an effective amount of a TRPM5 inhibitor.

Use of a TRPM5 inhibitor to regulate insulin and GLP-1 release

There exists a need in the art for high throughput screening assays that can identify compounds that specifically modulate the activity of fast-acting ion channels, such as TRPM5. Current methods, especially electrophysiological, suffer from a lack of sensitivity, rapid signal loss, low throughput, and are labor intensive. The claimed methods and compositions provide electrophysiology methods that allow prolonged sample testing and fluorescent assays with an optical readout that gives rapid readout of the results, has a high signal to noise background ratio, are easy to use, can be modified for automation and miniaturization, and provide verification that a compound specifically modulates TRPM5.

Non-desensitizing mutant of the transient receptor potential TRPM5 ion channel

The present invention is directed to the use of a compound of Formula I and physiologically acceptable salts thereof wherein G, G, G, R, R, R, R, R, and Rare defined herein. Compounds according to Formula I can be used to enhance a sweet taste produced by a tastant. The invention is also directed to compositions comprising a compound according to the above formula. Other aspects of the invention provide methods, compounds, and compositions for improved food products wherein the food product comprises a compound according to Formula I and a reduced amount of a sweet tastant.

Heterocyclic compounds as sweetener enhancers

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Lawrenceville, NJ, United States of America

Rok Cerne