Delving into the Latest Updates on GI-264879A with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

NPY1R

Mechanism

NPY1R antagonists(neuropeptide Y receptor Y1 antagonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication-

Inactive Indication

Obesity

Originator Organization

GlaxoSmithKline, Inc.

Active Organization-

Inactive Organization

GlaxoSmithKline, Inc.

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Neuropeptide Y has been proposed to play a major role in the hypothalamic regulation of feeding behavior through the activation of specific, central NPY receptor(s). In an effort to design small molecule antagonists of NPY receptors, we have synthesized a series of substituted dipeptides based on defined pharmacophores, previously identified by us and others as essential for the interaction with the peptide receptors. GI264879A behaves as a functional antagonist of Y1 receptors while displaying no binding selectivity for the different NPY receptor subtypes. We demonstrate here that administration of GI264879A to rats causes a significant decrease in food intake and body weight partly through a mechanism dependent on the integrity of the vagus nerve.

100 Deals associated with GI-264879A

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