Delving into the Latest Updates on GSK-2210875 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [5]

Target

mGluR2 x mGluR5

Action

modulators, antagonists

Mechanism

mGluR2 modulators(Metabotropic glutamate receptor 2 modulators), mGluR5 antagonists(Metabotropic glutamate receptor 5 antagonists)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Anxiety Disorders

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

GSK Plc

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Author: Vincenzo Garzya ; Olivier Lorthioir ; Catherine Ball ; Palmina Cavallini ; Michela Tessari ; Sonia Delle-Fratte ; Paul Smith ; Ezio Bettini ; Pier D’Alessandro ; Adelheid Roth ; Ben Tehan ; Parita Shah ; Michela Andreoli ; Caroline Goodacre ; Maria Pilla ; Roberto Benedetti ; Stephen Watson ; Sharon Butler ; Doug Minick ; Fiona Brown

The identification of novel orally active mGluR5 antagonist GSK2210875 is described.

01 Jan 2010·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2

Q4 · MEDICINE

Article

Author: Perez, Paloma ; Watson, Stephen P. ; Branch, Clive ; D'Alessandro, Pier L. ; Ugolini, Annarosa ; Osborne, Greg ; De Los Frailes, Maite ; Smith, Paul W. ; Sava, Anna ; Koppe, Emma L. ; Powney, Ben ; Garland, Stephen L. ; Nash, David ; Bianchi, Federica ; Rocheville, Magalie ; Roth, Adelheid ; Montanari, Dino ; Corti, Corrado ; de la Fuente, Jesus

The optimisation of an HTS hit series (1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators GSK1331258 and GSK1331268 is described. Structure-activity relationships, attenuation of dopaminergic activity, and potentiation of mGluR2 responses in rat hippocampal MPP-DG synapses are also reported.

100 Deals associated with GSK-2210875

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