Delving into the Latest Updates on GSK1331268 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

mGluR2

Action

modulators

Mechanism

mGluR2 modulators(Metabotropic glutamate receptor 2 modulators)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization

GSK Plc

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

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

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 GSK1331268

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