Delving into the Latest Updates on GR-138676 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

NK1R x NK3

Mechanism

NK1R antagonists(Neurokinin 1 receptor antagonists), NK3 antagonists(Neurokinin 3 receptor antagonists)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Glaxo Group Ltd.

Active Organization-

Inactive Organization

Glaxo Group Ltd.

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Gene Sequence

Sequence Code 552459465

GR138676, a conformationally constrained analogue of neurokinin B, is a novel, potent NK3 receptor antagonist. GR138676 was a competitive antagonist of neurokinin B-dependent arachidonic acid mobilization from prelabelled Chinese hamster ovary cells stably transfected with a human NK3 receptor gene (pKB 8.3) and of contractions induced by senktide in rat portal vein (pKB 8.2). However, GR138676 was also a competitive antagonist of the increase in intracellular calcium evoked by the selective NK1 agonist, GR73632, in the human astrocytoma U373MG cell-line (pKB 8.3). GR138676 had little activity at NK2 receptors, inhibiting binding of the NK2 antagonist radioligand [3H]-GR100679 to Chinese hamster ovary cells transfected with the human ileum NK2 receptor with a pKi of 6.0. In summary, despite its activity at NK1 receptors, GR138676 will be a useful tool for characterizing NK3 receptors as well as defining the physiological and pathophysiological function of this receptor subtype.

100 Deals associated with GR-138676

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