Delving into the Latest Updates on N8279 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

GHSR

Action

modulators

Mechanism

GHSR modulators(Ghrelin/growth hormone secretagogue receptor modulators)

Therapeutic Areas

Nervous System Diseases

Active Indication

Nervous System Diseases

Inactive Indication-

Originator Organization

Duke University

Active Organization

Duke University

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC24H25ClN2O6

InChIKeyPYURHFYFDIDSAT-UHFFFAOYSA-N

CAS Registry2920368-29-0

SignificanceThe modulation of growth hormone secretagogue receptor-1a (GHSR_1a) signaling is a promising strategy for treating brain conditions of metabolism, aging, and addiction. GHSR_1a activation results in pleiotropic physiological outcomes through distinct and pharmacologically separable G protein- and β-arrestin (βarr)-dependent signaling pathways. Thus, pathway-selective modulation can enable improved pharmacotherapeutics that can promote therapeutic efficacy while mitigating side effects. Here, we describe the discovery of a brain-penetrant small molecule, N8279 (NCATS-SM8864), that biases GHSR_1a conformations toward Gα_q activation and reduces aberrant dopaminergic behavior in mice. N8279 represents a promising chemical scaffold to advance the development of better treatments for GHSR_1a-related brain disorders involving the pathological dysregulation of dopamine.

100 Deals associated with N8279

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