Delving into the Latest Updates on LK00764 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

2-(5-(4′-Chloro-[1,1′-biphenyl]-4-yl)-4H-1,2,4-triazol-3-yl)ethan-1-amine

Target

TAAR1

Action

agonists

Mechanism

TAAR1 agonists(Trace amine-associated receptor 1 agonists)

Therapeutic Areas

Other Diseases

Active Indication

Schizophrenia

Inactive Indication-

Originator Organization

Accellena

Active Organization

Accellena

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

A focused in-house library of about 1000 compounds comprising various heterocyclic motifs in combination with structural fragments similar to β-phenylethylamine or tyramine was screened for the agonistic activity towards trace amine-associated receptor 1 (TAAR1). The screening yielded two closely related hits displaying EC50 values in the upper submicromolar range. Extensive analog synthesis and testing for TAAR1 agonism in a BRET-based cellular assay identified compound 62 (LK00764) with EC50 = 4.0 nM. The compound demonstrated notable efficacy in such schizophrenia-related in vivo tests as MK-801-induced hyperactivity and spontaneous activity in rats, locomotor hyperactivity of dopamine transporter knockout (DAT-KO) rats, and stress-induced hyperthermia (i.p. administration). Further preclinical studies are necessary to evaluate efficacy, safety and tolerability of this potent TAAR1 agonist for the potential development of this compound as a new pharmacotherapy option for schizophrenia and other psychiatric disorders.

100 Deals associated with LK00764

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