Drug intelligence / Profile preview

OPC-14523

Development stage
Preclinical
Lead developer
Otsuka America Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

OPC-14523 is an investigational small molecule antidepressant developed by Otsuka America Pharmaceutical. It acts as a potent partial agonist at serotonin 5-hydroxytryptamine 1A (5-HT1A) receptors and also has high affinity for sigma receptors. Preclinical studies indicate that it increases serotonergic neurotransmission and exhibits 'antidepressant-like' effects in animal models of depression. Its mechanism involves modulation of both pre-synaptic and post-synaptic 5-HT1A receptors as a partial agonist, as well as activity at sigma non-opioid intracellular receptor 1. The compound has been studied primarily for the treatment of depression, especially refractory depression.

Other names
OPC-14523 hydrochlorideOPC14523 hydrochlorideOPC 14523 hydrochlorideOPC-14523 mesylateOPC14523 mesylateOPC 14523 mesylate1-{3-[4-(3-chlorophenyl)piperazin-1-yl]propyl}-5-methoxy-1,2,3,4-tetrahydroquinolin-2-one hydrochloride
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))SERT (Sodium-dependent serotonin transporter)

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