Drug intelligence / Profile preview

RS-67333

Development stage
Preclinical
Lead developer
Roche
Modality
Small Molecules
Administration
Intracerebral (animal Research), Not Clinically Approved For Human Administration
01

Overview

RS-67333 is a **selective partial agonist of the serotonin 5-HT4 receptor** with additional activity as a **submicromolar inhibitor of acetylcholinesterase**. It has been studied primarily for its **procognitive and neuroprotective effects**, particularly in the context of Alzheimer’s disease. RS-67333 stimulates the nonamyloidogenic processing of amyloid precursor protein, leading to increased sAPPα (neurotrophic protein) secretion and reduction of amyloid-β accumulation, suggesting both symptomatic and potential disease-modifying effects. It also moderately inhibits acetylcholinesterase, potentially enhancing cholinergic neurotransmission. RS-67333 shows selectivity for 5-HT4 receptors, with lower affinity for other serotonin receptor subtypes and other neurotransmitter receptors. It has been used experimentally for memory enhancement in animal models and to study mechanisms of antidepressant response, but is not an approved pharmaceutical.

Other names
RS67333RS-67333RS 67333
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)HTR4 (5-Hydroxytryptamine receptor 4)TMEM97 (Sigma-2 receptor complex (TMEM97/PGRMC1))

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