EMD386088 is a potent and selective 5-HT6 receptor agonist with nanomolar efficacy that displays minimal off-target activity across other serotonin receptor subtypes, except limited interaction with 5-HT3R, EMD386088 modulates ERK1/2 signaling pathways, supporting its utility in mechanistic research related to Alzheimer’s disease and schizophrenia.

In HEK293 cells, EMD386088 exhibits biphasic concentration-dependent regulation of ERK1/2 activity: it promotes ERK1/2 activation at lower concentrations (0–30 μM) but inhibits activation at higher levels (60 μM). Furthermore, EMD386088 induces dose- and time-dependent cell death within the range of 1–60 μM.

In vivo, EMD386088 modulates cognitive functions, frequently acting as a disruptor of memory processes at specific doses. In male Wistar rats, a dose of 5 mg/kg significantly impaired both Short-Term Memory (STM) and Long-Term Memory (LTM). Interestingly, a higher dose of 10 mg/kg produced no significant effects, demonstrating a non-linear dose-response. Similarly, in C57BL/6J mice, a 2 mg/kg dose significantly impaired spontaneous alternation—a metric for working memory and behavioral flexibility—while a 4 mg/kg dose showed no significant impairment.

DMSO: 80 mg/mL (324.23 mM), Sonication is recommended.