Drug intelligence / Profile preview

DM506

Development stage
Preclinical
Modality
Small Molecules
Administration
Systemic
01

Overview

**DM506** is a novel small molecule and synthetic derivative of ibogamine, belonging to the class of "psychoplastogens"—agents designed to rapidly and sustainably enhance neuronal plasticity without hallucinogenic or cardiotoxic side effects. DM506 inhibits both α9α10 and α7 subtypes of the nicotinic acetylcholine receptor (nAChR) via novel allosteric, non-competitive mechanisms, likely involving modulation of the extracellular-transmembrane domain junction and the cytoplasmic domain, respectively. It also decreases tonic GABA currents in the prelimbic cortex, possibly by modulating extrasynaptic GABA levels or indirect GABAA receptor inhibition. Preclinical studies show DM506 reduces cue-induced heroin-seeking behavior, producing anxiolytic- and sedative-like effects without apparent hallucinogenic or adverse psychotropic effects. Primary indications studied preclinically are opioid use disorder and anxiety-like states[1][2][3][5][7][8].

Other names
3-methyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole fumarate
02

Targets

α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)α6α3β2β3 nAChR (α6α3β2β3 nicotinic receptor)α7β2 nAChR (α7β2 nicotinic receptor)HTR2A (Serotonin receptor 5-HT2A)α9α10 nAChR (α9α10 nicotinic receptor)HTR2B (5-Hydroxytryptamine Receptor 2B)CHRNA7 (α7 nicotinic receptor)

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