Drug intelligence / Profile preview

6-(2-aminopropyl)benzofuran

Development stage
Preclinical
Lead developer
University of California, San Francisco
Modality
Small Molecules
Administration
Oral
01

Overview

6-(2-aminopropyl)benzofuran, commonly known as 6-APB, is a synthetic small molecule and benzofuran derivative that acts as a potent agonist of the serotonin 5-HT2B receptor. Originally developed as a psychoactive research chemical, it has been identified in preclinical studies at the University of California, San Francisco, as a potential therapeutic candidate for Dravet syndrome. In scn1lab mutant zebrafish models, which recapitulate the clinical features of Dravet syndrome, 6-APB has demonstrated significant antiepileptic activity by suppressing spontaneous electrographic seizures and convulsive swimming behaviors. Its mechanism of action is hypothesized to involve the activation of 5-HT2B receptors, which may modulate inhibitory signaling in the central nervous system, a pathway shared by other serotonergic drugs currently in clinical development for refractory childhood epilepsies.

Other names
6-APB6-benzofuran-2-ylpropan-2-amine6-benzofuran-6-ylpropan-2-amine
02

Targets

SERT (Sodium-dependent serotonin transporter)ADRA2C (α2C)TAAR1 (Trace amine-associated receptor 1)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)DAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)HTR2B (5-Hydroxytryptamine Receptor 2B)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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