desformylflustrabromine

Desformylflustrabromine (dFBr) is an indole alkaloid originally isolated from the marine bryozoan *Flustra foliacea*. It acts as a **positive allosteric modulator** of neuronal nicotinic acetylcholine receptors with **subtype specificity for α4β2 and α2β2 receptors**, showing no effect on homomeric α7 receptors. The compound potentiates acetylcholine responses at nanomolar concentrations (pEC50 = 120 nM) and displays 14.7-fold selectivity for α4β2 over α7 receptors. It has demonstrated multiple therapeutic effects in preclinical studies including **analgesic and anti-allodynic effects** in neuropathic pain models, **anti-addictive properties** by reducing nicotine and ethanol consumption, **pro-cognitive actions**, and potential utility in **treating compulsive behaviors** seen in OCD. Notably, dFBr relieves the inhibition of α4β2 and α2β2 receptors by β-Amyloid (1-42) peptide, suggesting potential application in **Alzheimer's disease**. The compound crosses the blood-brain barrier and has been shown to be non-addictive in animal studies. Water-soluble hydrochloride salts have been synthesized for pharmaceutical applications.

Other names

Deformylflustrabromine