DEFORMYLFLUSTRABROMINE HYDROCHLORIDE

α ₄ β ₂ nAChR

Desformylflustrabromine hydrochloride is a selective agonist of α ₄ β ₂ neuronal nicotinic acetylcholine receptor (nAChR) with a pEC ₅₀ of 6.48. ACh-induced currents are potentiated and inhibited by Desformylflustrabromine hydrochloride in the high sensitivity (HS) and low sensitivity (LS) isoform preparations, although Desformylflustrabromine hydrochloride displays a higher potency on the LS isoform (pEC ₅₀ =6.4±0.2) compare with the HS isoform (pEC ₅₀ =5.6±0.2). Desformylflustrabromine hydrochloride potentiates ACh-induced responses of wild-type receptors expressed using the HS isoform preparation maximally by 350±20%, which is similar to receptors expressed via the LS isoform preparation (350±30%).