Lupanine

Lupanine (D-Lupanine) is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine shows binding affinity for nicotinic receptor (nAChR) with a K_i value of 500 nM^[1]. IC50 & Target:Ki: 500 nM (Nicotinic receptor) and 11000 nM (Muscarinic receptor)^[1] In Vitro:Lupanine shows binding affinity for nicotinic receptor with a K_i value of 500 nM. While, Lupanine shows a very weak affinity for the muscarinic receptor with a K_i value of 11000 nM^[1].
Lupanine (0-100 μM) is a weak agonist and desensitizer in SH-SY5Y cells, with EC₅₀ and DC₅₀ of 10.7 μM and 28.2 μM, respectively^[2].
In Vivo:Lupanine (100-300 mg/kg for i.p.; 175-700 mg/kg for p.o.) is much less toxic in one single injection in EOPS male Swiss mice (20-22 g) and Hartley guinea-pigs (400-500 g)^[1].
Lupanine (1-7.5 mg/kg; i.v.) is more efficient than Sparteine for antagonizing secondary reflex hypertension in carotid occlusion and hypotension resulting from the stimulation of the pneumogastric nerve in both the cat and the dog^[1].
Lupanine has an inhibitory action on nicotinic type hypertension produced by injection of Acetylcholine (500 p.g/kg i.v.) in the Atropine-treated dog^[1].