Comparative Pharmacological Study of Sparteine and its Ketonic Derivative Lupanine from Seeds of Lupinus albus

Abstract

The pharmacological properties of lupanine (ketonic derivative of sparteine) isolated from seeds of Lupinus albus, in comparison with sparteine were investigated. Ganglioplegic activities and affinity for cholinergic receptors were studied. Lupanine 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. Furthermore, lupanine is much less toxic in one single injection in both the mouse and the guinea-pig. The two substances have an identical inhibitory action on nicotinic type hypertension produced by injection of acetylcholine (500 µg/ kg i.v.) in the atropine-treated dog. The in vitro binding study confirms the selectivity on nicotinic sites with similar affinities for the two drugs. Differences in the bio-availability and the pharmacokinetics of the two alkaloids are presumed. Lupanine may diffuse and disappear more rapidly in ganglia than sparteine.