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.
