Abstract:
The cholinergic effect of the methiodides of galanthamine and lycoramine, two alko- loids extracted from
Lycoris sqamigera Maxim. and
Narcissus papyraceus Ker-Gawl, was studied. Given intravenously, lycoramine and galanthamine caused, in rabbits and cats, a fall of blood pressure as well as an increase of the tonus and peristalsis of intestine. These responses could be antagonized by atropine. Solutions of galanthamine and lycora- mine (both 0.5%) caused contraction of the pupil of rabbits to a variable extent. Galanthamine (1×10
-6g/c.c.) and lycoramine (1×10
-5g/c.c.) produced contraction of iso- lated guinea-pig ileum and still lower concentrations of both preparations increased the contraction induced by acetylcholine, BaCl
2,and histamine. The effect of galanthamine on the M-choline reactive system was 5-10 times stronger than that of lycoramine. It was shown that galanthamine and lycoramine increased the response caused by acetylcholine in the frog rectus and the leech dorsal-muscle, the effect of galanthamine being slightly stronger than lycoramine. In cats and rats, the two drugs caused an in- crease of contracting response of gastrocnemius muscle to nerve stimulation. The effect of galanthamine and lycoramine on the nervemuscle preparations was concerned with stimulating frequencies and doses. Higher frequencies (25-100/sec) and larger doses caused, in many instances, depression of muscle contration; but lower frequencies (5-10/ sec) and smaller doses produced, in most instances, muscle contraction. The effect of galanthamine was 5 times stronger than that of lycoramine. After treatment with atro- pine, the cholinesterase inhibitors, galanthamine, and lycoramine were found to increase the depression of muscle contraction induced by acetylcholine in large doses. Galan- thamine, lycoramine, and neostigmine antagonized muscle paralysis induced by d-tubo- curarine, but not by succinylcholine. Like neostigmine, galanthamine and lycoramine antagonized the ganglionic blockade produced by TEA and C
6, and also increased the contraction response of nictitating mem- brane to nerve stimulation. The stimulating effect of lycoramine on the central M- and N-choline reactive system was stronger than that of galanthamine, In mice, the LD
50 of galanthamine, lycoramine, and neostigmine were found to be 0.958, 16.65, 0,174 mg/kg respectively. The usual toxic symptoms were: salivation, twitching, and convulsion. The animals died usually of respiratory paralysis.