筋弛緩薬およびその拮抗薬の研究 (第2報)

モノグアニジノ化合物のカエル骨格筋に対する作用

抄録

Effect of several monoguanidino derivatives was tested on the electrically elicited contraction of frog sciatic nerve-sartorius muscle preparation and following results were obtained:
β-Guanidinoethyl phosphate (II) is guanidine-like compound and promoted the muscle contraction at 10^-2-10^-3M and depressed it at 10^-1M. Creatine (III) and arginine (IV) did not affect the contraction. Benzyl-(VI), phenethyl-(VII), [2-(N-methyl-N-phenylamino)-ethyl]-(VIII), [2-N, N-diphenylamino)ethyl]-(IX), [2-(hexahydro-1-azepinyl)ethyl]-(X), and [2-(octahydro-1-azocinyl)ethyl]-guanidine (guanethidine) (XI) showed neuromuscular block as reported on 1, 1′-decamethylenediguanidine (V) previously. Antagonism between these neuromuscular-blocking monoguanidines and potassium chloride, neostigmine, and edrophonium was tested and it was found that the neuromuscular blocking action of these monoguanidines were antagonized by potassium ion but not by anticholinesterases. From these results, it is concluded that these monoguanidines are neither competitive- nor depolarizing-type muscle relaxants. Guanidine and II antagonized against all these neuromuscular blocking monoguanidines, d-tubocurarine chloride, and succinylcholine chloride. The mode of action of II would differ from that of guanidine, since prior to its antagonistic action, II showed a transient potentiation of neuromuscular blocking action of compounds mentioned above, while guanidine showed only an antagonistic action.