2-Aminoethylisothiuronium(AET)関連化合物の薬理作用(第1報)

抄録

Pharmacological properties of 2-aminoethylisothiuronium (AET) derivatives were examined with 2-aminoethylisothiuronium bromide hydrobromide (I), 2-aminoethyl-N'-phenylisothiuronium bromide hydrobromide (II), 2-(2-aminoethylmercapto) imidazoline bromide hydrobromide (III), 2-aminoethyl-N', N"-dimethylisothiuronium bromide hydrobromide (IV), 2-aminoethyl-N', N"-diethylisothiuronium bromide hydrobromide (V), 2-(2-aminoethylmercapto) benzimidazoline bromide hydrobromide (VI), 2-aminoethyl-N'-α-naphtylisothiuronium bromide hydrobromide (VII), 2-dimethylaminoethylisothiuronium chloride hydrochloride (VIII), 2-diethylaminoethylisothiuronium chloride hydrochloride (IX), 2-diethylaminoethyl-N'-phenylisothiuronium bromide hydrobromide (X), and 2-(2-diethylaminoethylmercapto) imidazoline chloride hydrochloride (XI). Among these compounds, only X showed a hypertensive action on rat, cat, dog, and guinea pig, and caused a prolonged contraction of nictitating membrane of cat. Pressor actions of noradrenaline and tyramine were weakly inhibited by II, VI, VII, and X. Five mg/kg of IV and V depressed the nictitating membrane contractions of cat evoked by preganglionic stimulation of the sympathetic nerve, but did not depress the contractions evoked by postganglionic stimulation. I, VIII, and IX showed marked positive inotropic and chronotropic actions, but II, VI, VII, and X did negative inotropic and chronotropic actions on isolated heart of guinea pig. II, V, VII, and X possessed a marked muscle relaxing action on diaphragm of rat. Their activities were found to be almost the same as that of succinylcholine chloride or more. Local anesthetic, antispasmodic actions, and acute toxicity were also tested.