THE EFFECTS OF 1, 3-DIOXOLANE DERIVATIVE (ESPERAN) ON THE SMOOTH MUSCLE AND ITS INTRINSIC NERVES OF GUINEA-PIG STOMACH

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The general pharmacological actions of 1, 3-dioxolane derivative (Esperan) were investigated. Esperan reduced tonic tension and the size of the spontaneous contractions, but did not affect the frequency. These findings were not influenced by hyoscine (1μg/ml), atropine (1μg/ml) and tetrodotoxin (0.1μg/ml), nor by α-blocker (phentolamine) (1 μg/ml), or β-blocker (propranolol) (1 μg/ml). Esperan blocked completely the action of ACh and the dose response curve showed that it is a competitive blocker. The excitatory nerve response by electrical stimulation was rapidly and completely suppressed by esperan (0.1 μg/m/), but the inhibitory response was not modified by the drug. Eserine- and ACh-induced facilitation of the excitatory response was also suppressed by Esperan. The contraction in the longitudinal muscle and relaxation in the circular muscle induced by serotonin (5-HT) was not modified by Esperan (1 μg/ml). However, facilitation of the excitatory nerve response by 5-HT was completely blocked by Esperan. Therefore, it may be concluded that Esperan blocks only "M"-receptors, but not "D"-receptors. Thus the present experiments show that esperan has two separate effects: (1) a potent atropine-like action, (2) a papaverine-like action.
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