S-Alkoxycarbonylthiamine 類の消化管運動に対する薬理学的研究

抄録

Peristaltic movements of dog intestine (Thiry-Vella loop), and rabbit stomach and duodenum were inhibited by the intravenous administration with higher dosage (5-25 mg/kg) of thiamine (B₁-HCl) or 0, 5-dicarbethoxythiamine (DCET), a derivative of S-Alkoxycarbonylthiamine (S-CAT). Inhibitory effects of B₁-HCI on the peristaltic movements were superior to those of POET, while propulsion of charcoal meal both in the small intestine and large intestine of mice was not affected by B₁-HCI or POET.
In the isolated intestine of rabbits, its pendular movements were inhibited by thiamine derivatives with the following order of potency; DCET≥ Scarbobutoxythiamine (CBT) > S-carbethoxythiamine (CET) =B₁-HCI. Inhibitory effect of B₁-HCl on the peristaltic reflex in the guinea-pig isolated intestine was similar to that of hexamethonium, while that of POET was atropine-like. In the guinea-pig isolated intestine, B₁-HCl specifically antagnized to the nicotine contracture but S-CAT did to not only nicotine but also other spasmogens such as acetylcholine, histamine, barium. Anti-barium effects of thiole derivatives (CET, POET) were also observed in the isolated circular muscle strips of dog intestine, but no effects were observed by the administration of thiazole derivatives (B₁-HCl, O-carbethoxythiamine).
These findings suggest that inhibitory effects of B₁-HCI on the gastrointestinal motility were due to the depression of parasympathetic ganglion in the Auerbach's nerve plexus, but those of S-CAT were not so specific as B₁-HCl.