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At least 19 recordsLinked to original sources

Influence of bethanechol on retained particles deposited on the first bifurcation of rabbits.

Retention of 4 micron 51Cr labelled Teflon particles administered to nine male rabbits via trachea was measured externally. About 5 microliter of a suspension with a particle concentration of 40 mg X ml-1 was deposited on the first bifurcation through a fiberoptic bronchoscope under urethane anesthesia. Over a period of two weeks, the rabbits were exposed twice, under the influence of the cholinergic drug bethanechol chloride and in a control examination. The time period during which 90% of deposited particles had cleared was significantly shorter in the presence of bethanechol (16 h) than in the control experiment (70 h). The magnitude of the fraction which cleared within the first hour did not differ significantly for drug administration and control, being 39.0% and 36.8%, respectively. The fraction which did not clear within the first hour tended (p = 0.1) to clear faster, half-time 10.4 h, when bethanechol chloride was given than it did in the controls, half-time 31.3 h. A reasonable interpretation of the results is that the cholinergic compound, bethanechol, increases bronchial secretion, which results in a reversed movement of the particles that previously penetrated the mucous layer, back to the mucous layer.

Animals↗

[Influence of a muscle relaxant, tizanidine, on gastric acid secretion and gastric ulcer in rats].

Effects of tizanidine, a centrally acting muscle relaxant, on gastric acid secretion and gastric ulcers were studied in the rat. Tizanidine (5 mg/kg, s.c.) did not influence basal acid secretion, but inhibited the centrally stimulated acid secretion in anesthetized rats. Intraduodenal administration of tizanidine (10 mg/kg) also inhibited the centrally stimulated acid secretion. The compound potentiated bethanechol-induced acid secretion at 10 mg/kg, s.c. Clonidine was found to have similar effects to tizanidine at the lower dose. Both tizanidine and clonidine inhibited basal acid secretion at a relatively low dose in conscious rats. Tizanidine (5 mg/kg, s.c.) did not modify indomethacin- and stress-induced ulcers, but Shay ulcers were slightly inhibited by the drug. Indomethacin ulcers were significantly inhibited by 10 mg/kg, s.c., 10 mg/kg, p.o. or 20 mg/kg, p.o. of tizanidine. Clonidine also was found to be a strong inhibitory agent of indomethacin-, stress- and Shay-ulcers. These results suggest that similar to clonidine, a high dosage of tizanidine influences gastric acid secretion and gastric ulcers, although the activity is lower than that of clonidine.

Anesthesia↗

Effects on gastric acid secretion of a steroidal alkaloid, epipachysamine-A, extracted from Pachysandra terminalis Sieb. et Zucc.

Effect of a steroidal alkaloid, epipachysamine-A, extracted from Pachysandra terminalis Sieb. et Zucc. on gastric acid secretion was studied in rats. Epipachysamine-A prevented 2-deoxy-D-glucose- or thyrotropin-releasing hormone-stimulated gastric acid secretion in anesthetized rats. However, the compound did not influence bethanechol- or electrical vagal stimulation-induced gastric acid secretion. These results suggest that the effect of epipachysamine-A is due to the influence on the central nervous regulatory mechanism in the gastric acid secretion.

Alkaloids↗

Effect of cimetropium bromide and other antispasmodic compounds on in vitro guinea-pig gallbladder.

The effect of cimetropium bromide, a new antimuscarinic compound, on bethanechol- and electrically-induced contractions was studied on isolated guinea-pig gallbladder. Atropine and two other widely employed antispasmodics (i.e., rociverine and octylonium bromide) were employed as reference compounds. Cimetropium and atropine proved to be competitive antimuscarinics, their pA2 being 7.77 +/- 0.14 and 8.31 +/- 0.14, respectively. On the contrary, rociverine displayed a dual effect being a competitive antagonist at low (up to 10(-5) mol/l) and a mixed one at high (greater than 10(-5) mol/l) concentrations. When tested against bethanechol- and electrically-induced contractions, all the compounds, with the exception of octylonium bromide, showed a concentration-dependent relaxant effect. In both experimental conditions, the potency of cimetropium was of the same order of magnitude as that of atropine and 150-200 times higher than that of rociverine. These data, together with the reported activity on human gallbladder in vivo and the well known involvement of cholinergic system in the control of gallbladder motility, could represent the rationale for the clinical use of cimetropium in the treatment of biliary colics as well as spasms of biliary tree.

Animals↗

Inhibition of gastric acid secretion in the dog by the H2-receptor antagonists, ranitidine, cimetidine, and metiamide.

The new H2-receptor antagonist, ranitidine, has been compared with cimetidine and metiamide as an inhibitor of gastric acid secretion in the dog. All three compounds were effective both intravenously or by mouth in inhibiting secretion induced by histamine, pentagastrin, or bethanechol. This inhibition was mainly attributable to a reduction in the volume of secretion, although there was also a significant reduction in the concentration of acid secreted. Metiamide was slightly less active than cimetidine, but ranitidine was four to nine times more potent than cimetidine, depending on the secretagogue used. The antisecretory activity of ranitidine does not result from a limitation in blood flow to the gastric mucosa.

Animals↗