AbstractHyoscine and drotaverine effectiveness was compared for the purposes of achieving optimum distension following insufflation in CT colonography. The in vitro effects of hyoscine and drotaverine on tone and contractility of SM preparations isolated from different areas of human colon were studied by isometric registration of contractile activity. Both medications have a relaxing effect on SM preparations and inhibit their spontaneous contractions. The drotaverine-induced effects were reliably more marked than the hyoscine-induced ones. CT colonography was performed in 70 patients who were injected with equal doses of either hyoscine (n=32) or drotaverine (n=38). The degree of drug-induced distension in both groups was determined by measuring the lumen of the colon on a 2D reconstruction. In most colon areas the width of the distended lumen was greater in the drotaverine-treated patients. We concluded that drotaverine can be used as a means to facilitate colonic distension.

Ursolic acid (UA) in concentrations of 1×10-7 mol/L-5×10-5 mol/L induced relaxation in gastric smooth muscle (SM) tissues, in a concentration-dependent manner. The relaxation did not change membrane potential and slow wave contraction patterns. A significant decrease in amplitude and frequency of spikepotentials was observed. UA-induced reactivity was removed when SM preparations were treated with nifedipine (1×10-6 mol/L). Ca 2+-induced contractions of the depolarized SM preparations (42 mmol/L K + ; Ca 2+-free Krebs solution) were substantially reduced in the presence of UA. It was determined that, in certain concentrations, UA influenced L-type Са 2+ channels, and reduced the Ca 2+ influx.

AbstractA The acetylcholinesterase inhibitors galantamine and tacrine are used to treat Alzheimer’s disease. However, these compounds also affect the gastrointestinal (GI) tract. Here, we compared and analyzed both the effects of galantamine-and tacrine on the evacuatory kinetics of the GI tract in rats. Rats were untreated (n=15) or treated with galantamine (one daily dose of 1 mg/kg per os for 21 days; n=17) or tacrine (one daily dose of 0.5 mg/kg per os for 21 days; n=13) and evacuatory kinetics were assessed using radiological methods. Galantamine initially slowed and then accelerated evacuation, which is characteristic of the majority of cholinesterase inhibitors and is a result of the endogenous acetylcholine accumulated in the GI tissues. In the tacrine-treated rats the contrast medium was kept in the stomach and cecum and its evacuation time was reliably increased. These results indicate that when administered for 20 days, galantamine and tacrine have different effects on motor and evacuatory function in the GI tract of rats, because at certain levels of the tract the tacrine-action is dominated by specific non-cholinergic and non-anticholinesterase mechanisms.

Introduction: Examination of the potential possibilities of 2-chloro-N-(1-(3,4-dimethoxyphenyl)propan-2-yl)-2-phenylacetamide (IQP) to affect bioelectrogenesis and the contractile activity of isolated smooth muscles (SM) from stomach. Aim: Having in mind the structural similarities between the molecules of papaverine and IQP, the aim of the present study was to examine such features of the newly synthesized molecule that may potentially affect the muscle tonus, spontaneous bioelectrical and contractile activities of smooth muscles isolated from the stomach, basing on specific mechanisms of papaverine. Materials and methods: The synthesis of IQP is based on the initially formed aziridine ring by principles of Gilbert’s reaction. Impact of IQP on the bioelectrogenesis and the contractile activity of isolated smooth muscles from male Wistar rats was measured by the single sucrose-gap method and isometrically recorded. Results: IQP (1×10-5 – 2.5×10-4 mol/l) causes muscle relaxation, producing changes in two processes that have influence on the mechanical activity of smooth muscles:1.    Blocked Ca2+ influx through the potential-dependent membrane Ca2+ channels, followed in turn by lowering the Ca2+ intracellular levels. This effect is proved by the changes in the frequency and amplitude of spike-potentials in sucrose-bridge experiments when IQP is applied.2.    Activation of a cAMP-dependent signal cascade. The relaxing effect of IQP was significantly reduced in the presence of KT5720(5×10-6 mol/l), an inhibitor of protein kinase A. Conclusion: We assume that there might be interconnections between these two IQP-dependent processes, because PKA-dependent phosphorylation of the L-type Ca2+ channels in smooth muscles provokes a reaction of inactivation.

The effects of hexapeptide (M.W. 1400) isolated from pig intestine enterocytes and called enterogenin on the motility of gastrointestinal smooth muscle of guinea‐pigs and rats have been studied in vitro. The enhancement of bioelectric and contractile activity observed after treatment with enterogenin is inhibited significantly by the blockers of D2 receptors, halopehdol and droperidol. On the basis of experiments carried out with Ca2+‐antagonists, enterogenin is shown to have a stimulating effect on the intake of Ca2+ by smooth muscle cells. This is considered to be the mechanism of enterogenin action on smooth muscles.