• Korean Journal of Veterinary Research
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• v.34 no.1
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• pp.63-67
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• 1994

Berberine $(10^{-7}-10^5M)$ increased the contractility dose-dependently in isolated rabbit ileal and jejunal segments. Atropine and hemicholinium abolished this response but not mecamylamine. Berberine$(10^{-8}-10^5M)$ enhanced the transmurally-stimulated(80 V, 0.5 ms, 0.05 Hz) twitch response in the isolated guinea-pig ileal segments. Atropine and hemicholinium also abolished this response but not mecamylamine. Effect of KCI, carbachol and histamine were not affected by pretreatment with berberine$(10^{-5}M)$. The results of our study suggest that berberine increases the intestinal contractility by increasing a small amount of acetylcholine release from the postganglionic parasympathetic nerve terminal but not by a direct activation of muscarinic receptors.

• Journal of Convergence for Information Technology
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• v.11 no.10
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• pp.131-137
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• 2021

The aim of the study was to observe the influence and related mechanism of histamine and its analogues used for hypersensitivity tests and used as an indicator of impurities in drugs on the tissue-specific intestinal contraction. Intestinal contraction includes the activation of thick or thin filament regulation. However, there are few reports addressing the question whether this regulation is involved in histamine-induced regulation. We hypothesized that histamine plays a role in tissue-dependent regulation of intestinal contractility. Denuded ileal/colonic longitudinal and circular muscles of male rats were used and isometric contractions were recorded using a data acquisition system. Interestingly, histamine alone didn't increase the contraction of the circular muscle but increased the contraction of the longitudinal muscle. Histamine together with atropine (M3 receptor antagonist) didn't inhibit the contraction of the longitudinal and circular muscle. Therefore, histamine alone and together with atropine increases the ileal longitudinal muscle contraction suggesting that additional mechanisms (decreased receptor density, postreceptor signaling or distribution of agonists) might be involved in the regulation of ileal muscle contractility. In conclusion, histamine and/or atropine has some effect on the regulation of the longitudinal contractility regardless of M3 receptor and the simpler test would be preferred as the drug impurity test compared to more complicated tests.

• Journal of Convergence for Information Technology
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• v.10 no.10
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• pp.109-114
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• 2020

The aim of the study was to observe the influence and related mechanism of rebamipide on the intestinal contraction. Intestinal contraction includes the activation of thick or thin filament regulation. However, there are few reports addressing the question whether this regulation is involved in rebamipide-induced regulation. We hypothesized that rebamipide plays a role in intestinal contraction evoked by carbachol in rat intestine. Interestingly, rebamipide alone didn't inhibit and rather slightly increased the contraction in the denuded muscle. Therefore, rebamipide alone and together with indomethacin increases the ileal contraction suggesting that additional pathways might be involved in the regulation of ileal contractility. In conclusion, rebamipide has some effect on the regulation of contractility and anti-ulcer by NSAIDs.

• Biomolecules & Therapeutics
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• v.13 no.1
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• pp.26-31
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• 2005

The present study examined effects of a water-soluble fraction from mulberry leaves (ML water fraction) on the circulatory and autonomic nervous systems, which were compared with those of acetylcholine (ACh) used as a reference drug in order to elucidate its mechanism of action. Intravenous administration of ACh or a ML water fraction produced temporary depressor and tachycardiac responses in a dose-dependent manner in unrestrained, conscious Sprague-Dawley rats. The systemic hemodynamic effects of ACh and a ML water fraction were almost completely blocked by pretreatment with atropine, a muscarinic antagonist. The depressor responses to ACh and a ML water fraction were slightly enhanced and prolonged by pretreatment with neostigmine, an anticholinesterase, whereas the tachycardiac responses were remarkably blocked by pretreatment with pentolinium, a ganglionic blocking agent. In vitro experiments using the ileum isolated from rats showed that ACh and a ML water fraction increased ileal contractility in a dose-dependent manner. The increases in ileal contractility were also completely abolished in the presence of atropine. Finally, the specific binding of [$^3H$]quinuclidinyl benzilate, a muscarinic antagonist, to rat cortical synaptic membranes was inhibited by a ML water fraction in a concentration-dependent manner with an IC$_{50}$ value of 9.5 mg/ml. The results suggest that the effects of a ML water fraction are mediated through direct stimulation of muscarinic cholinergic receptors by unknown cholinomimetic substance(s) contained in that fraction.

• The Korean Journal of Physiology and Pharmacology
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• v.1 no.6
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• pp.769-774
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• 1997

Non-neuronal high affinity binding sites for benzodiazepines have been found in many peripheral tissues including cardiac muscle and vascular smooth muscle, and have been designated as 'peripheral benzodiazepine receptor'. Benzodiazepines have been shown to induce relaxation of the ileal, vesical, and uterine smooth muscles. However, it is still unclear about possible involvement of peripheral benzodiazepine receptor on the contractility of trachealis muscle. This study was performed to investigate the role of the peripheral benzodiazepine receptor on the contractility of canine trachealis muscle. Canine trachealis muscle strips of 15 mm long were suspended in an isolated organ bath containing 1 ml of physiological salt solution maintained at $37^{\circ}C$, and aerated with $95%\;O_2/5%\;CO_2$. Isometric myography was performed, and the results of the experiments were as follows: Ro5-4684, FGIN-1-27 and clonazepam reduced a basal tone of isolated canine trachealis muscle strip concentration dependently, relaxant actions of RoS-4684 and FGIN-1-27 were antagonized by PK11195, a peripheral benzodiazepine receptor antagonist. Flumazenil, a central type antagonist, did not antagonize the relaxant action of Peripheral type agonists. Saturation binding assay of [3H]Ro5-4864 showed a high affinity$(Kd=5.33{\pm}1.27nM,\;Bmax=\;867.3{\pm}147.2\;fmol/mg\;protein)$ binding site on the canine trachealis muscle. Ro 5-4684 suppressed the bethanechol-, 5-hydroxyoyptamine- and histamine- induced contractions. Platelet activating factor (PAF) exerted strong and prolonged contraction in trachealis muscle strip. Strong tonic contraction by PAE was attenuated by Ro 5-4684, but not by WEB 2086, a PAF antagonist. Based on these results, it is concluded that the peripheral benzodiazepine receptor mediates the inhibitory regulation of contractilty of canine trachealis muscle.

• Journal of Yeungnam Medical Science
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• v.6 no.2
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• pp.13-22
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• 1989

To investigate the effect of diazepam on the contractility of the intestinal smooth muscle, longitudinal muscle strip isolated from rat ileum was prepared for myography in isolated organ bath. 1) Basal tone of ileal muscle was reduced by diazepam concentration-dependently. 2) Higher concentrations(30 and 100 microM) of diazepam inhibited(p<0.05, p<0.001) the carbachol-induced contraction in a concentration-dependent manner ; but lower concentration of diazepam(10 microM) enhanced(p<0.05). 3) Histamine-induced contraction was inhibited by pretreatment with diazepam in a concentration-dependent manner. 4) $Ca^{++}$-induced tension recovery in calcium-free solution was inhibited in the presence of diazepam concentration-dependently. These results suggest diazepam reduces the contractility of the longitudinal muscle isolated from rat ileum via interference with influx of calcium into the muscle cells.