Mepenzolate Bromide - CAS 76-90-4
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Not Intended for Therapeutic Use. For research use only.
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Mepenzolate Bromide is a muscarinic antagonist used to treat gastrointestinal disorders, and decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction.
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1.Superiority of pulmonary administration of mepenzolate bromide over other routes as treatment for chronic obstructive pulmonary disease.
Tanaka K1, Kurotsu S1, Asano T1, Yamakawa N1, Kobayashi D1, Yamashita Y1, Yamazaki H1, Ishihara T1, Watanabe H2, Maruyama T2, Suzuki H3, Mizushima T1. Sci Rep. 2014 Mar 28;4:4510. doi: 10.1038/srep04510.
We recently proposed that mepenzolate bromide (mepenzolate) would be therapeutically effective against chronic obstructive pulmonary disease (COPD) due to its both anti-inflammatory and bronchodilatory activities. In this study, we examined the benefits and adverse effects associated with different routes of mepenzolate administration in mice. Oral administration of mepenzolate caused not only bronchodilation but also decreased the severity of elastase-induced pulmonary emphysema; however, compared with the intratracheal route of administration, about 5000 times higher dose was required to achieve this effect. Intravenously or intrarectally administered mepenzolate also showed these pharmacological effects. The intratracheal route of mepenzolate administration, but not other routes, resulted in protective effects against elastase-induced pulmonary damage and bronchodilation at a much lower dose than that which affected defecation and heart rate.
2.Muscarinic cholinergic receptors in human narcolepsy: a PET study.
Sudo Y1, Suhara T, Honda Y, Nakajima T, Okubo Y, Suzuki K, Nakashima Y, Yoshikawa K, Okauchi T, Sasaki Y, Matsushita M. Neurology. 1998 Nov;51(5):1297-302.
OBJECTIVES: To investigate the function of the muscarinic cholinergic receptor (mAchR) in narcolepsy and the effects of pharmacotherapy on mAchRs.
3.Quantitative capillary column gas chromatographic method for the determination of glycopyrronium in human plasma.
Murray GR, Calvey TN, Williams NE, Chan K. J Chromatogr. 1984 Jun 8;308:143-51.
A new sensitive and selective capillary column gas chromatographic method for the anti-cholinergic agent glycopyrronium bromide in human plasma is described. The procedure involves preliminary ion-pair extraction of the drug into dichloromethane, followed by concentration and analysis of the ion-pair complex by capillary column gas chromatography using a nitrogen-sensitive detector. The method depends on the thermal dequaternisation of the quaternary ammonium compound and can be used to detect 5 ng/ml in a 3-ml plasma sample. The assay procedure has been applied to the determination of the plasma concentration of glycopyrronium after intravenous administration to an anaesthetised patient.
4.Isolation of cholinergic active ingredients in aqueous extracts of Mareya micrantha using the longitudinal muscle of isolated guinea-pig ileum as a pharmacological activity marker.
Tsai CS1, Guede-Guina F, Smith MO, Vangah-Manda M, Ochillo RF. J Ethnopharmacol. 1995 Mar;45(3):215-22.
In our attempt to isolate the pharmacologically active ingredients in the aqueous extracts of Mareya micrantha, we have selected the contractions of the longitudinal muscle of the isolated guinea-pig ileum preparation as a pharmacological marker to monitor retention of pharmacological activity during the chromatographic separation. The aqueous extracts of Mareya micrantha elicited concentration-dependent contractions of the preparation. The maximum response elicited by the aqueous extracts was 50% of the maximum response elicited by the maximum dose of acetylcholine (ACh), 10(-7) M. Mepenzolate (10(-8)-10(-5) M), a specific muscarinic receptor antagonist, similarly antagonized contractions elicited by the aqueous extracts suggesting that the cholinergic ingredient(s) in the extract are acting at the muscarinic receptors of the preparation. Fraction 2-4, which was separated from the aqueous extracts by Sephadex gel chromatography, dose-dependently elicited contractions of the preparation.
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CAS 76-90-4 Mepenzolate Bromide

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