| Bioactivity | Mepenzolate bromide is an orally administered muscarinic receptor antagonist with Kis of 0.68 and 2.6 nM for hM2R and hM3R, respectively. Mepenzolate bromide can be used to suppress the gastrointestinal hypermotility associated with irritable bowel syndrome[1].Mepenzolate bromide is a GPR109A inhibitor[2]. |
| Target | mAChR |
| Invitro | Mepenzolate not only exerts an anti-inflammatory effect via a muscarinic receptor-independent mechanism, but also a bronchodilatory effect via a muscarinic receptor-dependent mechanism. Mepenzolate is a subtype-non-specific muscarinic antagonist whose bronchodilatory effect and inhibitory effect on intestinal motility can be explained by its antagonistic action on M3R[1]. |
| In Vivo | Mepenzolate bromide, a GPR109A receptor blocker, abolishes the beneficial effects of niacin on body weight, colon wet weight as well as colonic levels of myeloperoxidase (MPO) and VEGF[2]. Mepenzolate bromide is a muscarinic antagonist. Intratracheal administration or inhalation of Mepenzolate bromide decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction. Mepenzolate bromide may be an effective therapeutic for the treatment of chronic obstructive pulmonary disease (COPD) due to its anti-inflammatory and bronchodilatory activities[3]. Animal Model: |
| Name | Mepenzolate bromide |
| CAS | 76-90-4 |
| Formula | C21H26BrNO3 |
| Molar Mass | 420.34 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Yasunobu Yamashita,et al.Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities. Bioorg Med Chem. 2014 Jul 1;22(13):3488-97. [2]. Hesham Aly Salem, et al. Effect of Niacin on Inflammation and Angiogenesis in a Murine Model of Ulcerative Colitis. Sci Rep. 2017 Aug 2;7(1):7139. [3]. Ken-Ichiro Tanaka, et al. Mepenzolate bromide displays beneficial effects in a mouse model of chronic obstructive pulmonary disease. Nat Commun. 2013;4:2686. |
Mepenzolate bromide
CAS: 76-90-4 F: C21H26BrNO3 W: 420.34
Mepenzolate bromide is an orally administered muscarinic receptor antagonist with Kis of 0.68 and 2.6 nM for hM2R and hM
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