(±)-Bisoprolol hemifumarate (CAS 104344-23-2)
QUICK LINKS
(±)-Bisoprolol hemifumarate is a selective beta1-AR adrenergic antagonist that possesses beta1/beta2 selectivity of approximately 100-fold and a Kd of 2-3 nM at the beta1-AR (beta1 receptor). This blocks the action of epinephrine and other hormones that affect heart rate and constriction of blood vessels. For example, it reduces the production of angiotensin II, aldosterone, endothelin-1, and nitric oxide. Studies have shown that (±)-Bisoprolol hemifumarate has antihypertensive, antianginal, and antiarrhythmic effects. In vitro studies have been conducted in a variety of cell cultures, including human umbilical vein endothelial cells, human coronary artery endothelial cells, and rat aortic smooth muscle cells. In these studies, (±)-Bisoprolol hemifumarate was found to reduce the proliferation of vascular smooth muscle cells, inhibit the production of inflammatory cytokines, and reduce the expression of adhesion molecules. Additionally, it was reported to reduce the expression of proteins involved in the renin-angiotensin system, which is responsible for regulating blood pressure.
(±)-Bisoprolol hemifumarate (CAS 104344-23-2) References
- [Acneiform eruptions induced by cetuximab]. | Walon, L., et al. 2003. Ann Dermatol Venereol. 130: 443-6. PMID: 12843857
- Degradation of raw or film-incorporated beta-cyclodextrin by enzymes and colonic bacteria. | Fetzner, A., et al. 2004. Eur J Pharm Biopharm. 58: 91-7. PMID: 15207542
- Pharmacokinetic variability of routinely administered bisoprolol in middle-aged and elderly Japanese patients. | Taguchi, M., et al. 2005. Biol Pharm Bull. 28: 876-81. PMID: 15863897
- Determination of landiolol, an ultra-short-acting β₁-receptor antagonist, in human plasma by liquid chromatography-tandem mass spectrometry. | He, Q., et al. 2012. J Chromatogr B Analyt Technol Biomed Life Sci. 891-892: 7-11. PMID: 22418070
- Variability of bioavailability and intestinal absorption characteristics of bisoprolol. | Ishida, K., et al. 2013. Drug Metab Pharmacokinet. 28: 491-6. PMID: 23719964
- Development and evaluation of fixed dose bi therapy sublingual tablets for treatment stress hypertension and anxiety. | El-Nabarawi, MA., et al. 2013. J Pharm Bioallied Sci. 5: 191-201. PMID: 24082695
- Direct labelling of myocardial beta 1-adrenoceptors. Comparison of binding affinity of 3H-(-)-bisoprolol with its blocking potency. | Kaumann, AJ. and Lemoine, H. 1985. Naunyn Schmiedebergs Arch Pharmacol. 331: 27-39. PMID: 2866449
- Studies on the receptor profile of bisoprolol. | Klockow, M., et al. 1986. Arzneimittelforschung. 36: 197-200. PMID: 2870719
- Oral and maxillofacial manifestations of chronic kidney disease-mineral and bone disorder: a multicenter retrospective study. | Pontes, FSC., et al. 2018. Oral Surg Oral Med Oral Pathol Oral Radiol. 125: 31-43. PMID: 29104033
- Functional characteristics of a renal H+/lipophilic cation antiport system in porcine LLC-PK1 cells and rats. | Matsui, R., et al. 2018. Drug Metab Pharmacokinet. 33: 96-102. PMID: 29338932
- Bisoprolol: A comprehensive profile. | Bakheit, AH., et al. 2021. Profiles Drug Subst Excip Relat Methodol. 46: 51-89. PMID: 33461700
- Enhanced Transdermal Delivery of Bisoprolol Hemifumarate via Combined Effect of Iontophoresis and Chemical Enhancers: Ex Vivo Permeation/In Vivo Pharmacokinetic Studies. | Teaima, MH., et al. 2021. Pharmaceutics. 13: PMID: 34068544
- In vitro effects of thirty-eight cardiac drugs on human serum paraoxonase. | Argan, O., et al. 2022. Chem Biol Drug Des. 100: 80-89. PMID: 35395139
- Azobisisobutyronitrile loaded on mesoporous silica particles: A new stressor for solid-state oxidative forced degradation studies. | Petřík, J., et al. 2023. J Pharm Biomed Anal. 232: 115417. PMID: 37120974
- Sensitive determination of bisoprolol enantiomers in plasma and urine by high-performance liquid chromatography using fluorescence detection, and application to preliminary study in humans. | Suzuki, T., et al. 1993. J Chromatogr. 619: 267-73. PMID: 8263099
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
(±)-Bisoprolol hemifumarate, 10 mg | sc-203531 | 10 mg | $169.00 | |||
(±)-Bisoprolol hemifumarate, 25 mg | sc-203531B | 25 mg | $270.00 | |||
(±)-Bisoprolol hemifumarate, 50 mg | sc-203531A | 50 mg | $517.00 |