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Chirality May 2020The modern β-adrenergic agonists (β-blockers) possess one or more than one chiral center in their structure. Two enantiomers exhibit distinct pharmacodynamic and... (Review)
Review
The modern β-adrenergic agonists (β-blockers) possess one or more than one chiral center in their structure. Two enantiomers exhibit distinct pharmacodynamic and pharmacokinetic behaviors. Current progress in drug designing has resulted in the ability to understand the role of chirality in modern therapeutics. Furthermore, with a greater understanding of the molecular structure of precise drug targets, development of new drugs is directed towards the pure enantiomers instead of its racemates. The present review deals with a discussion on the stereochemical facets of chiral clinical β-blockers. This review provides details of stereo-selectivity in the pharmacological behavior of some of β-blockers and their metabolites. An effort has been made on highlighting the distinction between the therapeutic behavior of the racemic mixtures and pure enantiomers.
Topics: Adrenergic beta-Antagonists; Humans; Stereoisomerism
PubMed: 32105373
DOI: 10.1002/chir.23200 -
Molecules (Basel, Switzerland) Jan 2021β-adrenergic antagonists (β-blockers) with at least one chiral center are an exceedingly important class of drugs used mostly to treat cardiovascular diseases. At... (Review)
Review
β-adrenergic antagonists (β-blockers) with at least one chiral center are an exceedingly important class of drugs used mostly to treat cardiovascular diseases. At least 70 β-blockers have been investigated in history. However, only a few β-blockers, e.g., timolol, are clinically marketed as an optically pure enantiomer. Therefore, the separation of racemates of β-blockers is essential both in the laboratory and industry. Many approaches have been explored to obtain the single enantiomeric β-blocker, including high performance liquid chromatography, supercritical fluid chromatography and simulated moving bed chromatography. In this article, a review is presented on different chromatographic methods applied for the enantioseparation of β-blockers, covering high performance liquid chromatography (HPLC), supercritical fluid chromatography (SFC) and simulated moving bed chromatography (SMB).
Topics: Adrenergic beta-Antagonists; Chromatography, High Pressure Liquid; Chromatography, Supercritical Fluid; Stereoisomerism
PubMed: 33477385
DOI: 10.3390/molecules26020468 -
The Canadian Journal of Cardiology Nov 2023
Topics: Humans; Digoxin; Atrial Fibrillation; Adrenergic beta-Antagonists; Anti-Arrhythmia Agents; Heart Rate
PubMed: 37453646
DOI: 10.1016/j.cjca.2023.07.013 -
Journal of Cancer Research and Clinical... Feb 2017In this review, we aimed to present and discuss the available preclinical and epidemiological evidences regarding the modulation of cancer cell proliferation by... (Review)
Review
PURPOSE
In this review, we aimed to present and discuss the available preclinical and epidemiological evidences regarding the modulation of cancer cell proliferation by β-adrenoceptors (β-AR), with a specific focus on the putative effects of β-blockers according to their pharmacological properties.
METHODS
A comprehensive review of the published literature was conducted, and the evidences concerning the involvement of β-AR in cancer as well as the possible role of β-blockers were selected and discussed.
RESULTS
The majority of reviewed studies show that: (1) All the cancer types express both β1- and β2-AR, with the exception of neuroblastoma only seeming to express β2-AR; (2) adrenergic agonists are able to increase proliferation of several types of cancers; (3) the proliferative effect seems to be mediated by both β1- and β2-AR; (4) binding to β-AR results in a cAMP transient flux which activates two major downstream effector systems: protein kinase A and EPAC and (5) β-blockers might be putative adjuvants for cancer treatment.
CONCLUSIONS
Overall, the reviewed studies show strong evidences that β-AR activation, through several intracellular mechanisms, modulate tumor cell proliferation suggesting β-blockers can be a feasible therapeutic approach to antagonize β-adrenergic response or have a protective effect per se. This review highlight the need for intensifying the research not only on the molecular mechanisms underlying the β-adrenergic influence in cancer, but also on the implications of biased agonism of β-blockers as potential antitumor agents.
Topics: Adrenergic beta-Antagonists; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Clinical Trials as Topic; Humans; Neoplasms; Norepinephrine; Receptors, Adrenergic, beta; Signal Transduction; Tumor Microenvironment
PubMed: 27709364
DOI: 10.1007/s00432-016-2278-1 -
Journal of the American College of... Jun 2023
Topics: Humans; Adrenergic beta-Antagonists
PubMed: 37316111
DOI: 10.1016/j.jacc.2023.04.028 -
Heart (British Cardiac Society) Aug 2022
Topics: Adrenergic beta-Antagonists; Cardiomyopathies; Humans; Takotsubo Cardiomyopathy
PubMed: 35483872
DOI: 10.1136/heartjnl-2022-320950 -
CMAJ : Canadian Medical Association... Nov 2017
Topics: Adrenergic beta-Antagonists; Aging; Essential Tremor; Humans; Primidone
PubMed: 29109210
DOI: 10.1503/cmaj.170128 -
The American Journal of Medicine Aug 2020
Topics: Adrenergic beta-Antagonists; Humans; Performance Anxiety; Propranolol; Students, Medical; Test Taking Skills
PubMed: 32061732
DOI: 10.1016/j.amjmed.2020.01.017 -
Heart Rhythm Sep 2022
Topics: Adrenergic beta-Antagonists; Female; Humans; Infant; Long QT Syndrome; Pregnancy
PubMed: 35700907
DOI: 10.1016/j.hrthm.2022.06.009 -
Cardiovascular & Hematological Agents... 2015Beta-blockers are considered as suitable drugs to treat essential hypertension also in elderly patients and they are currently recommended for treatment of hypertension,... (Review)
Review
Beta-blockers are considered as suitable drugs to treat essential hypertension also in elderly patients and they are currently recommended for treatment of hypertension, even in older patients, by the ESH/ESC Guidelines. Different meta-analyses and results of some large clinical trials have shown that here is no clinically difference between β-blockers and other drug classes in decreasing high blood pressure in elderly hypertensive patients. The new vasodilating β-blockers, as nebivolol, carvedilol and celiprolol, offer additional important advantages, compared with traditional β-blockers. The cardio-protective effect of β-blockers (except atenolol) is not inferior to that obtained with other drug classes which is independent of age and gender of the patients.
Topics: Adrenergic beta-Antagonists; Aged; Animals; Antihypertensive Agents; Contraindications; Humans; Hypertension
PubMed: 25761100
DOI: 10.2174/1871525713666150310112759