Emerging diuretics for the treatment of heart failure

Adenosine is a purine nucleoside, responsible for the regulation of a wide range of physiological and pathophysiological conditions by binding with four G-protein-coupled receptors (GPCRs), namely A1, A2A, A2B and A3 adenosine receptors (ARs). In particular, A1 AR is ubiquitously present, mediating a variety of physiological processes throughout the body, thus represents a promising drug target for the management of various pathological conditions. Agonists of A1 AR are found to be useful for the treatment of atrial arrhythmia, angina, type-2 diabetes, glaucoma, neuropathic pain, epilepsy, depression and Huntington’s disease, whereas antagonists are being investigated for the treatment of diuresis, congestive heart failure, asthma, COPD, anxiety and dementia. However, treatment with full A1 AR agonists has been associated with numerous challenges like cardiovascular side effects, off-target activation as well as desensitization of A1 AR leading to tachyphylaxis. In this regard, partial agonists of A1 AR have been found to be beneficial in enhancing insulin sensitivity and subsequently reducing blood glucose level, while avoiding severe CVS side effects and tachyphylaxis. Allosteric enhancer of A1 AR is found to be potent for the treatment of neuropathic pain, culminating the side effects related to off-target tissue activation of A1 AR. This review provides an overview of the medicinal chemistry and therapeutic potential of various agonists/partial agonists, antagonists and allosteric modulators of A1 AR, with a particular emphasis on their current status and future perspectives in clinical settings.

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Cardiorenal Syndrome: Biomarkers Linking Kidney Damage with Heart Failure

Soni

Yuan

Ronco

et al. 2009

Biomarkers Med.

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All the vital organs of the body share information by virtue of various biological mediators. Primary pathology of a major organ can lead to dysfunction of the other. Cardiorenal syndrome is an important example of such organ crosstalk. Primary dysfunction of the heart or kidney can lead to injury of the other organ. As molecular injury occurs prior to clinical dysfunction, effective interventions can be planned if one can detect this organ dysfunction at an earlier stage by virtue of some biological markers. Such biomarkers can be substances in urine, serum, imaging maneuvers or any other quantifiable parameters. Some currently available biomarkers are not sensitive enough to provide timely diagnosis of the disorder. An important research priority is the development of newer biomarkers or a panel of biomarkers for the early diagnosis of organ dysfunction, as well as nature of injury, guidance for therapeutic interventions and prognosis. Many newer biomarkers have been studied for both heart and kidney dysfunction. This article focuses on newer biomarkers for the cardiorenal syndrome.

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Emerging diuretics for the treatment of heart failure

Cited by 3 publications

References 39 publications

Diuretics in clinical practice. Part I: mechanisms of action, pharmacological effects and clinical indications of diuretic compounds

Diuretics in clinical practice. Part I: mechanisms of action, pharmacological effects and clinical indications of diuretic compounds

Medicinal Chemistry and Therapeutic Potential of Agonists, Antagonists and Allosteric Modulators of A1 Adenosine Receptor: Current Status and Perspectives

Cardiorenal Syndrome: Biomarkers Linking Kidney Damage with Heart Failure

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