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

Medicinal Chemistry and Therapeutic Potential of Agonists, Antagonists and Allosteric Modulators of A1 Adenosine Receptor: Current Status and Perspectives. Curr Pharm Des. 2019 Jul 15;: Authors: Deb PK, Deka S, Borah P, Abed SN, Klotz KN Abstract 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 ...
Source: Epilepsy Curr - Category: Neurology Authors: Tags: Curr Pharm Des Source Type: research

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Publication date: Available online 20 September 2020Source: Materials Today: ProceedingsAuthor(s): Mohd Javeed Mehdi, N Srinivasrao, A Sireesha
Source: Materials Today: Proceedings - Category: Materials Science Source Type: research
There is good news and bad news when it comes to our understanding of inflammation in the pathogenesis and treatment of major depressive disorder (MDD). The bad news is that, like the dexamethasone suppression test or the efficacy of antidepressants before it, inflammation is oversold as an answer to the mystery of depression and its treatment. The good news is that an unusually replicable set of findings (for psychiatry) increasingly paints a consistent picture of the ways in which inflammation is of value in understanding MDD.
Source: Biological Psychiatry - Category: Psychiatry Authors: Tags: Commentary Source Type: research
Challenges to the diagnosis and treatment of patients with psychiatric disorders have long been acknowledged in the field. In recent years, efforts have been made to identify genomic biomarkers for psychiatric disorders. A link between immune function and major depressive disorder (MDD) has been suggested for decades (1), but the identification of differentially expressed genes (DEGs) that underlie immune function as biomarkers for MDD has been more recent. Hundreds of DEGs have been reported for transcriptome-wide association studies (TWASs) of MDD.
Source: Biological Psychiatry - Category: Psychiatry Authors: Tags: Commentary Source Type: research
Our brains are built to consider and reflect on the unknown. These adaptive features protect us from potential threats in dynamic and complex environments, but they can also lead us to perseverate on perceived threats and fear an unknown future. Ranging across a spectrum from adaptive to maladaptive, anxious and fearful behavior exists in many animal species. In an effort to develop new therapeutics and understand the etiology of anxiety-related conditions, such as anxiety disorders, obsessive-compulsive disorder, panic disorder, and posttraumatic stress disorder, research using laboratory animal models has focused on the ...
Source: Biological Psychiatry - Category: Psychiatry Authors: Tags: Early Career Investigator Commentary Source Type: research
to: “Major Depressive Disorder Is Associated With Differential Expression of Innate Immune and Neutrophil-Related Gene Networks in Peripheral Blood: A Quantitative Review of Whole-Genome Transcriptional Data From Case-Control Studies,” by Wittenberg et al. (Biol Psychiatry 2020; 88:625–637); http s://doi.org/10.1016/j.biopsych.2020.05.006.
Source: Biological Psychiatry - Category: Psychiatry Tags: Erratum Source Type: research
CONCLUSION: The 2010 SPILF-AFSSAPS guiding criteria for Streptococcus pneumoniae CAP are found in very variable proportions and do not, in their current form, make it possible to accurately guide towards a pneumococcal etiology in patients included in the PACSCAN study. PMID: 32950610 [PubMed - as supplied by publisher]
Source: Medecine et Maladies Infectieuses - Category: Infectious Diseases Tags: Med Mal Infect Source Type: research
Presentation of CF, airway clearance regimens, diabetes in CF, and other highlights from the cystic fibrosis episode of The Cribsiders podcast.Medscape Pediatrics
Source: Medscape Allergy Headlines - Category: Allergy & Immunology Tags: Pediatrics Commentary Source Type: news
Authors: MacDonald-Ramos K, Michán L, Martínez-Ibarra A, Cerbón M Abstract Silymarin is obtained from the Milk thistle plant Silybum marianum and has been used over the centuries to treat principally liver disease, although it has also been studied for its beneficial effects in cardioprotection, neuroprotection, immune modulation, and cancer among others. Importantly, silymarin's active component silybin is a flavonolignan that exhibits different activities such as; scavenger, anti-oxidant, anti-inflammatory, and recently revealed, insulin-sensitizing properties which have been explored in clin...
Source: Annals of Hepatology - Category: Gastroenterology Tags: Ann Hepatol Source Type: research
CONCLUSION: Type 4 collagen could predict the presence of significant and advanced fibrosis in NAFLD patients and it would be a useful tool in routine clinical practice. PMID: 32949785 [PubMed - as supplied by publisher]
Source: Annals of Hepatology - Category: Gastroenterology Tags: Ann Hepatol Source Type: research
Abstract Pulmonary comorbidities and ASA physical status class III and IV can significantly increase the rate of major complications after ISC placement. Patients with an underlying pulmonary comorbidity or lung disease (chronic obstructive pulmonary disease, asthma, or obstructive sleep apnea) have a 2.2-fold increased risk of having any complication and a 2.4-fold increased risk of having a major pulmonary complication compared to those without pulmonary comorbidities. Patients with pulmonary comorbidities may benefit from alternative pain management strategies to avoid complications in the early postoperative p...
Source: The Orthopedic Clinics of North America - Category: Orthopaedics Authors: Tags: Orthop Clin North Am Source Type: research
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