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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Source: NeuroImage: Clinical - Category: Radiology Source Type: research
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Source: Academic Radiology - Category: Radiology Source Type: research
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Source: Social Science and Medicine - Category: Psychiatry & Psychology Source Type: research
Discussion/conclusionThe study hypothesis was confirmed: there were no differences according to primary versus secondary osteoarthritis in preoperative profile or results. Elbow osteoarthritis entails mechanical impingement. Arthroscopic debridement gave good results independently of primary or post-traumatic etiology.Level of evidenceIII, prospective comparative observational multicenter cohort study.
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Source: L Encephale - Category: Psychiatry Tags: Encephale Source Type: research
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Source: L Encephale - Category: Psychiatry Tags: Encephale Source Type: research
This study is a prospective, exploratory, qualitative analysis. Twenty midwives from Grenoble Alpes University Hospital who took care of one of the selected patients participated in this study. Two women had schizophrenia and one bipolar disorder. Interviews realized with a semi-structured guide were fully transcribed, anonymized and thematically analyzed. Topics have been structured according to the number of occurrences to build a thematic tree. RESULTS: Midwives felt insecure and resourceless when the postpartum care was unclear, insufficiently anticipated and in case of a danger for the women or the children. They ...
Source: L Encephale - Category: Psychiatry Tags: Encephale Source Type: research
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Source: L Encephale - Category: Psychiatry Tags: Encephale Source Type: research
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Source: Journal of Functional Foods - Category: Nutrition Source Type: research
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