Mechanism of action of species-selective P2X7 receptor antagonists
نویسندگان
چکیده
منابع مشابه
QSAR studies and application of genetic algorithm - multiple linear regressions in prediction of novel p2x7 receptor antagonists’ activity
Quantitative structure-activity relationship (QSAR) models were employed for prediction the activity of P2X7 receptor antagonists. A data set consisted of 50 purine derivatives was utilized in the model construction where 40 and 10 of these compounds were in the training and test sets respectively. A suitable group of calculated molecular descriptors was selected by employing stepwise multiple ...
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The ATP-gated P2X7 receptor (P2X7R) is a non-selective cation channel which senses high extracellular ATP concentrations and has been suggested as a target for the treatment of neuroinflammation and neurodegenerative diseases. The use of P2X7R antagonists may therefore be a viable approach for treating CNS pathologies, including epileptic disorders. Recent studies showed anticonvulsant potentia...
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The P2X7 receptor is a trimeric ATP-gated cation channel found predominantly, but not exclusively, on immune cells. P2X7 activation results in a number of downstream events, including the release of proinflammatory mediators and cell death and proliferation. As such, P2X7 plays important roles in various inflammatory, immune, neurologic and musculoskeletal disorders. This review focuses on the ...
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The 5-HT7 receptor is the most recent addition to the 5-HT receptor family and has been linked to a variety of physiological and pathophysiological processes. Well established antidepressant pharmaceuticals have recently been found to activate the 5-HT7 receptor, supporting the role of the 5-HT7 receptor in the antidepressant mechanism. The synthesis of potent selective 5-HT7 receptor antagonis...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2009
ISSN: 0007-1188,1476-5381
DOI: 10.1111/j.1476-5381.2009.00135.x