Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat
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منابع مشابه
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15 صفحه اولQSAR 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 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 ...
متن کاملIsoquinolines as antagonists of the P2X7 nucleotide receptor: high selectivity for the human versus rat receptor homologues.
1-[N, O-Bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine (KN-62) and N-[1-[N-methyl-p-(5 isoquinolinesulfonyl)benzyl]-2-(4 phenylpiperazine)ethyl]-5-isoquinolinesulfonamide (KN-04) potently inhibit the human lymphocyte P2Z receptor, an ATP-gated cation channel [Br J Pharmacol 120:1483-1490 (1997)]. Although the molecular identity of the lymphocyte P2Z receptor has not been est...
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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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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2010
ISSN: 0007-1188
DOI: 10.1111/j.1476-5381.2010.01025.x