Effects of antagonists at the human recombinant P2X7 receptor
نویسندگان
چکیده
منابع مشابه
The P2X7 receptor channel: recent developments and the use of P2X7 antagonists in models of disease.
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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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 effects of cholecystokinin (CCK) receptor antagonists on hypothermia induced by cocaine or morphine have been studied in mice. In the present work, subcutaneous (SC) injection of cocaine (50-150 mg/kg) or morphine (125-500 mg/kg) induced hypothermia in mice. Administration of CCKA receptor antagonist MK-329 (0.5-1.5 mg/kg), CCKB receptor antagonist L-365, 260 (0.5-1.5 mgl kg) and CCK r...
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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...
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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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 1998
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0701958