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编 号:F391882
分子式:C20H16N2O5S
分子量:396.42
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma.

体内研究:
PIT (10 mg/kg; i.p.; for 5 days) significantly protects both the white matter and the cortical plate lesions against the insult in mice with S-bromo-willardiine injection induced tonic and tonicoclonic seizures.

体外研究:
PIT (0.1-10 μM) non-competitively and dose-dependently diminishs human P2Y1 receptor signaling with an IC50 value of 0.14 μM.PIT (0.1-10 μM) completely blocks the agonist activity of 2-MeSADP.PIT (1 nM-10 μM) dose-dependently inhibits the accumulation of inositol phosphates induced by the agonist 2-MeSADP.PIT (1 nM-10 μM) dose-dependently blocks the P2Y1 receptor signaling induced by the endogenous agonist ADP.PIT (0.1-3 μM) increases ATP-responses 2-5 fold, while higher concentrations (3-100 μM) inhibits ATP-mediated inward current with an IC50 value of 13.2 μM.PIT shows a low affinity for a range of membrane receptors, including: α1, α2-adrenoceptors, 5-HT1A, 5-HT1B, 5-HT2, 5-HT3, D1, D2, muscarinic, central benzodiazepine, H1, μ-opioid, dihydropyridine and batrachotoxin receptors with pKi values of PIT 相关抗体:
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