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PIT

CAS No. : 56583-49-4

MCE 国际站：PIT

产品活性：PIT (2,2'-Pyridylisatogen tosylate) 是 P2Y1 受体 的选择性和非竞争性拮抗剂，对人 P2Y1 受体的 IC₅₀ 值为 0.14 μM。PIT 在不影响核苷酸结合的情况下拮抗 P2Y1 受体信号。PIT 是一些平滑肌中代谢性嘌呤受体 (P2Y 家族) 对 ATP 反应的不可逆拮抗剂。PIT 可用于慢性支气管炎和哮喘的研究。

研究领域：GPCR/G Protein

作用靶点：P2Y Receptor

In Vitro: 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-HT_1A, 5-HT_1B, 5-HT₂, 5-HT₃, D₁, D₂, muscarinic, central benzodiazepine, H₁, μ-opioid, dihydropyridine and batrachotoxin receptors with pK_i values of <5.
PIT shows affinity to an adenosine (A₁) receptor with a pK_i value of 5.3.
PIT (12.5-50 μM) irreversibly antagonizes relaxations of ATP in guinea-pig isolated taenia caeca.

In Vivo: 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.

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