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GR79236

CAS No. : 124555-18-6

MCE 国际站：GR79236

产品活性：GR79236 是一种高效，选择性和具有口服活性的腺苷 A1 受体 (adenosine A1 receptor) 激动剂，对于 A1 和 A2 受体的 K_i 值分别为 3.1 nM 和 1300 nM。GR79236 具有抗伤害和抗炎作用。

研究领域：GPCR/G Protein

作用靶点：Adenosine Receptor

In Vitro: GR79236 inhibits Isoprenaline-stimulated cAMP accumulation in DDT-MF2 cells with an IC₅₀ of 2.6 nM.
GR79236 inhibits catecholamine-induced lipolysis in human, rat and dog isolated adipocytes.

In Vivo: GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED₅₀s of 0.13 mg/kg and 0.3 mg/kg, respectively).
Oral administration of GR79236 (0.1-10 mg/kg) to fed rats induces minimal changes in the plasma concentration of non-esterified fatty acids and in the blood concentrations of glucose and lactate.
Intravenous infusion of GR79236 to fasted pithed rats, or oral administration of GR79236 to fasted conscious rats and dogs, produces time- and dose-dependent decreases in the plasma non-esterified fatty acid concentration. In the fasted rats, doses of GR79236 that lowered plasma levels of non-esterified fatty acids also produced hypotriglyceridaemia and anti-ketotic effects.

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