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CAS No. : 720704-34-7
MCE 国际站:GSK356278
产品活性:GSK356278 是一种有效,选择性,具有口服活性和可透过血脑屏障的磷酸二酯酶 4 (PDE4) 抑制剂,对人 PDE4A,PDE4B 和 PDE4D 的 pIC50 值分别为 8.6、8.8 和 8.7。GSK356278 具有抗炎活性,并具有抗焦虑和增强认知的作用。
研究领域:Metabolic Enzyme/Protease
作用靶点:Phosphodiesterase (PDE)
In Vitro: GSK356278 competes with [3H]rolipram for the high affinity rolipram binding site (HARBS) with a pKi of 8.6 in a competitive filtration-binding assay to the recombinant human PDE4B2B enzyme expressed in yeast membranes.
GSK356278 bounds to the HARBS in rats, mice, marmosets, and ferrets with pKis of 7.9, 7.8, 8.4, and 8.5, respectively.
GSK356278 inhibits LPS-induced release of TNF-α in human whole blood, with a pIC50 of 7.6.
In Vivo: GSK356278 (0.003-30 mg/kg; p.o.) shows anti-inflammatory activity in rodents at exposures that does not induce pica feeding.
GSK356278 (0.1-0.1 mg/kg; p.o.) demonstrates efficacy in a nonhuman primate model of anxiety at exposures that do not induce emesis.
GSK356278 (4 doses at 0.03, 0.1, 0.3, and 1.0 mg/kg for 6 weeks; p.o.) enhances performance in a nonhuman primate object retrieval test.GSK356278 exhibits oral bioavailability (rat 91%, monkey 23%) and Cmax (rat 205, monkey 41 nM) following oral administration (rat 1, monkey 0.2 mg/kg).
GSK356278 exhibits terminal elimination half-lives (rat 2.2, monkey 1.5 h) due to moderate blood clearance (rat 40, monkey 16 mL/min/kg) combined with volumes of distribution (rat 6.3, monkey 2.1 L/kg) following intravenous administration (rat 1, monkey 0.2 mg/kg).
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