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JNJ-55308942

CAS No. : 2166558-11-6

MCE 站：JNJ-55308942

产品活性：JNJ-55308942 是一种高亲和力、选择性、可透过血脑屏障的 P2X7 功能拮抗剂 (hP2X7: IC₅₀=10 nM, K_i=7.1 nM; rP2X7: IC₅₀=15 nM, K_i=2.9 nM)。JNJ-55308942 口服生物利用度高，可与大脑 P2X7 结合并阻断 IL-1β 从成年啮齿动物脑中释放。

研究领域：Membrane Transporter/Ion Channel

作用靶点：P2X Receptor

In Vitro: JNJ-55308942 shows pK_is of 8.1and 8.5 for recombinant human and rat P2X7 channels, respectively. In human blood and in mouse blood and microglia, JNJ-55308942 attenuates IL-1β release in a potent and concentration-dependent manner.

In Vivo: JNJ-55308942 (30?mg/kg; p.o.) attenuates LPS-induced microglial activation in mice.
In a model of Bacillus Calmette-Guerin (BCG)-induced depression, JNJ-55308942 dosed orally (30?mg/kg), reversed the BCG-induced deficits of sucrose preference and social interaction. After oral dosing, the compound exhibited both dose and concentration-dependent occupancy of rat brain P2X7 with an ED₅₀ of 0.07?mg/kg. The P2X7 antagonist (3?mg/kg, oral) blocked Bz-ATP-induced brain IL-1β release in conscious rats, demonstrating functional effects of target engagement in the brain.
JNJ-55308942 (5 mg/kg; p.o.) shows the F, V_ss, CL, C_max and AUC_24h values are 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively.

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