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Lu AF27139

CAS No. : 2097117-06-9

MCE 站：Lu AF27139

产品活性：Lu AF27139 是一种有效的、选择性的、具有口服活性的 P2X7 受体拮抗剂（IC₅₀s 值对人和大鼠分别为 12 和 2.4 nM，Kis 对小鼠、人和大鼠分别为 22、54 和 13 nM ）。Lu AF27139 具有啮齿动物活性和 CNS 渗透特性。Lu AF27139 具有研究中枢神经系统疾病的潜力。

研究领域：Membrane Transporter/Ion Channel

作用靶点：P2X Receptor

In Vitro: Lu AF27139 (compound 1) (10-200 nM) inhibits 100 μM BzATP-induced current in HEK293 cells stably transfected with the rat P2X7R in a dose response manner with an IC₅₀ of 66 nM.
Lu AF27139 (compound 1) (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose.
Lu AF27139 (compound 1) inhibits LPS-primed ａnd BzATP-induced IL-1β release from THP-1 cells with an IC₅₀ of 38 ± 2.5 nM.
Lu AF27139 (compound 1) concentration-dependently blocks IL-1β release in rat ａnd mouse primary cortical microglia primed with LPS ａnd induces with 1 mM BzATP with IC50’s of 38 ± 19 nM in rat ａnd 26 ± 6 nM in mice.

In Vivo: Lu AF27139 (compound 1) (p.o.; 3, 10, ａnd 100 mg/kg) reduces intracerebroventricular (icv) administered LPS-primed ａnd BzATP-triggered IL-1β release in the frontal cortex of rats ａnd mice.
Assessment of Pharmacokinetics (PK) profile of Lu AF27139 (compound 1) in rat.

dose	Cu, plasma (nM)a		Cu, brain (nM)a		Cu, spinal cord (nM)a
(mg/kg, po)	(1 h)	(2 h)	(1 h)	(2 h)	(1 h)	(2 h)
T1	22.4 ± 4.2	22.8 ± 10	5.4 ± 2.6	6.4 ± 2.0	5.20 ± 0.80	10.0 ± 2.0

a: Free plasma, brain, ａnd spinal cord concentrations of Lu AF27139 in rat were determined by the formula (Ct*f_u), where Ct is the total tissue (plasma, brain, or spinal cord) drug concentration ａnd f_u is the fraction unbound in these tissues as determined by ex vivo equilibrium dialysis. Values are expressed as mean ± SEM for n = 3 animals. f_u, plasma = 0.02 ± 0.00, f_u, spinal cord = 0.07 ± 0.03, ａnd f_u, brain = 0.09 ± 0.03. Values are expressed as mean ± SEM for n ≥ 3 experiments.

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