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JNJ-26489112

CAS No. : 871824-55-4

MCE 站：JNJ-26489112

产品活性：JNJ-26489112 是一种中枢神经系统活性剂，在啮齿类动物中具有广谱抗惊厥活性，可对抗音源性、电性和化学性惊厥。JNJ-26489112 抑制电压门控 Na⁺ 通道和 N 型 Ca²⁺ 通道，也是一种有效的 K⁺ 通道开发剂。JNJ-26489112 对 CA-II (IC₅₀=35 μM) 和 CA-I (18 μM) 有很弱的抑制作用。

研究领域：Neuronal Signaling  |  Membrane Transporter/Ion Channel

作用靶点：Calcium Channel  |  Sodium Channel  |  Potassium Channel

In Vitro: JNJ-26489112 inhibits calcium influx in response to depolarization (fluorescence-based assay) with an IC₅₀ of 34 μM. In a whole-cell, patch-clamp experiment with low-frequency stimulation (0.07 Hz), intended to measure N-type channel activity directly, JNJ-26489112 causes a concentration-dependent increase in inhibition, with an IC₅₀ of 70 μM. JNJ-26489112 is a KCNQ2 channel opener, particularly at -50 mV.

In Vivo: JNJ-26489112 (i.p.) effectively blocks chemically-induced, forelimb clonic seizures in mice ( male CF-1 albino mice) that are caused by subcutaneous bicuculine (Bic), picrotoxin (Pic), or pentylenetetrazol (PTZ), with 1-h ED50 values of 197, 189, or 109 mg/kg, respectively.
In adult male rats, JNJ-26489112 (p.o; 10 mg/kg) treatment shows the Cmax, tmax, F, t1/2, and AUC (total exposure) values in plasma were 9090 ng/mL (33 μM), 53 min, 95%, 8.2 h, and 53,200 ng-h/mL. Linear, dose-related increases in exposure were observed at 10, 30, and 300 mg/kg. JNJ-26489112 (i.v.; 2 mg/kg) treatment shows the Vdss is 390 mL/kg and the CL is 96 mL/h-kg. In female beagle dogs, JNJ-26489112 (p.o; 10 mg/kg) treatment shows the Cmax, tmax, F, t1/2, and AUC values in plasma are 11,500 ng/mL (41 μM), 55 min, 83%, 20 h, and 212,000 ng-h/mL. . JNJ-26489112 (i.v.; 2 mg/kg) treatment shows the the Vdss and CL values are 630 mL/kg and 30 mL/h-kg, respectively.

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