化学性质：                                                                                                             

产品描述：                                                                                                            

N-type calcium channel blocker-1 is an orally active analgesic agent which shows high affinity to functionally block N-type calcium channels with an IC50 of 0.7 μM in the IMR32 assay.

N-type calcium channel blocker-1 shows good activities in the IMR32 assay (IC50=0.7 μM). N-type calcium channel blocker-1 is the most orally active N-type calcium channel blocker for analgesia found in a series of compounds[1].

N-type calcium channel blocker-1 shows good activities in the acetic acid anti-writhing model (ED50=4 mg/kg, iv). N-type calcium channel blocker-1 exhibits oral activity (ED50=12 mg/kg, po). A time course study of N-type calcium channel blocker-1 in the anti-writhing model indicates that the CF-1 mice have maximal effect at 120 min after oral dosing at 60 mg/kg. Further evaluation of N-type calcium channel blocker-1 demonstrates several important and advantageous features: the pharmacokinetic profile of N-type calcium channel blocker-1 is improved (Versus of 5.9 L/kg and CL of 26 mL/min/kg) and the logPn of 26 is favorable for CNS agent (logPn measured to be 3.20)[1].

[1]. Hu LY, et al. The discovery of [1-(4-dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethylbutyl)-phen yl]-(3-methyl-but-2-enyl)-amine, an N-type Ca+2 channel blocker with oral activity for analgesia. Bioorg Med Chem. 2000 Jun;8(6):1203-12.

特别提醒：