1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-(哌啶-1-基)-1H-吡唑-3-甲酰胺

生物活性靶点体外研究体内研究 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-(哌啶-1-基)-1H-吡唑-3-甲酰胺试剂级价格

CAS号:183232-66-8
英文名:AM 251
中文名:1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-(哌啶-1-基)-1H-吡唑-3-甲酰胺
CBNumber:CB2169367
分子式:C22H21Cl2IN4O
分子量:555.24
MOL File:183232-66-8.mol

1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-(哌啶-1-基)-1H-吡唑-3-甲酰胺化学性质

熔点 :195-196℃
密度 :1.65±0.1 g/cm3(Predicted)
储存条件 :Store at RT
溶解度 :DMSO: >10 mg/mL, soluble
酸度系数(pKa) :11.31±0.20(Predicted)
形态 :solid
颜色 :white
稳定性 :Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
CAS 数据库 :183232-66-8

安全信息

危险品标志 :Xi
危险类别码 :36/37/38
安全说明 :26-36
WGK Germany :3
海关编码 :2933.39.6190

1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-(哌啶-1-基)-1H-吡唑-3-甲酰胺性质、用途与生产工艺

生物活性 AM251是选择性大麻素1 (CB1) 受体拮抗剂，IC50 为8 nM。AM251也是 GPR55 的激动剂，EC50为39 nM。
靶点

IC50: 8 nM (CB1 receptor)
体外研究

AM251 is a CB1 receptor antagonist/inverse agonist. AM251 produces an agonist response in HEK293 cells, similar to that found in the yeast expression system. AM-251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2 ^+/+ and CB2 ^-/- peritoneal macrophages.
体内研究

The CB1 antagonist AM251 (3 mg/kg, i.p.) decreases capsaicin-evoked nocifensive behavior (F _1,18 =28.45, p<0.0001). This suppressive effect is genotype dependent (F _1,18 =14.83, p<0.01), and the interaction between the effects of genotype and AM251 approached significance (F _1,18 =4.704, p=0.0587). Planned comparisons reveal that AM251 reduces nocifensive behaviors in fatty-acid amide hydrolase (FAAH) KO mice (p<0.01) but fails to alter nocifensive behavior in WT mice (p>0.2) relative to their respective vehicle controls. AM251 (3 mg/kg, i.p.) reduces the duration of heat hypersensitivity in FAAH KO (F _1,9 =21.43, p<0.01) but not WT mice (p>0.3). AM251 suppresses capsaicin-evoked heat hypersensitivity in a time-dependent manner in FAAH KO (F _5,9 =4.349, p<0.01) but not in WT mice (p>0.3). Post-hoc analysis reveals that FAAH KO mice receiving vehicle (i.p.) display heightened thermal hypersensitivity at 30 (p<0.05), 60 (p<0.05), and 90 (p<0.001) minutes post-capsaicin in comparison to FAAH KO animals receiving AM251). One-way ANOVA shows that AM251 (AM-251) injected into the rats significantly decreases both of the percentage of entries in the open arms and time spent in the open arms, compare to controls. The Tukey-Kramer test analysis reveals a significant reduction for the doses of 1 mg/kg (P<0.05) and 5 mg/kg (P<0.01) compare to control rats in the time spent in the open arms. Also, AM251 significantly decreases percentage of entries in the open arms for the doses of 1 and 5 mg/kg (P<0.05).