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183232-66-8

中文名稱 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
英文名稱 AM 251
CAS 183232-66-8
分子式 C22H21Cl2IN4O
分子量 555.24
MOL 文件 183232-66-8.mol
更新日期 2024/12/13 09:52:59
183232-66-8 結(jié)構(gòu)式 183232-66-8 結(jié)構(gòu)式

基本信息

中文別名
化合物AM251
1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-1-哌啶基-1H-吡唑-3-甲酰胺
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
英文別名
AM AM
AM 251
CS-985
AM 251 NEW
AM-251 ,99%
AM251
AM-251
AM 251 (pharmaceutical)
1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide
1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-1-PIPERIDINYL-1 H-PYRAZOLE-3-CARBOXAMIDE
1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-
所屬類別
生物化工:Cannabinoid Receptor 拮抗劑

物理化學(xué)性質(zhì)

熔點195-196℃
密度1.65±0.1 g/cm3(Predicted)
儲存條件Store at RT
溶解度DMSO: >10 mg/mL, soluble
溶解度DMSO:>10 mg/mL
酸度系數(shù)(pKa)11.31±0.20(Predicted)
形態(tài)solid
顏色white
穩(wěn)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 數(shù)據(jù)庫183232-66-8

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H319-H335
危險品標(biāo)志Xi
危險類別碼36/37/38
安全說明26-36
WGK Germany3
WGK Germany3
海關(guān)編碼2933.39.6190

常見問題列表

生物活性
AM251是選擇性大麻素1 (CB1) 受體拮抗劑,IC50 為8 nM。AM251也是 GPR55 的激動劑,EC50為39 nM。
靶點

IC50: 8 nM (CB1 receptor)

體外研究

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.

體內(nèi)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).

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