1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-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-吗啉-1H-吡唑-3-甲酰胺试剂级价格

CAS号:202463-68-1
英文名:1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-4-MORPHOLINYL-1H-PYRAZOLE-3-CARBOXAMIDE
中文名:1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-1H-吡唑-3-甲酰胺
CBNumber:CB9297436
分子式:C21H19Cl2IN4O2
分子量:557.21
MOL File:202463-68-1.mol

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

密度 :1.70±0.1 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMSO: >6 mg/mL
形态 :solid
酸度系数(pKa) :10.76±0.20(Predicted)
颜色 :white

安全信息

危险品标志 :T
危险类别码 :25-36/37/38
安全说明 :26-36/37/39-45
危险品运输编号 :UN 2811 6.1/PG 3
WGK Germany :3

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

生物活性 AM281 是一种选择性 CB1 受体拮抗剂，IC50 为 9.91 nM。AM281 抑制 CB2 受体，IC50 为 13000 nM。
靶点

CB1

9.91 nM (IC ₅₀ )

CB2

13000 nM (IC ₅₀ )
体外研究

AM281 (0.01-10 μM) promotes a concentration dependent increase in 10 μM Aβ 25-35 induced neurotoxicity in SH-SY5Y cells in the presence of 10 μM KSO 1-6.

体内研究

Acute administration (2.5, 5 and 10 mg/kg) of AM281 shortens exploration time and improves memory performance, as does chronic administration (0.62, 1.25 and 2.5 mg/kg) of AM281.
Chronic administration of AM281 at 2.5 mg/kg improves recognition index to the 22.1±4.8 and single dose of AM281 at 5 mg/kg improves the memory impairment to the 8.5±4, as compared with vehicle-treated which is 4.8±2.5. Administration of AM281 at a dose of 2.5 mg/kg in chronic form and 5 mg/kg in acute dose improve memory.

Animal Model:	Male NMRI mice with the weight of 25-30 g
Dosage:	0.62, 1.25 and 2.5 mg/kg (chronic administration); 2.5, 5 and 10 mg/kg (acute administration)
Administration:	Administrated i.p. every day concurrently with morphine except the day of experiment (chronic administration); Singly injected 40 min before second trial (acute administration)
Result:	The simultaneous daily administration of AM281 with morphine significantly shortened the exploration time, as compared with morphine-dependent mice receiving vehicle. Acute administration at a dose of 5 mg/kg, significantly augmented recognition index.