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202463-68-1

中文名称 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
英文名称 1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-4-MORPHOLINYL-1H-PYRAZOLE-3-CARBOXAMIDE
CAS 202463-68-1
分子式 C21H19Cl2IN4O2
分子量 557.21
MOL 文件 202463-68-1.mol
更新日期 2024/07/21 13:45:15
202463-68-1 结构式 202463-68-1 结构式

基本信息

中文别名
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
1-(2,4-二氯苯)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺
1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺
英文别名
AM 281
CS-1127
AM-281 ,99%
AM281
AM-281
1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholin-4-ylpyrazole-3-carboxamide
1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-4-MORPHOLINYL-1H-PYRAZOLE-3-CARBOXAMIDE
1H-Pyrazole-3-carboxamide,1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-
1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide AM 281
所属类别
生物化工:激动剂抑制剂

物理化学性质

储存条件2-8°C
储存条件2-8°C
溶解度DMSO: >6 mg/mL
溶解度二甲基亚砜:>6 mg/mL
形态solid
颜色white

安全数据

危险性符号(GHS)
GHS06
警示词危险
危险性描述H300-H315-H319-H335
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
危险品运输编号UN 2811 6.1/PG 3
WGK Germany3
WGK Germany3

常见问题列表

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.
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