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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

用途

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。

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名称

[ CAS 号 ]:
202463-68-1

[ 中文名 ]:
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

[ 英文名 ]:
AM281

[中文别名 ]:

[英文别名 ]:

AM 281
Tocris-1115
S1595_Selleck
MFCD01861180

生物活性

[ 描述 ]:

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。

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 大麻素受体

[ 靶点 ]

CB1:9.91 nM (IC50)

CB2:13000 nM (IC50)

[体外研究]

AM281(0.01-10μM)促进10μM aβ25-35诱导的SH-SY5Y细胞神经毒性的浓度依赖性增加(在10μM KSO 1-6存在下)[2]。

[体内研究]

急性给药(2.5、5和10 mg/kg)AM281缩短了探索时间,改善了记忆力,慢性服用AM281(0.62、1.25和2.5 mg/kg)也同样如此[3]。与对照组(4.8±2.5)相比,长期服用2.5 mg/kg的AM281可使识别指数提高到22.1±4.8,单剂量5 mg/kg的AM281可使记忆障碍改善至8.5±4。以2.5 mg/kg剂量(慢性)和5 mg/kg(急性剂量)给药AM281可改善记忆力[3]。动物模型：雄性NMRI小鼠,体重25-30g[3]剂量：0.62,1.25,2.5mg/kg(慢性给药)；2.5,5,10mg/kg(急性给药)：除实验当天(慢性给药)外,每天静脉注射吗啡；结果：与吗啡依赖小鼠相比,AM281与吗啡同时给药可显著缩短小鼠的探索时间。急性给药5mg/kg,可显著增强识别指数。

[参考文献]

[1]. K S S Dossou, et al. Development and preliminary validation of a plate-based CB1/CB2 receptor functional assay. Anal Biochem. 2013 Jun 15;437(2):138-43.

[2]. Milton, NG, et al. Effects of the CB1 cannabinoid receptor antagonist AM281 on kissorphin protection against amyloid-β neurotoxicity.

[3]. G Vaseghi, et al. The effect of AM281, a cannabinoid antagonist, on memory performance during spontaneous morphine withdrawal in mice. Res Pharm Sci. 2013 Jan;8(1):59-64.

物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 分子式 ]:
C₂₁H₁₉Cl₂IN₄O₂

[ 分子量 ]:
557.212

[ 精确质量 ]:
555.992981

[ PSA ]:
59.39000

[ LogP ]:
4.90

[ 外观性状 ]:
白色至灰白色固体

[ 折射率 ]:
1.706

[ 储存条件 ]:
2-8C

安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H315-H319-H335

[ 警示性声明 ]:
P261-P264-P301 + P310-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
26-36/37/39-45

[ 危险品运输编码 ]:
UN 2811 6

文献

Cannabinoid agonists rearrange synaptic vesicles at excitatory synapses and depress motoneuron activity in vivo.

Neuropharmacology 92 , 69-79, (2015)

Impairment of motor skills is one of the most common acute adverse effects of cannabis. Related studies have focused mainly on psychomotor alterations, and little is known about the direct impact of c...

Activation of CB2 receptor is required for the therapeutic effect of ABHD6 inhibition in experimental autoimmune encephalomyelitis.

Neuropharmacology 99 , 196-209, (2015)

Alpha/beta-hydrolase domain 6 (ABHD6) is a novel 2-arachidonoylglycerol (2-AG) hydrolytic enzyme, that can fine-tune the endocannabinoid signaling in the central nervous system. Recently we and others...

Cannabinoid receptor 1 inhibition improves the intestinal microcirculation in experimental endotoxemia.

Clin. Hemorheol. Microcirc. 58(2) , 333-42, (2014)

Impairment of the intestinal microcirculation in endotoxemia may cause a deterioration of the mucosal barrier function thus releasing intraluminal bacteria and their toxins into the systemic circulati...

更多文献

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

用途

名称

生物活性

物理化学性质

安全信息

文献

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