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AM630

 
Catalog No.
A3168
CB2受体拮抗剂
组合的产品项目
规格价格库存 数量
5mg
¥ 772.00
Ship with 10-15 days
10mg
¥ 1,363.00
Ship with 10-15 days
50mg
¥ 5,181.00
Ship with 10-15 days

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A

背景

AM630是一种选择性的和竞争性的大麻素受体拮抗剂,作用于CB1受体和CB2受体,Ki值分别为5 μM和31.2 nM[1]。

在转染CB1的CHO细胞中,AM630显著抑制毛喉素刺激的cAMP的产生。在转染CB2的细胞中,AM630促进毛喉素刺激的cAMP的产生,EC50值为230.4 nM。AM630也抑制GTPγS与转染CB2细胞的细胞膜的结合。此外,在TG感觉神经元中,AM630可激活TRPA1通道,随后使TRPA1和TRPV1通道脱敏。而且,在WT小鼠中,AM630显著减弱辣椒素(CAP)诱导的热痛觉过敏[1,2]。

参考文献:
1.  Ross R A, Brockie H C, Stevenson L A, et al. Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630. British journal of pharmacology, 1999, 126(3): 665-672.
2.  Patil M, Patwardhan A, Salas M M, et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology, 2011, 61(4): 778-788.

文献引用

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt504.36
Cas No.164178-33-0
FormulaC23H25IN2O3
SynonymsAM 630;AM-630
Solubility≥25.2 mg/mL in DMSO; insoluble in H2O; ≥2.53 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name[6-iodo-2-methyl-1-(2-morpholin-4-ylethyl)indol-3-yl]-(4-methoxyphenyl)methanone
SDFDownload SDF
Canonical SMILESCC1=C(C2=C(N1CCN3CCOCC3)C=C(C=C2)I)C(=O)C4=CC=C(C=C4)OC
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

试验操作

Cell experiment:[1]

Cell lines

Trigeminal ganglia (TG) sensory neurons

Reaction Conditions

10 μM AM630 for 3 min incubation

Applications

The application of cannabinoid receptor antagonist AM630 (10 μM) activated a robust Ca2+ accumulation in a subset (35 ~ 40%) of TG neurons. The AM630-evoked Ca2+ influxes into TG sensory neurons were concentration-dependent, with an EC50 value being 15.6 μM.

Animal experiment:[2]

Animal models

Swiss ICR mice

Dosage form

1, 2 or 3 mg/kg

Administered intraperitoneally twice a day for 7 days

Applications

Chronic AM630 treatment alleviated anxiety-like behaviors in the light-dark box and elevated plus maze tests. Meanwhile, chronic AM630 treatment increased gene and reduced protein expression of CB2 receptors, GABAAα2 and GABAAγ2 in cortex and amygdala.

Note

The technical data provided above is for reference only.

References:

1. Patil M, Patwardhan A, Salas MM, et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology, 2011, 61(4): 778-788.

2. García-Gutiérrez MS, García-Bueno B, Zoppi S, et al. Chronic blockade of cannabinoid CB2 receptors induces anxiolytic-like actions associated with alterations in GABA(A) receptors. British Journal of Pharmacology, 2012, 165(4): 951-964.

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