AM 281
(Synonyms: 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) 目录号 : GC16480
A CB1 receptor antagonist/inverse agonist
Cas No.:202463-68-1
Sample solution is provided at 25 µL, 10mM.
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AM 281 is a potent and selective antagonist/inverse agonist of CB1 cannabinoid receptor with Ki values of 12 and 4200 nM for CB1 and CB2 receptors, respectively [1].
CB1 cannabinoid receptor is a G protein-coupled receptor and is mainly expressed in the brain. Cannabinoid receptors play an important role in memory, mood, appetite and pain-sensation.
AM 281 is a potent and selective CB1 cannabinoid receptor antagonist/inverse agonist. In rat forebrain membranes, AM281 exhibited high affinity for CB1 receptor with Ki value of 12 nM. In mouse spleen membrane, AM281 exhibited very low affinity for CB2 receptor with Ki value of 4200 nM [1]. In mouse cerebellar homogenates, AM281 exhibited affinities for CB1 receptor with Ki values of 1.8, 2.8, 84, 208 and 2512 nM when competed with SR141716A, CP55,940, WIN 55,212-2, THC and methanandamide, respectively [2].
In morphine withdrawal mice, AM281 (2.5 mg/kg) significantly improved the memory impairment caused by morphine withdrawal [3].
References:
[1]. Lan R, Gatley J, Lu Q, et al. Design and synthesis of the CB1 selective cannabinoid antagonist AM281: a potential human SPECT ligand. AAPS PharmSci, 1999, 1(2): E4.
[2]. Gatley SJ, Lan R, Volkow ND, et al. Imaging the brain marijuana receptor: development of a radioligand that binds to cannabinoid CB1 receptors in vivo. J Neurochem, 1998, 70(1): 417-423.
[3]. Vaseghi G, Rabbani M, Hajhashemi V. The CB(1) receptor antagonist, AM281, improves recognition loss induced by naloxone in morphine withdrawal mice. Basic Clin Pharmacol Toxicol, 2012, 111(3): 161-165.
| Cas No. | 202463-68-1 | SDF | |
| 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 | ||
| 化学名 | 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholino-1H-pyrazole-3-carboxamide | ||
| Canonical SMILES | IC1=CC=C(C=C1)C2=C(C)C(C(NN3CCOCC3)=O)=NN2C(C(Cl)=C4)=CC=C4Cl | ||
| 分子式 | C21H19Cl2IN4O2 | 分子量 | 557.22 |
| 溶解度 | ≥ 1.86mg/mL in DMSO with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7946 mL | 8.9731 mL | 17.9462 mL |
| 5 mM | 0.3589 mL | 1.7946 mL | 3.5892 mL |
| 10 mM | 0.1795 mL | 0.8973 mL | 1.7946 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet