| CAS NO: | 202463-68-1 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 557.22 |
| Cas No. | 202463-68-1 |
| Formula | C21H19Cl2IN4O2 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥1.86 mg/mL in DMSO with gentle warming and ultrasonic |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。 |
AM 281是一种强效的和选择性的CB1大麻素受体拮抗剂/反相激动剂,作用于CB1和CB2受体的Ki值分别为12和4200 nM [1].
CB1大麻素受体是一种G蛋白偶联受体,主要在大脑中表达.大麻素受体在记忆\情绪\食欲和疼痛感觉中起重要作用.
AM 281是一种强效的和选择性的CB1大麻素受体拮抗剂/反相激动剂.在大鼠前脑膜中,AM281对CB1受体表现出高亲和力,Ki值为12 nM.在小鼠脾膜中,AM281对CB2受体表现出很低的亲和力,Ki值为4200 nM [1].在小鼠小脑匀浆中,当与SR141716A\CP55,940\WIN55\212-2\THC和methanandamide竞争时,AM281对CB 1受体表现出亲和力,Ki值分别为1.8\2.8\84\208和2512 nM [2].
在吗啡戒断小鼠中,AM281(2.5 mg/kg)显著改善吗啡戒断引起的记忆障碍[3].
参考文献：
[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.
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