AM 281
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
- 1. Lin Ye, Shuhao Li, et al. "CB1R Promotes Chronic Alcohol-Induced Neuronal Necroptosis in Mice Prefrontal Cortex." Alcohol Alcohol. 2021 Feb 24;56(2):230-239. PMID:33382401
- 2. Dingang Zhang, Xiaochen Liu, et al. "Cannabinoid 1 receptor (CB1R) antagonists play a neuroprotective role in chronic alcoholic hippocampal injury related to pyroptosis pathway." Alcohol Clin Exp Res. 2020 Aug;44(8):1585-1597. PMID:32524615
- 2. Li L, Dong X, et al. "Opposite effects of cannabinoid CB(1) and CB(2) receptors on antipsychotic clozapine-induced cardiotoxicity." Br J Pharmacol. 2019 Feb 1. PMID:30707759
| 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 |
| SDF | Download SDF |
| 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 | 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。 |
质量控制和MSDS
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