Axon 2155
CAS [869802-58-4]
MF C17H21N5OSMW 343.45
Potent and selective non-competitive mGlu1 receptor antagonist (IC50: 10 nM); showing 34-fold selectivity over mGluR5 and no significant activity at other mGluR receptors, neurotransmitter receptors, ion channels, and transporters. A 841720 demonstrated full efficacy in various in vivo animal pain models.
KEYWORDS: A 841720 | supplier | mGluR1 antagonist | A841720 | A-841720 | CAS [869802-58-4] | Metabotropic | Glutamate | mGluR1 | mGlu1 | Antagonist | Receptors
GZ Zheng et al. Structure-Activity Relationship of Triazafluorenone Derivatives as Potent and Selective mGluR1 Antagonists. J. Med. Chem. 2005, 48, 7374-7388. |
O El-Kouhen et al. Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist. Br. J. Pharmacol. 2006, 149, 761-774. |
9-(Dimethylamino)-3-(hexahydro-1H-azepin-1-yl)-pyrido[3",2":4,5]thieno[3,2-d]pyrimidin-4(3H)-one
[869802-58-4]
Axon Medchem的业务之一,是独有的Axon Ligands配体库,在世界范围内,被认为是药物研发的标准。这其中,针对850余种生物靶标(包括细胞信号、基因转录、凋亡、细胞周期调控、CNS等),Axon Medchem拥有多达2000余种小分子抑制剂或调节剂。除了配体库,Axon Medchem还是欧洲著名的CRO公司,主要针对生物活性分子和药物类似分子展开合成及协议开发工作,在过去的10年中,Axon Medchem已经发现了多种潜在药物分子,并在生物医药界享有一定的声誉。