Axon 2401
CAS [1314801-63-2]
MF C15H21BrN2MW 309.24
High affinity and selective α3β4 nAChR ligand (Ki value 2.6 nM at α3β4 nAChR) with both partial agonistic and antagonistic effects, and >90-fold selective over the other major subtypes, the α4β2 and α7 nAChR. AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding, and shows a mechanism of action very different from varenicline (Axon 1384 (HCl salt) and Axon 2074 (tartrate salt)).
A. Cippitelli et al. AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. Br J Pharmacol. 2015 Apr;172(7):1834-45. |
L. Toll et al. AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats. Neuropsychopharmacology. 2012 May;37(6):1367-76. |
E.W. Tuan et al. AT-1001 is a Partial Agonist with High Affinity and Selectivity at Human and Rat α3β4 Nicotinic Cholinergic Receptors. Mol Pharmacol. 2015 Jul 10. pii: mol.115.099978. [Epub ahead of print] |
N-(2-bromophenyl)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine
[1314801-63-2]
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。