去甲槟榔次碱
中文名称 | 去甲槟榔次碱 |
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中文同义词 | 去甲槟榔次碱盐酸盐;甲槟榔次碱盐酸盐 |
英文名称 | GUVACINE HYDROCHLORIDE |
英文同义词 | GUVACINE HYDROCHLORIDE >96% \ GABA UPTAK;1,2,5,6-Tetrahydro-;1,2,5,6-Tetrahydro-3-pyridinecarboxylic Acid Hydrochloride;3-Pyridinecarboxylic acid, 1,2,5,6-tetrahydro-, hydrochloride;Guvacine hydrochloride >=97% (NMR), solid;GUVACINE HYDROCHLORIDE;Norareca alkaloid hydrochloride |
CAS号 | 6027-91-4 |
分子式 | C6H10ClNO2 |
分子量 | 163.6021 |
EINECS号 | |
相关类别 | 中药对照品;化工原料;GABA and Glycine Receptor ModulatorsNeurotransmitters;GABAergics;Ion Channels;Ligand-Gated Ion Channels;Others;Amines;Heterocycles;Intermediates & Fine Chemicals;Nicotine Derivatives;Pharmaceuticals |
Mol文件 | 6027-91-4.mol |
结构式 |
去甲槟榔次碱 性质
熔点 | 316 °C (decomp) |
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储存条件 | Inert atmosphere,Room Temperature |
溶解度 | 在水中可溶 |
形态 | 固体 |
颜色 | 白色 |
IC50: 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), 1870 μM (human BGT-3)
Guvacine hydrochloride is a potent inhibitor of GABA transporter, dispalys modest selectivity for cloned GABA transporters with IC 50 s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3). Guvacine has low affinity at hBGT-1 (IC 50 >1 mM). Guvacine hydrochloride is a potent inhibitor of GABA uptake, but does not inhibit sodium-independent GABA binding, and is weak or inactive as a GABA receptor agonist. Guvacine inhibits the uptake GABA and β-alanine with IC 50 s of 23 ± 2 μM, 66 ± 11 μM in the Cat spinal cord, and 8 ± 1 μM, 123 ± 28 μM in the rat cerebral cortex, respectively.