CAS NO: | 17780-75-5 |
包装 | 价格(元) |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Storage | Store at -20°C |
M.Wt | 308.6 |
Cas No. | 17780-75-5 |
Formula | C13H15Cl2NO·HCl |
Synonyms | N-2,4-Dichlorophenoxypropyl-N-methylpropargylamine |
Solubility | ≥17.65 mg/mL in DMSO; ≥18.2 mg/mL in EtOH; ≥24.8 mg/mL in H2O |
Chemical Name | N-[3-(2,4-dichlorophenoxy)propyl]-N-methyl-2-propyn-1-amine, monohydrochloride |
Canonical SMILES | ClC1=CC=C(OCCCN(C)CC#C)C(Cl)=C1.Cl |
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。 |
Clorgyline (hydrochloride) is an irreversible, potent and selective monoamine oxidase (MAO) A inhibitor with Ki values of 0.054 and 58 μM and IC50 values of 0.0012 and 1.9 μM for MAO-A and MAO-B, respectively [1][2].
Monoamine oxidases (MAOs) are FAD depending enzymes and exists in two forms, namely MAO-A and MAO-B. MAOs are responsible for the regulation and metabolism of major monoamine neurotransmitters such as 5-hydroxytryptamine (5-HT), norepinephrine (NE), and dopamine (DA). MAO-A preferentially oxidizes serotonin. Human MAO-A inhibitors are antidepressants and antianxiety agents [1].
Clorgyline is an irreversible, potent and selective MAO-A inhibitor. In wild-type mice, clorgyline significantly inhibited MAO-A enzymatic activity by approximately 80%. Clorgyline also significantly elevated striatal levels of 5-HT and NE, and significantly decreased DOPAC levels, suggesting that inhibition of MAO-A activity decreased the metabolism of DA. In YAC128 HD mice, clorgyline (1.5 mg/kg for 21 days) inhibited MAO-A enzymatic activity in cortical tissue by approximately 90% and significantly elevated striatal 5-HT and NE levels. Clorgyline treatment also improved anxiety-like phenotypes and reduced depressive-like behavior [3].
References:
[1]. Abdelhafez OM, Amin KM, Ali HI, et al. Synthesis of new 7-oxycoumarin derivatives as potent and selective monoamine oxidase A inhibitors. J Med Chem. 2012 Dec 13;55(23):10424-36.
[2]. Mazouz F, Gueddari S, Burstein C, et al. 5-[4-(benzyloxy)phenyl]-1,3,4-oxadiazol-2(3H)-one derivatives and related analogues: new reversible, highly potent, and selective monamine oxidase type B inhibitors. J Med Chem. 1993 Apr 30;36(9):1157-67.
[3]. Garcia-Miralles M, Ooi J, Ferrari Bardile C, et al. Treatment with the MAO-A inhibitor clorgyline elevates monoamine neurotransmitter levels and improves affective phenotypes in a mouse model of Huntington disease. Exp Neurol. 2016 Apr;278:4-10.