Clorgyline (hydrochloride)
(Synonyms: 盐酸氯吉林) 目录号 : GC14122
Clorgyline (hydrochloride)是一种不可逆、强效和选择性单胺氧化酶（MAO）A 抑制剂，对MAO-A和MAO-B的Ki值分别为0.054和58μM，IC50值分别为 0.0012和1.9μM。
Cas No.:17780-75-5
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Clorgyline (hydrochloride) is an irreversible, potent and selective inhibitor of monoamine oxidase (MAO) A, with Ki values of 0.054 and 58μM for MAO-A and MAO-B, and IC50 values of 0.0012 and 1.9μM, respectively[1, 2]. MAO is responsible for the regulation and metabolism of major monoamine neurotransmitters such as serotonin (5-HT), norepinephrine (NE) and dopamine (DA)[3]. Clorgyline (hydrochloride) has little effect on the content of conjugated dopamine in rat striatal slices[4].
In vivo, Clorgyline (hydrochloride) (1.5mg/kg/day) was intraperitoneally injected into Huntington's disease mice for 21 days, which inhibited the activity of monoamine oxidase A (MAO-A) in the cortical tissue of mice by about 90%, significantly increased the levels of neurotransmitters 5-HT and NE in the striatum, improved anxiety-like phenotypes, and reduced depressive-like behaviors[5]. Treatment of rats with Clorgyline (hydrochloride) (2mg/kg/day) for 28 days increased the rats' nicotine intake[6].
References:
[1] Rullo M, La Spada G, Catto M, et al. Monoamine Oxidase Inhibition for the Treatment of Neurodegenerative Diseases: Rationale, Assay Methodologies, and Reference Compounds[M]//Methods in Neurodegenerative Disease Drug Discovery. New York, NY: Springer US, 2024: 137-150.
[2] Abdelhafez O M, Amin K M, Ali H I, et al. Synthesis of new 7-oxycoumarin derivatives as potent and selective monoamine oxidase A inhibitors[J]. Journal of Medicinal Chemistry, 2012, 55(23): 10424-10436.
[3] Naoi M, Maruyama W, Shamoto-Nagai M. Type A monoamine oxidase and serotonin are coordinately involved in depressive disorders: from neurotransmitter imbalance to impaired neurogenesis[J]. Journal of Neural Transmission, 2018, 125: 53-66.
[4] Tyce G M, Rorie D K. Conjugated dopamine in superfusates of slices of rat striatum[J]. Journal of Neurochemistry, 1982, 39(5): 1333-1339.
[5] Garcia-Miralles M, Ooi J, Bardile C F, et al. Treatment with the MAO-A inhibitor clorgyline elevates monoamine neurotransmitter levels and improves affective phenotypes in a mouse model of Huntington disease[J]. Experimental neurology, 2016, 278: 4-10.
[6] Guillem K, Vouillac C, Azar M R, et al. Monoamine oxidase A rather than monoamine oxidase B inhibition increases nicotine reinforcement in rats[J]. European Journal of Neuroscience, 2006, 24(12): 3532-3540.
Clorgyline (hydrochloride)是一种不可逆、强效和选择性单胺氧化酶（MAO）A 抑制剂，对MAO-A和MAO-B的Ki值分别为0.054和58μM，IC50值分别为 0.0012和1.9μM[1, 2]。MAO负责主要单胺神经递质如5-羟色胺（5-HT）、去甲肾上腺素（NE）和多巴胺（DA）的调节和代谢[3]。Clorgyline (hydrochloride)对大鼠纹状体切片中共轭多巴胺的含量影响不大[4]。
在体内，Clorgyline (hydrochloride)（1.5mg/kg/day）通过腹腔注射治疗亨廷顿病小鼠21天，抑制了小鼠皮质组织中单胺氧化酶A（MAO-A）的活性约90%，显著升高了纹状体内神经递质5-HT和NE水平，改善了焦虑样表型，减少了抑郁样行为[5]。Clorgyline (hydrochloride)（2mg/kg/day）处理大鼠28天，增加了大鼠对尼古丁的摄入量[6]。
| Animal experiment [1]: | |
Animal models | Three-month-old male FVB/N mice、four-month-old YAC128 HD and littermate wild-type mice |
Preparation Method | For the Clorgyline (hydrochloride) dosing study, 3 month old WT mice were divided into four groups of 10 mice each. Three groups received Clorgyline (hydrochloride) at a dose of 0.5, 1.5, or 3mg/kg and the fourth group received an equivalent volume of PBS. For the YAC128 treatment study, three independent cohorts of 4 month old mice were used, giving a total of 17-22 mice per treatment/group. For each cohort, mice were divided into three groups. One group of YAC128 HD mice received Clorgyline (hydrochloride) at a dose of 1.5mg/kg and two groups, one of WT mice and another one of YAC128 HD mice, received an equivalent volume of PBS. Treatments were administered daily before noon at a volume of 10mL/kg i.p. for 21 days and were continued throughout the behavioural testing phase, which commenced on day 22. During the behavioural testing phase, mice were treated in the afternoon following completion of the corresponding behavioural test. Mice were sacrificed once the behavioural testing was finished at day 26 or 28. |
Dosage form | 1.5mg/kg/day; 21 days; i.p. |
Applications | In wild-type mice, Clorgyline (hydrochloride) significantly inhibited Monoamine oxidases A (MAO-A) enzymatic activity by approximately 80%. Clorgyline (hydrochloride) also significantly elevated striatal levels of 5-HT and NE, and significantly decreased 3,4-Dihydroxyphenylacetic acid (DOPAC) levels, suggesting that inhibition of MAO-A activity decreased the metabolism of dopamine (DA). In YAC128 HD mice, Clorgyline (hydrochloride) inhibited MAO-A enzymatic activity in cortical tissue by approximately 90% and significantly elevated striatal 5-HT and NE levels. Clorgyline (hydrochloride) treatment also improved anxiety-like phenotypes and reduced depressive-like behavior. |
References: | |
| Cas No. | 17780-75-5 | SDF | |
| 别名 | 盐酸氯吉林 | ||
| 化学名 | 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 | ||
| 分子式 | C13H15Cl2NO • HCl | 分子量 | 308.6 |
| 溶解度 | ≥ 17.65mg/mL in DMSO, 120 mg/mL in H2O (388.82 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2404 mL | 16.2022 mL | 32.4044 mL |
| 5 mM | 0.6481 mL | 3.2404 mL | 6.4809 mL |
| 10 mM | 0.324 mL | 1.6202 mL | 3.2404 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet