Chlorpromazine HCl
(Synonyms: 盐酸氯丙嗪) 目录号 : GC14216
A typical antipsychotic
Cas No.:69-09-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Hippocampus neurons |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
10 ~ 100 μM |
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Applications |
Chlorpromazine HCl at 10 ~ 100 μM dose-dependently decreased mIPSC amplitude. Besides, Chlorpromazine HCl significantly accelerated the decay of mIPSC at the concentrations ≥ 30 μM in a dose-dependent manner. However, there was no significant difference on the 10 ~ 90% rise time between the control group and the Chlorpromazine HCl treatment groups. |
| Animal experiment [2]: | |
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Animal models |
A rat model of hypoxia |
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Dosage form |
30 mg/kg; i.p. |
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Applications |
In a rat model of hypoxia, Chlorpromazine HCl reduced irreversible loss of synaptic transmission in brain tissues. Chlorpromazine HCl also significantly delayed the occurrence of the hypoxia-induced spreading depression in rats by slowing down the influx of Ca2+ into neurons. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Mozrzymas JW, Barberis A, Michalak K, Cherubini E. Chlorpromazine inhibits miniature GABAergic currents by reducing the binding and by increasing the unbinding rate of GABAA receptors. J Neurosci. 1999 Apr 1;19(7):2474-88. [2]. Balestrino M, Somjen GG. Chlorpromazine protects brain tissue in hypoxia by delaying spreading depression-mediated calcium influx. Brain Res. 1986 Oct 22;385(2):219-26. |
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Dopamine receptors are a class of G protein-coupled receptors that are prominent in the central nervous system. Dopamine receptors are implicated in many neurological processes. Thus, dopamine receptors are common neurologic drug targets. Antipsychotics are often dopamine receptor antagonists while typically psychostimulants are indirect agonists of dopamine receptors. Chlorpromazine is a dopamine antagonist.
In vitro: The antipsychotic activity of chlorpromazine has been associated with its ability to act as a dopamine-receptor antagonist. the manner in which chlorpromazine, with its phenothiazine ring structure, interacted with a receptor for dopamine. Furthermore, chlorpromazine inhibited the binding of [3H]spiperone, and the inhibition curve was consistent with a single class of binding sites [1].
In vivo: Daily administration of chlorpromazine to rats for 21 days induced catalepsy, tolerance to catalepsy and locomotor sensitization following PCP challenge. Results suggest that daily chlorpromazine treatment induced DA/NMDA-receptor sensitization to total locomotor activity following PCP challenge [2].
Clinical trial: Chlorpromazine is clinical used as a conventional antipsychotic drug that has been used for the management of psychotic disorders since its FDA approval in 1954.
多巴胺受体是一类突出在中枢神经系统中的G蛋白偶联受体。多巴胺受体涉及许多神经系统过程，因此成为常见的神经药物靶点。抗精神病药通常是多巴胺受体拮抗剂，而通常的精神刺激剂是多巴胺受体间接激动剂。氯丙嗪是一种多巴胺受体拮抗剂。
体外实验：氯丙嗪的抗精神病活性与其作为多巴胺受体拮抗剂的能力有关。氯丙嗪的苯并噻唑环结构与多巴胺受体相互作用的方式已被研究。此外，氯丙嗪抑制了[3H]斯匹隆的结合，抑制曲线与单类结合位点一致[1]。
体内实验：将氯丙嗪每日给予大鼠21天后，诱导了强直、对强直的耐受性和PCP挑战后的运动感受性增强。结果表明，每日氯丙嗪治疗引起了DA/NMDA受体对PCP挑战后总运动活动的敏感性增强[2]。
临床试验：氯丙嗪是一种传统的抗精神病药物，自1954年获得FDA批准以来，一直被用于治疗精神疾病的管理。
Reference:
[1] Harrold MW, Chang YA, Wallace RA, Farooqui T, Wallace LJ, Uretsky N, Miller DD. Charged analogues of chlorpromazine as dopamine antagonists. J Med Chem. 1987 Sep;30(9):1631-5.
[2] Nsimba SE. Effects of daily chlorpromazine administration on behavioural and physiological parameters in the rat. Indian J Physiol Pharmacol. 2009 Jul-Sep;53(3):209-18.
| Cas No. | 69-09-0 | SDF | |
| 别名 | 盐酸氯丙嗪 | ||
| 化学名 | 3-(2-chlorophenothiazin-10-yl)-N,N-dimethylpropan-1-amine;hydrochloride | ||
| Canonical SMILES | CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl.Cl | ||
| 分子式 | C17H19ClN2S.HCl | 分子量 | 355.33 |
| 溶解度 | ≥ 17.8 mg/mL in DMSO, ≥ 74.8 mg/mL in EtOH, ≥ 71.4 mg/mL in Water | 储存条件 | Store at RT,protect from light,unstable in solution, ready to use. |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8143 mL | 14.0714 mL | 28.1429 mL |
| 5 mM | 0.5629 mL | 2.8143 mL | 5.6286 mL |
| 10 mM | 0.2814 mL | 1.4071 mL | 2.8143 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。