Clocapramine (Clocarpramine)
(Synonyms: Clocarpramine; 3-Chlorocarpipramine) 目录号 : GC31037
Clocapramine是多巴胺D2和5-HT2A受体拮抗剂。
Cas No.:47739-98-0
Sample solution is provided at 25 µL, 10mM.
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Clocapramine is an antagonist of the D2, 5-HT2A receptors.
Clocapramine has a moderate affinity for D2-receptors in vitro. Clocapramine shows higher affinity for 5-HT2A than for D2-receptors in vitro[1].
Clocapramine shows the lowest potency for D2-occupancy in vivo[1]. An in vivo receptor binding technique is used to evaluate the binding profiles of typical and atypical antipsychotic drugs to striatal dopamine-D2 and frontal serotonin-5-HT2 receptors in a rat brain using more specific ligands. Clocapramine produces ratios of potency in occupying 5-HT2 versus D2 receptors that fall between these two groups (ED50 of 14.5 mg/kg for D2, 4.9 mg/kg for 5-HT2)[2].
[1]. Schotte A, et al. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used. Jpn J Pharmacol. 1995 Dec;69(4):399-412. [2]. Sumiyoshi T, et al. Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy. Neuropsychopharmacology. 1995 Feb;12(1):57-64.
Animal experiment: | Rats[2] Male Wistar rats (210 to 240 g) are housed in a temperature-controlled room with a 12-hour dark/light cycle (lights on at 8:30) and have free access to food and water. For competition studies, rats are pretreated with an intraperitoneal injection of varying doses of antipsychotic drugs or the same volume (0.21 to 0.24 mL) of the corresponding vehicle (DMSO), 10 minutes prior to the injection of [3H]-YM-09151-2 or [3H]-ketanserin. |
References: [1]. Schotte A, et al. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used. Jpn J Pharmacol. 1995 Dec;69(4):399-412. | |
| Cas No. | 47739-98-0 | SDF | |
| 别名 | Clocarpramine; 3-Chlorocarpipramine | ||
| Canonical SMILES | O=C(C1(N2CCCCC2)CCN(CCCN3C4=CC(Cl)=CC=C4CCC5=CC=CC=C53)CC1)N | ||
| 分子式 | C28H37ClN4O | 分子量 | 481.07 |
| 溶解度 | Soluble in DMSO | 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。 |
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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 | 2.0787 mL | 10.3935 mL | 20.787 mL |
| 5 mM | 0.4157 mL | 2.0787 mL | 4.1574 mL |
| 10 mM | 0.2079 mL | 1.0393 mL | 2.0787 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet