CGP 36216 hydrochloride
目录号 : GC13676
Selective GABAB antagonist
Cas No.:123691-29-2
Sample solution is provided at 25 µL, 10mM.
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CGP 36216 hydrochloride is a potent and selective antagonist of GABAB receptors with IC50 value of 43 µM.
GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) and are linked through G-proteins to potassium channels. Expression of GABAB receptors are found in the central as well as in the autonomic division of the peripheral nervous system. GABAB receptors play a key role in regulating membrane excitability and synaptic transmission in the brain.
In rat neocortical preparations maintained in Mg2+-free Krebs medium, CGP 36216 acts as antagonism of baclofen-induced suppression of spontaneous discharges in a concentration-dependent manner. However, CGP 36216, up to 1 mM, was ineffective in antagonising baclofen-induced hyperpolarisations, mediated through gamma-aminobutyric acid (B) GABAB postsynaptic receptors 1.
In electrically stimulated brain slices preloaded with [3H] GABA, CGP 36216 increased the release of [3H] GABA, that was reversed by baclofen. While CGP 36216 is ineffective at GABAB postsynaptic receptors, it is appreciably more active at presynaptic receptors1.
Reference:
1. Ong J, Bexis S, Marino V, et al. CGP 36216 is a selective antagonist at GABA(B) presynaptic receptors in rat brain. European journal of pharmacology. 2001;415(2-3):191-195.
| Cas No. | 123691-29-2 | SDF | |
| 化学名 | (3-aminopropyl)(ethyl)phosphinic acid hydrochloride | ||
| Canonical SMILES | CCP(CCCN)(O)=O.Cl | ||
| 分子式 | C5H14NO2P.HCl | 分子量 | 187.6 |
| 溶解度 | <18.76mg/ml in DMSO; <18.76mg/ml in Water | 储存条件 | Desiccate at RT |
| 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 | 5.3305 mL | 26.6525 mL | 53.3049 mL |
| 5 mM | 1.0661 mL | 5.3305 mL | 10.661 mL |
| 10 mM | 0.533 mL | 2.6652 mL | 5.3305 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