MDL 72832 hydrochloride
目录号 : GC10985
ligand for 5-HT1A receptor, potent and selective
Cas No.:113777-40-5
Sample solution is provided at 25 µL, 10mM.
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MDL 72832 hydrochloride is a potent and selective ligand for 5-HT1A receptor with pIC50 value of 9.1 [1].
The 5-HT1A receptor is a G protein-coupled receptor for endogenous neurotransmitter serotonin (5-HT) and mediates inhibitory neurotransmission.
MDL 72832 hydrochloride is a potent and selective ligand for 5-HT1A receptor [1]. Also, MDL 72832 exhibited affinity with pKD values of 6.32 and 6.34 for 5-HT1C and 5-HT1D receptors, respectively [1].
In rats, MDL 72832 inhibited 8-OH-DPAT-induced cardiovascular effects. In guinea-pigs, 8-OH-DPAT inhibited the contraction of the field-stimulated guinea-pig ileum in a concentration-dependent way. While MDL 72832 inhibited 8-OH-DPAT-induced neuronal inhibition. MDL 72832 is a ligand for 5-HT1A receptor with mixed antagonist and agonist properties [1]. In pre-satiated rats, (+) -MDL 72832 (1.0 mg/kg) stimulated food intake and (-) -MDL 72832 (0.03 mg/kg) significantly increased food intake [2]. In rats, MDL 72832 increased postsynaptic 5-HT1A receptors mediating hypothermia and exhibited agonist property [3].
References:
[1]. Mir AK, Hibert M, Tricklebank MD, et al. MDL 72832: a potent and stereoselective ligand at central and peripheral 5-HT1A receptors. Eur J Pharmacol, 1988, 149(1-2): 107-120.
[2]. Neill JC, Cooper SJ. MDL 72832, a selective 5-HT1A receptor ligand, stereospecifically increases food intake. Eur J Pharmacol, 1988, 151(2): 329-332.
[3]. Millan MJ, Rivet JM, Canton H, et al. Induction of hypothermia as a model of 5-hydroxytryptamine1A receptor-mediated activity in the rat: a pharmacological characterization of the actions of novel agonists and antagonists. J Pharmacol Exp Ther, 1993, 264(3): 1364-1376.
| Cas No. | 113777-40-5 | SDF | |
| 化学名 | 8-(4-(((2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methyl)amino)butyl)-8-azaspiro[4.5]decane-7,9-dione hydrochloride | ||
| Canonical SMILES | O=C(N1CCCCNCC2COC3=CC=CC=C3O2)CC4(CC1=O)CCCC4.Cl | ||
| 分子式 | C22H30N2O4.HCl | 分子量 | 422.95 |
| 溶解度 | Soluble to 5 mM in Water | 储存条件 | Store 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 | 2.3643 mL | 11.8217 mL | 23.6435 mL |
| 5 mM | 0.4729 mL | 2.3643 mL | 4.7287 mL |
| 10 mM | 0.2364 mL | 1.1822 mL | 2.3643 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