Pardoprunox hydrochloride (SLV-308 hydrochloride)
(Synonyms: 盐酸帕多芦诺,SLV-308 hydrochloride; DU-126891 hydrochloride) 目录号 : GC30980
A dopamine D2 and D3 receptor partial agonist and 5-HT1A agonist
Cas No.:269718-83-4
Sample solution is provided at 25 µL, 10mM.
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Pardoprunox is a partial agonist of dopamine D2 and D3 receptors (EC50s = 10 and 0.63 nM, respectively) and a full agonist of the serotonin (5-HT) receptor subtype 5-HT1A (EC50 = 501 nM) in radioligand binding assays.1 It is selective for dopamine D2 and D3 and 5-HT1A receptors over a panel of neurotransmitter receptors (Kis = >1,000 nM). Pardoprunox reduces the accumulation of cAMP induced by forskolin in a concentration-dependent manner and blocks quinpirole-induced inhibition of dopamine release (pA2 = 8.5) in rat striatal slices. Pardoprunox increases contralateral turning behavior in a 6-OHDA rat model of Parkinson’s disease (ED50 = 0.03 mg/kg).2 It also reduces hyperlocomotion induced by amphetamine and induces 5-HT1A-mediated flat body posturing and lower lip retraction in rats. Pardoprunox (0.01-0.3 mg/kg) increases locomotor activity in a marmoset model of Parkinson’s disease induced by MPTP in a dose-dependent manner. Formulations containing pardoprunox are under clinical investigation for the treatment of Parkinson’s disease-associated motor fluctuations.3
1.Glennon, J.C., Van Scharrenburg, G., Ronken, E., et al.In vitro characterization of SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone, monohydrochloride): A novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonistSynapse60(8)599-608(2006) 2.Jones, C.A., Johnston, L.C., Jackson, M.J., et al.An in vivo pharmacological evaluation of pardoprunox (SLV308)—A novel combined dopamine D2/D3 receptor partial agonist and 5-HT1A receptor agonist with efficacy in experimental models of Parkinson's diseaseEur. Neuropsychopharmacol.20(8)582-593(2010) 3.Rascol, O., Brozova, J., Hauser, R.A., et al.Pardoprunox as adjunct therapy to levodopa in patients with Parkinson's disease experiencing motor fluctuations: Results of a double-blind, randomized, placebo-controlled, trialParkinsonism Relat. Disord.18(4)370-376(2012)
| Cas No. | 269718-83-4 | SDF | |
| 别名 | 盐酸帕多芦诺,SLV-308 hydrochloride; DU-126891 hydrochloride | ||
| Canonical SMILES | O=C1OC2=C(N3CCN(C)CC3)C=CC=C2N1.[H]Cl | ||
| 分子式 | C12H16ClN3O2 | 分子量 | 269.73 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 5 mg/ml,Ethanol: 0.1 mg/ml,PBS (pH 7.2): 5 mg/ml | 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 | 3.7074 mL | 18.5371 mL | 37.0741 mL |
| 5 mM | 0.7415 mL | 3.7074 mL | 7.4148 mL |
| 10 mM | 0.3707 mL | 1.8537 mL | 3.7074 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