1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
  3. Pramipexole dihydrochloride hydrate

Pramipexole dihydrochloride hydrate 

目录号: HY-B0410A 纯度: >98.0%
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Pramipexole dihydrochloride hydrate 是一种选择性的 D2 型多巴胺受体 (dopamine receptor) 激动剂,对 D2 型受体、D2、D3、D4 亚型受体的 Ki 值分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM。 Pramipexole dihydrochloride hydrate 可用于帕金森综合症和腿多动综合征的研究。Pramipexole dihydrochloride hydrate 可以透过血脑屏障。

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Pramipexole dihydrochloride hydrate Chemical Structure

Pramipexole dihydrochloride hydrate Chemical Structure

CAS No. : 191217-81-9

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Description

Pramipexole dihydrochloride hydrate is a selective dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS). Pramipexole dihydrochloride hydrate can cross the blood-brain barrier (BBB)[1][2][3].

IC50 & Target[1]

D2 Receptor

3.9 nM (Ki)

D3 Receptor

0.5 nM (Ki)

D4 Receptor

1.3 nM (Ki)

D2-type receptors

2.2 nM (Ki)

In Vitro

Pramipexole dihydrochloride hydrate (0.01-10 μM; 72 hours) produces dose-dependent increases of dendritic arborization and soma size[3].
Pramipexole dihydrochloride hydrate attenuates levodopa-induced toxicity in mesencephalic cultures, suggests that pramipexole may be cytoprotective to dopamine neurons in tissue culture[4].

In Vivo

Pramipexole dihydrochloride hydrate (0.25-1 mg/kg; i.p.) significantly reduces the infarction volume in animals[5].
Pramipexole dihydrochloride hydrate improves neurological recovery[5].
Pramipexole dihydrochloride hydrate prevents ischemic cell death via mitochondrial pathways in ischemic stroke[5].

Animal Model: Male Wistar rats weighing 250-300 g (16-18 weeks old)[5]
Dosage: 0.25 mg/kg, 1 mg/kg
Administration: Intraperitoneal injection, at 1 hour, 6 hours, 12 hours, 18 hours post-occlusion
Result: Decreased infarction volume as compared to tMCAO (transient middle cerebral artery occlusion)-only animals.
Molecular Weight

302.26

Formula

C₁₀H₂₁Cl₂N₃OS

CAS No.

191217-81-9

中文名称

普拉克索盐酸盐水合物

SMILES

[H]Cl.NC1=NC(CC[C@H](NCCC)C2)=C2S1.[H]Cl.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

References
  • 摩尔计算器

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Keywords:

Pramipexole dihydrochlorideDopamine ReceptorParkinson'sdiseasePDrestlesslegssyndromeRLSneurologicalrecoveryneuroprotectiontMCAOtransientmiddlecerebralarteryocclusionInhibitorinhibitorinhibit

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