PD128907 HCl

製品コードS2168 バッチS216801

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H19NO3.HCl
分子量 285.77 CAS No. 112960-16-4
Solubility (25°C)* 体外 DMSO 12 mg/mL (41.99 mM)
Water (warmed with 50ºC water bath) 3 mg/mL (10.49 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 PD128907 HClは、強力で選択的なドパミンD3受容体アゴニストであり、EC50値は0.64 nMで、ドパミンD2受容体に対して53倍の選択性を示します。
in vitro PD 128907 HCl is a potent and selective dopamine D3 receptor agonist, with EC50 of 0.64 nM, exhibits 53-fold selectivity over dopamine D2 receptor. When using [3H]spiperone as the radioligand in CHOKl-cells, PD 128907 exhibits about a l000-fold selectivity for human D3 receptors (Ki, 1 nM) versus human D2 receptors (Ki, 1183 nM) and a l0000-fold selectivity versus human D4receptors (Ki, 7000 nM) PD 128907 is used for studying the role of these receptors in the brain, in roles such as inhibitory autoreceptors that act to limit further dopamine release.
in vivo PD 128907 is active in reducing DA synthesis both in normal and γ-butyrolactone (GBL) treated rats. PD 128907 (3 mg/kg) reduces toxicity from cocaine overdose, completely prevented the convulsant and lethal effects of cocaine. The protection occurs through a D3-linked mechanism and that protection is extended to seizure kindling.

プロトコル(参考用のみ)

キナーゼアッセイ Ligand-binding assays
A series of equilibrium saturation studies are conducted using different Tris-HCl buffers. Briefly, 50μl of [3H]ligand (1 nM, final concentration in competition studies), 50 μl of either drug or buffer, and 400 μl of brain or CHO-Kl cell membranes in appropriate ice cold buffer are added to polypropylene micro tubes to give a total volume of 500 μl. Incubation proceeds for 60 min at 25°C and is terminated by rapid filtration followed by four washes with 1 ml buffer on a Brandel MR48 cell harvester through Whatman GF/B glass fiber filters (pre-soaked for about one hour in 0.5% PEI). Following the addition of 10 ml of liquid scintillation Ready Gel cocktail and an overnight extraction, the radioactivity remaining on the filters is counted with a Beckman LS 6800 liquid scintillation counter (50% efficiency). Specific binding is defined as total binding minus binding in presence of 1 μM haloperidol and this ranged from 90-95%. All assays are performed in triplicates. Crude membranes from CHO-Kl cells ranged from 40 μg-60 μg of protein per assay tube. Protein is determined by the Bradford assay using the microplate reader for analysis.
動物実験 動物モデル Mouse
投薬量 3 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/7756621/
  • https://pubmed.ncbi.nlm.nih.gov/7674830/
  • https://pubmed.ncbi.nlm.nih.gov/9482807/
  • https://pubmed.ncbi.nlm.nih.gov/8531103/
  • https://pubmed.ncbi.nlm.nih.gov/14711932/
  • https://pubmed.ncbi.nlm.nih.gov/18566292/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Dopamine D3 receptor in the nucleus accumbens alleviates neuroinflammation in a mouse model of depressive-like behavior [ Brain Behav Immun, 2021, 101:165-179] PubMed: 34971757

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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