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 3 mg/mL warmed with 50ºC water bath (10.49 mM)
Ethanol Insoluble
* <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 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.
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. [1] 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) [2] 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.[3]
in vivo PD 128907 is active in reducing DA synthesis both in normal and γ-butyrolactone (GBL) treated rats. [4] PD 128907 (3 mg/kg) reduces toxicity from cocaine overdose, completely prevented the convulsant and lethal effects of cocaine. [5] The protection occurs through a D3-linked mechanism and that protection is extended to seizure kindling. [6]

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.

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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