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(+)-PD 128907 hydrochloride

カタログ番号GC30848

(+)-PD 128907 塩酸塩は、選択的ドーパミン D2/D3 受容体アゴニストであり、Kis はそれぞれ、ヒトおよびラット D3 受容体に対して 1.7、0.84 nM、ヒトおよびラット D3 受容体に対して 179、770 nM です。

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(+)-PD 128907 hydrochloride 化学構造

Cas No.: 300576-59-4

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$243.00
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5mg
$220.00
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10mg
$304.00
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25mg
$607.00
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50mg
$911.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

(+)-PD 128907 hydrochloride is a selective dopamine D2/D3 receptor agonist, with Kis of 1.7, 0.84 nM for human and rat D3 receptors, 179, 770 n M for human and rat D3 receptors, respectively.

(+)-PD 128907 displaced [3H]spiperone binding from dopamine D3 receptors (Ki human=1.7 nM and rat=0.84 nM) with >100-fold and 900-fold selectivity over the human (Ki=179 nM) and rat (Ki=770 nM) dopamine D2 receptor[1][2].

(+)-PD 128907 significantly decreases dialysate DA levels in D3 knock out mice. The IC25 values are 61 nM and 1327 nM, respectively, for wild type and D3knock out mice. The ratio of the IC25 values shows that (+)-PD 128907 is 22 times more potent in decreasing dialysate DA levels in wild type as compared to mice lacking the D3 receptor. The D3 agonist evokes a dose related decrease in dialysate DA in wild type mice. Post-hoc analysis shows that all doses tested (0.03, 0.1 and 0.3 mg/kg) significantly inhibit dialysate DA. The IC25 values are 0.05 and 0.44 mg/kg for wild type and knock out mice, respectively, indicating that systemically administered (+)-PD 128907 is 9 times more potent in decreasing dialysate DA in the ventral striatum of wild type as compared to D3 knock out mice. Doses of 1 mg/kg or higher of (+)-PD 128907 markedly inhibits dialysate DA in both wild type and D3 knock out mice[3].

[1]. Collins GT, et al. Dopamine agonist-induced yawning in rats: a dopamine D3 receptor-mediated behavior. J Pharmacol Exp Ther. 2005 Jul;314(1):310-9. [2]. Bristow LJ, et al. The behavioural and neurochemical profile of the putative dopamine D3 receptor agonist, (+)-PD 128907, in the rat. Neuropharmacology. 1996 Mar;35(3):285-94. [3]. Zapata A, et al. Selective D3 receptor agonist effects of (+)-PD 128907 on dialysate dopamine at low doses. Neuropharmacology. 2001 Sep;41(3):351-9.

Chemical Properties

Cas No. 300576-59-4 SDF
Canonical SMILES CCCN1[C@@]2([H])[C@@](OCC1)([H])C3=CC(O)=CC=C3OC2.Cl
Formula C14H20ClNO3 M.Wt 285.77
溶解度 DMSO : 150 mg/mL (524.90 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.4993 mL 17.4966 mL 34.9932 mL
5 mM 0.6999 mL 3.4993 mL 6.9986 mL
10 mM 0.3499 mL 1.7497 mL 3.4993 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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