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PD 128907 HCl
本半岛bd体育手机客户端 不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PD 128907 HCl图片
CAS NO:112960-16-4
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

半岛bd体育手机客户端 介绍
理化性质和储存条件
Molecular Weight (MW)285.77
FormulaC14H19NO3.HCl
CAS No.112960-16-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 12 mg/mL (42.0 mM)
Water: 50 mg/mL (175.0 mM)
Ethanol: <1 mg/mL
Other infoChemical Name: (4aS,10bS)-4-Propyl-3,4a,5,10b-tetrahydro-2H-chromeno[4,3-b][1,4]oxazin-9-ol Hydrochloride
InChi Key: DCFXOTRONMKUJB-KYSPHBLOSA-N
InChi Code: InChI=1S/C14H19NO3.ClH/c1-2-5-15-6-7-17-14-11-8-10(16)3-4-13(11)18-9-12(14)15;/h3-4,8,12,14,16H,2,5-7,9H2,1H3;1H/t12-,14-;/m0./s1
SMILES Code: OC1=CC([C@]2([H])OCCN(CCC)[C@@]2([H])CO3)=C3C=C1.[H]Cl
SynonymsPD 128907 HCl; PD128907 HCl; PD-128907 HCl; (+)-PD 128907 HCl; (+)-PD-128907 HCl; (+)-PD128907 HCl; (+)-PD128907 hydrochloride; (+)-PD-128907 hydrochloride; (+)-PD 128907 hydrochloride; PBPO; PBTO;
实验参考方法
In Vitro

In vitro activity: 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.


Kinase Assay: (+)-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.

In VivoPD 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.
Animal modelMouse
Formulation & DosageDissolved in water; 3 mg/kg; i.p. injection
ReferencesNeuroreport. 1995 Jan 26;6(2):329-32; J Pharmacol Exp Ther. 2004 Mar;308(3):957-64.
生物活性

Dopamine D3/D2 receptor agonists dose dependently protected against the convulsant effects of cocaine in mice. J Pharmacol Exp Ther. 2004 Mar;308(3):957-64.

Top, time course for the protective effects of (+)-PD 128,907 against cocaine-induced convulsions. Bottom, (+)-PD 128,907 (3 mg/kg) significantly shifted the dose-effect curve to the right for the convulsant effects of cocaine. J Pharmacol Exp Ther. 2004 Mar;308(3):957-64.

D3 antagonist PD 58491 and the D3/D2 antagonist eticlopride blocked the anticonvulsant effects of (+)-PD 128,907. J Pharmacol Exp Ther. 2004 Mar;308(3):957-
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