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    PD 128907 HCl
    PD 128907 HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0039
    CAS #: 112960-16-4Purity ≥98%

    Description: PD 128907 HCl is a novel, potent and selective dopamine D3 receptor agonist with EC50 of 0.64 nM, it 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 10000-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.

    References: Neuroreport. 1995 Jan 26;6(2):329-32; J Pharmacol Exp Ther. 2004 Mar;308(3):957-64.

    Related CAS:123594-64-9 (PD 128907); 300576-59-4

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    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;


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    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. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    PD 128907 HCl

    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. 
     

    PD 128907 HCl

    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.  
     

    PD 128907 HCl

    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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