PD 128907 HCl

Alias: PD 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
Cat No.:V0039 Purity: ≥98%
PD 128907 HCl (PD-128907) 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.
PD 128907 HCl Chemical Structure CAS No.: 112960-16-4
Product category: Dopamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

PD 128907 HCl (PD-128907) 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. PD-128907 is frequently used as a tool compound to study how these receptors function in the brain, particularly as inhibitory autoreceptors, which act to prevent further dopamine release. Using [3H]spiperone as the radioligand in CHOKl-cells, PD 128907 shows approximately a 10000-fold selectivity versus human D4 receptors (Ki, 7000 nM) and a l000-fold selectivity for human D3 receptors (Ki, 1 nM) versus human D2 receptors (Ki, 1183 nM).

Biological Activity I Assay Protocols (From Reference)
Targets
D3 receptor ( EC50 = 0.64 nM )
ln Vitro

In vitro activity: PD 128907 HCl is a potent and selective dopamine D3 receptor agonist with an EC50 of 0.64 nM with a 53-fold selectivity over the dopamine D2 receptor.[1] PD 128907 shows roughly 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 D4 receptors (Ki, 7000 nM) when using [3H]spiperone as the radioligand in CHOKl-cells.[2] PD 128907 is employed in the investigation of these receptors' functions in the brain, including their function as inhibitory autoreceptors, which control the release of additional dopamine.[3]

ln Vivo
PD 128907 effectively lowers the synthesis of DA in rats treated with GBL and in rats receiving normal treatment.[4] PD 128907 (3 mg/kg) totally avoids the convulsive and deadly effects of cocaine, reducing the toxicity from overdose.[5] A D3-linked mechanism provides the protection, which also extends to seizure kindling.[6]
Enzyme Assay
(+)-PD 128907 hydrochloride is a selective agonist of the D2/D3 dopamine receptor. Its Kis values for human and rat D3 receptors are 1.7, 0.84 nM, and 179, 770 n M, respectively.
Animal Protocol
Dissolved in water; 3 mg/kg; i.p. injection
Mouse
References

[1]. Neuroreport . 1995 Jan 26;6(2):329-32.

[2]. Life Sci . 1995;57(15):1401-10.

[3]. J Neurosci . 1998 Mar 15;18(6):2231-8.

[4]. J Pharmacol Exp Ther . 1995 Dec;275(3):1355-66.

[5]. J Pharmacol Exp Ther . 2004 Mar;308(3):957-64.

[6]. J Pharmacol Exp Ther . 2008 Sep;326(3):930-8.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H20CLNO3
Molecular Weight
285.77
Exact Mass
285.11
CAS #
112960-16-4
SMILES
CCCN1CCO[C@H]2[C@H]1COC3=C2C=C(C=C3)O.Cl
InChi Key
DCFXOTRONMKUJB-QMDUSEKHSA-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-;/m1./s1
Chemical Name
(4aR,10bR)-4-propyl-3,4a,5,10b-tetrahydro-2H-chromeno[4,3-b][1,4]oxazin-9-ol;hydrochloride
Synonyms
PD 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
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~12 mg/mL (~42.0 mM)
Water: ~50 mg/mL (~175.0 mM)
Ethanol: <1 mg/mL
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • 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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