[CAS NO. 300576-59-4] (+)-PD 128907 hydrochloride
PRODUCTS SPECIFICATIONS [300576-59-4]
DESCRIPTION [300576-59-4]
Overview
| MDL | MFCD00210210 |
|---|---|
| Molecular Weight | 285.77 |
| Molecular Formula | C14H20ClNO3 |
| SMILES | CCCN1[C@@]2([H])[C@@](OCC1)([H])C3=CC(O)=CC=C3OC2.Cl |
Summary
(+)-PD 128907 hydrochloride is a selective dopamine D 2 /D 3 receptor agonist, with K i s of 1.7, 0.84 nM for human and rat D 3 receptors, 179, 770 n M for human and rat D 3 receptors, respectively.
IC50 & Target
In Vitro
(+)-PD 128907 displaced [ 3 H]spiperone binding from dopamine D 3 receptors (K i human=1.7 nM and rat=0.84 nM) with >100-fold and 900-fold selectivity over the human (K i =179 nM) and rat (K i =770 nM) dopamine D 2 receptor [1] [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
(+)-PD 128907 significantly decreases dialysate DA levels in D 3 knock out mice. The IC 25 values are 61 nM and 1327 nM, respectively, for wild type and D 3 knock out mice. The ratio of the IC 25 values shows that (+)-PD 128907 is 22 times more potent in decreasing dialysate DA levels in wild type as compared to mice lacking the D 3 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 IC 25 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 D 3 knock out mice. Doses of 1 mg/kg or higher of (+)-PD 128907 markedly inhibits dialysate DA in both wild type and D 3 knock out mice [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 20.83 mg/mL ( 72.89 mM ; Need ultrasonic)
H 2 O : 16.67 mg/mL ( 58.33 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [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.