product name PD128907 HCl
Description: 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 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.
285.77
Formula
C14H19NO3.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
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19414376
| 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: Cell Assay: |
|---|---|
| In Vivo | PD 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 model | Mouse |
| Formulation & Dosage | Dissolved in water; 3 mg/kg; i.p. injection |
| References | Neuroreport. 1995 Jan 26;6(2):329-32; J Pharmacol Exp Ther. 2004 Mar;308(3):957-64. |
