Home Neuronal Signaling Dopamine Receptor agonist PD128907 HCl

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PD128907 HCl Dopamine Receptor agonist

Cat.No.S2168

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.
PD128907 HCl Dopamine Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 285.77

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Quality Control

Batch: S216801 DMSO]12 mg/mL]false]Water]3 mg/mL]false]Ethanol]Insoluble]false Purity: 99.44%
  • Cited in Nature Medicine for its top-tier quality
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99.44

Solubility

In vitro
Batch:

DMSO : 12 mg/mL (41.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 3 mg/mL

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 285.77 Formula

C14H19NO3.HCl

 Storage (From the date of receipt)
CAS No. 112960-16-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCCN1CCOC2C1COC3=C2C=C(C=C3)O.Cl

Mechanism of Action

Targets/IC50/Ki
D3 receptor
0.64 nM(EC50)
In vitro
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.
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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/8531103/
  • [5] https://pubmed.ncbi.nlm.nih.gov/14711932/
  • [6] https://pubmed.ncbi.nlm.nih.gov/18566292/

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