1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor

GSK598809 

Cat. No.: HY-19654
Handling Instructions

GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.

For research use only. We do not sell to patients.

GSK598809 Chemical Structure

GSK598809 Chemical Structure

CAS No. : 863680-45-9

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.

IC50 & Target

pKi: DRD3[1][2].

In Vivo

Cocaine and GSK598809 each increases peak mean arterial blood pressure. Least square mean differences are significant for both doses of cocaine compared with its vehicle. Likewise, least square mean differences are significant for both doses of GSK598809 as compared with its vehicle. The experimental question of interest, that is, whether GSK598809 significantly increases cocaine effects on peak mean arterial blood pressure, is probed by a prior it tests on the means of the fitted regression model. The dose of 3 mg/kg GSK598809 significantly increases the pressor effects of 5.6 mg/kg cocaine and of 1.7 mg/kg cocaine[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0768 mL 10.3840 mL 20.7680 mL
5 mM 0.4154 mL 2.0768 mL 4.1536 mL
10 mM 0.2077 mL 1.0384 mL 2.0768 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Dogs[1]
Male beagle dogs are used throughout the study. The experiment is conducted in phases. In the first (hemodynamics) phase, the dogs are dosed at weekly intervals over a period of 9 weeks with combinations of either GSK598809 or vehicle, followed by either cocaine or vehicle. After the baseline measurements are recorded, technical staff briefly returns to the animal room to administer GSK598809 (or vehicle) to all the dogs via oral gavage and activate the timers on the preloaded and preprogrammed infusion pumps[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

481.51

Formula

C₂₂H₂₃F₄N₅OS

CAS No.

863680-45-9

SMILES

CC1=C(C2=NN=C(SCCCN3CC4(C5=CC=C(C(F)(F)F)C=C5F)CC4C3)N2C)OC=N1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
GSK598809
Cat. No.:
HY-19654
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GSK598809

Cat. No.: HY-19654