GSK163090 Chemical Properties

Density 

1.216±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 16.5 mg/mL (39.71 mM)

form 

Solid

pka

14.20±0.20(Predicted)

color 

White to yellow

GSK163090 Usage And Synthesis

Uses

GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities[1].

in vivo

IC 50

5-HT_1A Receptor: 9.4 (pKi); 5-HT_1B Receptor: 8.5 (pKi); 5-HT_1D Receptor: 9.7 (pKi); D₂ Receptor: 6.3 (pKi); D₃ Receptor: 6.7 (pKi); 5-HT_2A Receptor: 6 (pKi); 5-HT_2B Receptor: 6.3 (pKi); 5-HT_2C Receptor: 5.8 (pKi); Human 5-HT₆ Receptor: <5.3 (pKi); Human 5-HT₇ Receptor: 6.8 (pKi)

References

[1] Leslie CP, et al. Discovery of 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, selective, and orally active 5-HT1A/B/D receptor antagonist. J Med Chem. 2010 Dec 9;53(23):8228-8240. DOI:10.1021/jm100714c

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