| Identification | Back Directory | [Name]
GSK163090 | [CAS]
844903-58-8 | [Synonyms]
CS-2298
GSK163090
GSK163090 (GSK-163090
GSK163090; GSK-163090; GSK 163090.
5-HT1A/B/D receptor antagonist GS163090
1-[3-[2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl]phenyl]-2-imidazolidinone
2-Imidazolidinone,1-[3-[2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl]phenyl]- | [Molecular Formula]
C25H29N5O | [MOL File]
844903-58-8.mol | [Molecular Weight]
415.53 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]
In male Sprague-Dawley rats, GSK163090 (compound 36) treatment shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg[1]. | [IC 50]
5-HT1A Receptor: 9.4 (pKi); 5-HT1B Receptor: 8.5 (pKi); 5-HT1D Receptor: 9.7 (pKi); D2 Receptor: 6.3 (pKi); D3 Receptor: 6.7 (pKi); 5-HT2A Receptor: 6 (pKi); 5-HT2B Receptor: 6.3 (pKi); 5-HT2C Receptor: 5.8 (pKi); Human 5-HT6 Receptor: <5.3 (pKi); Human 5-HT7 Receptor: 6.8 (pKi) | [storage]
Store at -20°C | [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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