GSK163090 - CAS 844903-58-8
Catalog number: 844903-58-8
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C25H29N5O
Molecular Weight:
415.54
COA:
Inquire
Targets:
5-HT Receptor
Description:
GSK163090 is Potent, selective, and orally active 5-HT1A/B/D receptor antagonist.
Purity:
98%
Related CAS:
844903-52-2(GSK-163090 HCl)
Appearance:
Solid powder
Synonyms:
1-(3-(2-(4-(2-methylquinolin-5-yl)piperazin-1-yl)ethyl)phenyl)imidazolidin-2-one; GSK163090; GSK-163090; GSK 163090
Solubility:
Soluble in DMSO, not in water
Storage:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years if stored properly
InChIKey:
ANGUXJDGJCHGOG-UHFFFAOYSA-N
InChI:
1S/C25H29N5O/c1-19-8-9-22-23(27-19)6-3-7-24(22)29-16-14-28(15-17-29)12-10-20-4-2-5-21(18-20)30-13-11-26-25(30)31/h2-9,18H,10-17H2,1H3,(H,26,31)
Canonical SMILES:
O=C1NCCN1C2=CC=CC(CCN3CCN(C4=C5C=CC(C)=NC5=CC=C4)CC3)=C2
1.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.
Leslie CP1, Biagetti M, Bison S, Bromidge SM, Di Fabio R, Donati D, Falchi A, Garnier MJ, Jaxa-Chamiec A, Manchee G, Merlo G, Pizzi DA, Stasi LP, Tibasco J, Vong A, Ward SE, Zonzini L. J Med Chem. 2010 Dec 9;53(23):8228-40. doi: 10.1021/jm100714c. Epub 2010 Nov 5.
In an effort to identify selective drug like pan-antagonists of the 5-HT1 autoreceptors, studies were conducted to elaborate a previously reported dual acting 5-HT1 antagonist/SSRI structure. A novel series of compounds was identified showing low intrinsic activities and potent affinities across the 5-HT1A, 5-HT1B, and 5-HT1D receptors as well as high selectivity against the serotonin transporter. From among these compounds, 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (36) was found to combine potent in vivo activity with a strong preclinical developability profile, and on this basis it was selected as a drug candidate with the aim of assessing its potential as a fast-onset antidepressant/anxiolytic.
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CAS 844903-58-8 GSK163090

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