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RS 102221 hydrochloride

Cat. No. 1050

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Chemical Name: 8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonamido)phenyl-5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dione hydrochloride

Biological Activity

Potent and selective 5-HT_2C antagonist (pK_i = 8.7). Displays ~ 100-fold selectivity over the 5-HT_2A and 5-HT_2B subtypes and is > 100-fold selective over other 5-HT receptors, α- and β-adrenergic and muscarinic ACh receptors.

Licensing Information

Sold with the permission of Roche Bioscience

Technical Data

M.Wt:

649.08

Formula:

C₂₇H₃₁F₃N₄O₇S.HCl

Solubility:

Soluble to 100 mM in DMSO

Purity:

>98 %

Storage:

Store at RT

CAS No:

187397-18-8

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

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Safety Data Sheet: View Safety Data Sheet

References

Weinhardt et al (1996) Some benzenesulphonamido-substituted valerophenones that are selective antagonists for the 5-HT_2C receptor. Bioorg.Med.Chem.Lett. 6 2687.

Bonhaus et al (1997) RS-102221: a novel high affinity and selective 5-HT_2C receptor antagonist. Neuropharmacology 36 621. PMID: 9225287.

Bonhaus et al (1998) Absorption and brain penetration of a high affinity, highly selective 5-HT_2C receptor antagonist, RS-102221. Ann.N.Y.Acad.Sci. 861 269. PMID: 9928284.

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