5.08146

WAY-100635 Maleate

• Synonyme(s) : WAY-100635 Maleate, 5-HT _1A Serotonis Receptor Antagonist, WAY-100635 Maleate, WAY 100635, WAY100635, 5-HT_1A Serotonis Receptor Antagonist, WAY-100635 Maleate, WAY 100635, WAY100635
• Formule empirique (notation de Hill) : C₂₅H₃₄N₄O₂ · xC₄H₄O₄
• Numéro CAS: 634908-75-1
• Poids moléculaire : 422.56 (free base basis)
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD01321056
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Propriétés

• assay: ≥97% (HPLC)
• Quality Segment: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: off-white
• solubility: water: 50 mM
• storage temp.: 2-8°C
• SMILES string: N3(CCN(CC3)c4c(cccc4)OC)CCN(c2ncccc2)C(=O)C1CCCCC1.OC(=O)\C=C/C(=O)O
• InChI: 1S/C25H34N4O2.C4H4O4/c1-31-23-12-6-5-11-22(23)28-18-15-27(16-19-28)17-20-29(24-13-7-8-14-26-24)25(30)21-9-3-2-4-10-21;5-3(6)1-2-4(7)8/h5-8,11-14,21H,2-4,9-10,15-20H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
• InChI key: XIGAHNVCEFUYOV-BTJKTKAUSA-N

Description

General description

A selective 5-HT_1A receptor antagonist (pKi = 7.9-9.2). WAY-100635 has been reported to have good inhibitory action centrally and peripherally (1mg/kg dose in rats) but has low intrinsic effects, making it a silent 5-HT_1A receptor antagonist. WAY-100635 displaced specific binding of the 5-HT_1A radioligand, [3H]8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin), to rat hippocampal membranes with a pIC₅₀ of 8.87. This represented a greater than 100-fold selectivity relative to binding at other 5-HT receptor subtypes and major neurotransmitter receptor, reuptake and ion channel sites. WAY-100635 has been used in a variety of vertebrate species in vivo and in vitro.

Biochem/physiol Actions

Primary Target
5-HT_1A

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warming is required for complete solubilization.

Other Notes

Hunt, G. E. et al. 2011. Brain Res. Bull.86, 65.

Caamano, R. I. et al. 2010. J. Exp. Biol.213, 1813.

Newman-Tancredi, A. et al. 1998. Naunyn Schmiedebergs Arch. Pharmacol.357, 205.
Forster, E. A. et al. 1995. Eur. J. Pharmacol.281, 81.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Informations sur la sécurité

• Classe de stockage: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable