A high affinity 5-HT6 Receptor antagonist (pKi = 9.0). Good solubility (to 100 mM in water or DMSO), oral availability, and penetrant to blood brain barrier. Over 200-fold selective for 5-HT6 receptors vs all receptors, ion channels and enzymes tested in Hirst et al. 2006 publication. Shows nootropic, antidepressant and axiolytic effects comparable to well-described drugs such as diazepam, and therefore has been proposed as novel treatment for schizoprenia and Alzheimer′s disease.
Biochem/physiol Actions
Primary Target 5-HT₆
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Wesolowska, A. et al. 2007. Pharmacol Rep.59, 664. Li, Z. et al. 2007. Brain Res.1134, 70.
Hirst, et al. 2006. Eur. J. Pharm.553, 109. Routledge, C. et al. 2000. Br. J. Pharmacol.130, 1606.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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