Biochem/physiol Actions
Primary Target5-HT5A
General description
A selective, brain penetrant, 5-HT5A receptor antagonis (pKi = 8.2). Competitively antagonised 5-HT-stimulated [35S]GTPγS binding to membranes from human embryonic kidney (HEK293) cells transiently expressing the guinea pig 5-HT5A receptor (pA2 8.1 ± 0.1) and displayed 100-fold selectivity versus the serotonin transporter and those 5-HT receptor subtypes (5-HT1A/B/D, 5-HT2A/C and 5-5-HT7).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Ferenc, K. et al. 2012. Behav. Pharmacol.23, 397.Thomas, D. R. et al. 2006. Neuropharmacol.51, 566. Corbett, D. F. et al. 2005. Bioorg. Med. Chem. Lett.15, 4014.
Packaging
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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