Description
General description
A cell-permeable phenylpropylamine derived anti-depressant that acts as a selective serotonin re-uptake inhibitor (SSRI). Reported to modulate the proliferation of T cells by increasing the Ca²⁺ influx thereby influencing the activities of protein kinase A (PKA) and protein kinase C (PKC). Inhibits leak K⁺ currents in a reversible and voltage-independent manner (IC₅₀ = 780 nM). Also shown to regulate the phosphorylation of DARPP-32 (dopamine-and cAMP-regulated phosphoprotein of Mr 32,000) and AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptors. Triggers oxidative stress-induced apoptotic cell death and initiates signaling pathways in neuronal cells leading to an activation of ERK and NF-κB.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Selective serotonin re-uptake inhibitor
Product does not compete with ATP.
Reversible: no
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Bartholoma, P., et al. 2002. Biochem. Pharmacol.63, 1507.
Bian, J.T., et al. 2002. Eur. J. Pharmacol.453, 159.
Zhang, A., et al. 2002. J. Med. Chem.45, 1930.
Svenningsson, P., et al. 2002. Proc. Natl. Acad. Sci. USA99, 3182.
Edgar, V.A., et al. 1999. Eur. J. Pharmacol.372, 65.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)