Chemical Name:2-Amino-6-methyl-4-propyl-[1,2,4]triazolo[1,5-a]pyrimid
in-5(4H)-one
Biological Activity:
Potent
phosphodiesterase (PDE) 4 inhibitor (IC50 = 35 nM for inhibition of
[3H]-rolipram binding to rat brain). Antidepressant following
systemic administration in vivo.
Wachtel (1983) Potential antidepressant
activity of rolipram and other selective cyclic adenosine 3',5'-monophosphate
phosphodiesterase inhibitors. Neuropharmacology 22 267. Kaulenet al (1989) Autoradiographic mapping of a selective cyclic adenosine
monophosphate phosphodiesterase in rat brain with the antidepressant [3H]rolipram.
Brain Res. 503 229. Zhaoet al (2003) Inhibitor
binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast
and [3H]rolipram. J.Pharmacol.Exp.Ther. 305 565.
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