Chemical Name:N-[4-(4-Methyl-1-piperazinyl)phenyl]-9-acridinamine
dihydrochloride
Biological Activity:
α2C-adrenoceptor antagonist
that displays ~ 50-fold selectivity over other α2-adrenoceptor subtypes
(Ki values are 28, 1470, 1700 and 3150 nM for human α2C, α2B, α2D and α2A subtypes respectively).
Potently antagonises adrenalin-stimulated 35GTPγS
binding in vitro (KB = 16 nM) and produces antidepressant and
antipsychotic-like effects in vivo.
Tricklebank (2007) JP-1302: a new tool to shed light on the roles of α2C-adrenoceptors in brain. Br.J.Pharmacol. 150 381. Sallinenet al (2007) Pharmacological characterization and CNS effects of a novel
highly selective α2C-adrenoceptor antagonist JP-1302.
Br.J.Pharmacol. 150 391.