BRL 44408 MALEATE

Uses

Selective a2A-adrenoceptor antagonist . Increases hippocampal noradrenaline release following systemic administration

Uses

BRL 44408 Maleate was used to study for norepinephrine reuptake modulators for preventing and treating vasomotor symptoms.

Uses

Selective α2A-adrenoceptor antagonist . Increases hippocampal noradrenaline release following systemic administration.

Biological Activity

Selective α 2A -adrenoceptor antagonist (K i = 1.7 nM and 144.5 nM at α 2A and α 2B -adrenergic receptors respectively). Increases hippocampal noradrenalin release following systemic administration. Also available as part of the α 2 -Adrenoceptor Tocriset™ .

Biochem/physiol Actions

BRL 44408 maleate is a selective α2A-adrenoceptor antagonist.

References

[1]. meana jj, callado lf, pazos a, et al. the subtype-selective alpha 2-adrenoceptor antagonists brl 44408 and arc 239 also recognize 5-ht1a receptors in the rat brain. eur j pharmacol, 1996, 312(3): 385-388.
[2]. owesson ca, seif i, mclaughlin dp, et al. different alpha(2) adrenoceptor subtypes control noradrenaline release and cell firing in the locus coeruleus of wildtype and monoamine oxidase-a knockout mice. eur j neurosci, 2003, 18(1): 34-42.
[3]. dwyer jm, platt bj, rizzo sj, et al. preclinical characterization of brl 44408: antidepressant- and analgesic-like activity through selective alpha2a-adrenoceptor antagonism. int j neuropsychopharmacol, 2010, 13(9): 1193-1205.