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BRL 44408 maleate

Names

[ CAS No. ]:
681806-46-2

[ Name ]:
BRL 44408 maleate

[Synonym ]:
BRL44408 maleate
2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole maleate
2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindolemaleate
2-[(2H-1-methyl-1,3-dihydroisoindole)methyl]-4,5-dihydroimidazole maleate
BRL 44408 maleate

Biological Activity

[Description]:

BRL-44408 maleate is an α2A-adrenoceptor antagonist (Ki: 8.5 nM). BRL-44408 maleate has antidepressant and analgesic activity. BRL-44408 also improves cecal ligation puncture (CLP)-induced acute lung injury[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Research Areas >> Neurological Disease

[Target]

Ki: 8.5 nM (α2A-adrenoceptor)[1]


[References]

[1]. Dwyer JM, et al. Preclinical characterization of BRL 44408: antidepressant- and analgesic-like activity through selective alpha2A-adrenoceptor antagonism. Int J Neuropsychopharmacol. 2010 Oct;13(9):1193-205.  

[2]. Cong Z, et al. α2A -AR antagonism by BRL-44408 maleate attenuates acute lung injury in rats with downregulation of ERK1/2, p38MAPK, and p65 pathway. J Cell Physiol. 2020 Oct;235(10):6905-6914.  

Chemical & Physical Properties

[ Molecular Formula ]:
C17H21N3O4

[ Molecular Weight ]:
331.36600

[ Exact Mass ]:
331.15300

[ PSA ]:
102.23000

[ LogP ]:
0.97900

Related Compounds