Drug intelligence / Profile preview

BRL 44408

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal, Intrathecal, Intracerebroventricular, Subcutaneous
01

Overview

BRL 44408 is a potent and selective small molecule antagonist of the alpha-2A adrenergic receptor (ADRA2A). It is widely used as a pharmacological probe to differentiate the functional contributions of the alpha-2A subtype from the alpha-2B and alpha-2C subtypes in various physiological systems. In preclinical research, BRL 44408 has been shown to reverse the antinociceptive effects of alpha-2 agonists like clonidine and dexmedetomidine in models of neuropathic and inflammatory pain. It also demonstrates the ability to modulate sympathetic outflow, influence gastric motility, and reduce the severity of intestinal inflammation in colitis models. While it is a critical tool in neuroscience and pharmacology research, it has not been approved for clinical use in humans.

Other names
2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole
02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))ADRA2A (α2A)

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