2-BFI (hydrochloride)

2-BFI is an agonist of the imidazoline I₂ receptor.¹ It selectively binds to the imidazoline I₂ receptor over α2-adrenergic receptors (α₂-ARs) in rabbit whole brain membranes (K_is = 0.0013 and 3.736 µM, respectively), as well as the imidazoline I₁ receptor in human platelet membranes (K_is = 0.0667 and 53 µM for the high- and low-affinity sites, respectively).^1,2 2-BFI (100 µmol/kg) reduces immobility time in the tail suspension test, an effect that can be reversed by idazoxan, methysergide (Item No. 27658), or haloperidol (Item No. 12014).³ Intracerebroventricular administration of 2-BFI (10 µg/animal) enhances morphine-induced antinociception in the tail-flick test in mice.⁴ 2-BFI improves neurological deficits, reduces brain edema, microglia activation, and neutrophil infiltration, and inhibits neuronal necrosis in a rat model of traumatic brain injury.⁵

WARNING This product is not for human or veterinary use.

1. Hudson, A.L., Chapleo, C.B., Lewis, J.W., et al. Identification of ligands selective for central I₂-imidazoline binding sites. Neurochem. Int. 30(1), 47-53 (1997).

2. Piletz, J.E., Zhu, H., and Chikkala, D.N. Comparison of ligand binding affinities at human I₁-imidazoline binding sites and the high affinity state of alpha-2 adrenoceptor subtypes. J. Pharmacol. Exp. Ther. 279(2), 694-702 (1996).

3. Tonello, R., Villarinho, J.G., da Silva Sant'Anna, G., et al. The potential antidepressant-like effect of imidazoline I₂ ligand 2-BFI in mice. Prog. Neuropsychopharmacol. Biol. Psychiatry 37(1), 15-21 (2012).

4. Sánchez-Blázquez, P., Boronat, M.A., Olmos, G., et al. Activation of I₂-imidazoline receptors enhances supraspinal morphine analgesia in mice: A model to detect agonist and antagonist activities at these receptors. Br. J. Pharmacol. 130(1), 146-152 (2000).

5. Ni, H., Rui, Q., Lin, X., et al. 2-BFI provides neuroprotection against inflammation and necroptosis in a rat model of traumatic brain injury. Front. Neurosci. 13, 674 (2019).