1H-Imidazole, 2-(2-benzofuranyl)-4,5-dihydro-

Names

[ Name ]:
1H-Imidazole, 2-(2-benzofuranyl)-4,5-dihydro-

[Synonym ]:
2-(2-Benzofuranyl)-2-imidazoline
2-benzofuran-2-yl-4,5-dihydro-1H-imidazole
2xcg
2-BFi
(3H)2-Bfi
3H-2-(2-benzofuranyl)-2-imidazoline
Tocris-0348
2-(2'-Imidazolinyl)benzofuran

Biological Activity

[Description]:

RX 801077 (2 BFI free base) is a selective imidazoline I2 receptor (I2R) agonist with a Ki value of 70.1 nM. RX 801077 shows anti-inflammation and neuroprotection. RX 801077 has the potential for the research of traumatic brain injury (TBI)[1][2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Imidazoline Receptor

Signaling Pathways >> GPCR/G Protein >> Imidazoline Receptor

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

[Target]

Ki: 70.1 nM (imidazoline I2 receptor)[2]

[In Vivo]

RX 801077 (5、10、20 mg/kg；腹腔注射；每天两次，持续 3 天) 在创伤性脑损伤大鼠模型中抑制 NLRP3 炎性体诱导的炎症和坏死性凋亡[2]。 Animal Model: 280-300 g, Male adult Sprague-Dawley rats (TBI model)[2] Dosage: 5, 10, 20 mg/kg Administration: I.p.; twice daily for 3 days Result: Attenuated neurological deficits, brain edema, BBB permeability and cortical tissue loss in a rat model of TBI, reduced microglial activation, neutrophil infiltration, and proinflammatory cytokine IL-1β secretion, reduced the expression of RIP1 and RIP3 in neurons in the pericontusional cortex.

[References]

[1]. Carpéné C, et al. Inhibition of amine oxidase activity by derivatives that recognize imidazoline I2 sites. J Pharmacol Exp Ther. 1995 Feb;272(2):681-8.

[2]. Ni H, et al. 2-BFI Provides Neuroprotection Against Inflammation and Necroptosis in a Rat Model of Traumatic Brain Injury. Front Neurosci. 2019 Jun 26;13:674.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₁H₁₀N₂O

[ Molecular Weight ]:
186.21

[ Exact Mass ]:
186.07900

[ PSA ]:
37.53000

[ LogP ]:
1.54700

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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