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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]. | [Definition]
ChEBI: 2-(2-benzofuranyl)-4,5-dihydro-1H-imidazole is a member of benzofurans. | [in vivo]
RX 801077 (5, 10, 20 mg/kg; i.p.; twice daily for 3 days) inhibits NLRP3 inflammasome-induced inflammation and necroptosis in a rat model of traumatic brain injury[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. PMID:7853182
[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. |
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Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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