Emapunil is a translocator protein [TSPO(18 kDa)] ligand.
Emapunil 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human Hs683 glioma cells
IC50 2.73 nM
90 minutes
To evaluate the affinity of AC-5216 for MBR in human Hs683 glioma cells, the results showed that AC-5216 has high affinity for MBR (IC50 2.73 nM).
Br J Pharmacol. 2004 Aug;142(7):1059-72
Rat C6 glioma cells
IC50 3.04 nM
90 minutes
To evaluate the affinity of AC-5216 for MBR in rat C6 glioma cells, the results showed that AC-5216 has high affinity for MBR (IC50 3.04 nM).
Br J Pharmacol. 2004 Aug;142(7):1059-72
Rat whole brain mitochondria
Ki 0.297 nM
90 minutes
To evaluate the affinity of AC-5216 for MBR in rat whole brain mitochondria, the results showed that AC-5216 has high affinity for MBR (Ki 0.297 nM).
Br J Pharmacol. 2004 Aug;142(7):1059-72
primate choroidal endothelial cells (RF/6A)
25 μM
24 hours
To study the effect of TSPO ligands on cholesterol efflux, results showed both ligands significantly increased cholesterol efflux to HDL and human serum.
Int J Mol Sci. 2018 Nov 24;19(12):3740
CA1 pyramidal neurons from Thy1-eGFP mice
3 µM
prevents dendritic spine loss induced by Aβ1-42 oligomers
Transl Psychiatry. 2023 Oct 27;13(1):332
hippocampal slices
300 nM
60 minutes
prevents LTP impairments induced by Aβ1-42 oligomers
Transl Psychiatry. 2023 Oct 27;13(1):332
human iPS-derived microglial cells (iPSdM)
30 μM
24 h
Study the effect of XBD173 on microglial morphology and phagocytic function, results showed XBD173 promoted filopodia formation and enhanced phagocytic capacity.
J Neuroinflammation. 2014 Jan 8;11:3
661 W photoreceptor-like cells
50 μM
48 h
Evaluate the effect of microglial conditioned medium on photoreceptor apoptosis, results showed XBD173 significantly reduced photoreceptor apoptosis.
J Neuroinflammation. 2014 Jan 8;11:3
BV-2 microglial cells
20 μM and 50 μM XBD173
24 h
Investigate the effect of XBD173 on inflammatory marker expression, results showed XBD173 significantly suppressed CCL2, IL6, and iNOS mRNA expression.
J Neuroinflammation. 2014 Jan 8;11:3
mouse primary microglia
50 µM
1 hour
XBD173 strongly diminished stimulation-induced ROS production after PMA or photoreceptor cell debris stimulation in microglia.
AC-5216 dose-dependently alleviated mechanical allodynia, with the maximum effect at 4.0 μg. Direct microinjection of neurosteroids AP and DOC had effects similar to AC-5216.
Neurosci Bull. 2016 Aug;32(4):311-22
Mice
MacGreen/Rs1h-/Y mice
Retinal explants
20 μM
24 h
Investigate the effect of XBD173 on microglial morphology, results showed XBD173 significantly reduced the number of LPS-induced amoeboid microglial cells.
J Neuroinflammation. 2014 Jan 8;11:3
C57BL/6J mice
Laser-induced choroidal neovascularization (CNV) model
Intraperitoneal injection
10 mg/kg
Daily starting one day before laser photocoagulation
XBD173 treatment significantly reduced phagocyte reactivity, vascular leakage, and neovascularization in the retina and RPE/choroid after laser injury.
Nat Commun. 2020 Jun 1;11(1):2709
Mice
Retinal ischemia model (HIOP-induced)
Intraperitoneal injection
10 mg/kg body weight
Twice daily (from 1 day pre-surgery to 3/7/14 days post-surgery)
XBD173 reduced inner retinal neuronal death post-ischemia by stabilizing neurosupportive glial functions (e.g., Müller cell glutamine synthetase activity and volume regulation).
J Neuroinflammation. 2019 Feb 18;16(1):43
BALB/cJ and Cx3cr1GFP/+ mice
Acute retinal degeneration models
Intraperitoneal injection
10 mg/kg
Twice daily for the first 2 days, then once daily for the remaining 3 days, total of 5 days
XBD173 treatment significantly reduced the number of CD11b-positive cells in the retina after light damage and decreased microglial reactivity, thereby protecting the retina from degeneration induced by light damage.
J Neuroinflammation. 2015 Nov 2;12:201
Rat
Vogel-type conflict test
Oral
0.1–3 mg/kg
Single administration, 1 hour before testing
To evaluate the anti-anxiety effects of AC-5216 in the Vogel-type conflict test in rats, the results showed that AC-5216 significantly increased the number of shocks received by rats at doses of 0.1–3 mg/kg, indicating its anti-anxiety effects.
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