Invest Ophthalmol Vis Sci. 2012 Jul 3;53(8):4416-25
Mouse primary alveolar macrophages
5 µM
18 hours
To evaluate the antagonistic effect of SR144528 on JWH133's anti-inflammatory action; results showed SR144528 reversed JWH133's suppression of IL-1β and TNF-α
Respir Res. 2022 Dec 3;23(1):326
RAW264.7 cells
1 µM
20 minutes
SR144528 was used as a CB2R antagonist to verify whether the protective effect of GW405833 was mediated by CB2R. The results showed that SR144528 pretreatment abolished the inhibitory effect of GW405833 on LPS-induced macrophage proliferation and inflammatory cytokine release.
Acta Pharmacol Sin. 2023 Jul;44(7):1391-1403
HK-2 cells
1 µM
24 hours
SR144528 reversed the inhibitory effects of celastrol on TGF-β1-induced expression of fibronectin, collagen I, and α-SMA
Cell Death Dis. 2018 May 22;9(6):601.
U87 human glioma cells
0.1 µM and 1 µM
30 minutes
To evaluate the effect of SR144528 on CBD-induced inhibition of cell migration, results showed SR144528 failed to prevent CBD's inhibitory effect
Br J Pharmacol. 2005 Apr;144(8):1032-6
Rat small mesenteric artery
1 µM
30 minutes
SR144528 had little effect on abn-cbd-induced relaxation
Br J Pharmacol. 2003 Apr;138(7):1320-32
SR144528 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/C mice
UUO-induced renal fibrosis model
Intraperitoneal injection
1 mg/kg
Once daily for 7 days
SR144528 abolished the beneficial effects of celastrol on UUO-induced renal fibrosis
Cell Death Dis. 2018 May 22;9(6):601.
Rats
Huntington's disease model
Intraperitoneal injection
1 mg/kg
30 minutes before and 2 hours after
SR144528 reversed the neuroprotective effects of HU-308
Glia. 2009 Aug 15;57(11):1154-67
BALB/c mice
D-GalN/LPS-induced acute liver failure model
Intraperitoneal injection
1 mg/kg
Single administration
SR144528 was used as a CB2R antagonist to verify whether the protective effect of GW405833 was mediated by CB2R. The results showed that SR144528 pretreatment abolished the protective effect of GW405833 on D-GalN/LPS-induced acute liver failure.
Acta Pharmacol Sin. 2023 Jul;44(7):1391-1403
Mice
Chronic intestinal inflammation model
Intraperitoneal injection
1 mg/kg
Single dose
To investigate the effect of SR144528 on PEA-induced inhibition of intestinal motility, results showed SR144528 did not significantly modify the inhibitory effect of PEA.
Br J Pharmacol. 2001 Nov;134(5):945-50
Mice
Carrageenan-induced inflammatory pain model and spared nerve injury (SNI) neuropathic pain model
Intraperitoneal injection
1 mg/kg
Single administration
SR144528 reversed the analgesic effects of celastrol in both carrageenan-induced inflammatory pain and SNI neuropathic pain models, indicating that the analgesic effects of celastrol are mediated through CB2 signaling.
Int J Mol Sci. 2014 Aug 6;15(8):13637-48
Mice
Oxaliplatin-induced peripheral neuropathy model
Intraperitoneal injection
1 mg/kg
Once daily until the end of the experiment
SR144528 abrogated the anti-nociceptive effect of BCP on mechanical allodynia, without impacting OXA-induced sensitivity to cold.
Antioxidants (Basel). 2023 Oct 22;12(10):1893
Rats
Neuropathic pain model
Intraperitoneal injection
1 mg/kg
Administered 30 min prior, lasting for 4 days
The CB2-selective antagonist SR144528 blocked both the anti-allodynic effects of (R,S)-AM1241 self-medication and the percentage of active lever responding in neuropathic (but not naive) rats.
Pain. 2011 Sep;152(9):1976-1987
Rat
Isolated heart ischemia-reperfusion model
Perfusion
1 μM
15 min pretreatment, continued until the end of the ischemic period
SR144528 completely blocked the cardioprotective effects of PEA and 2-AG, indicating that CB2 receptors play a major role in mediating the cardioprotective effects of endocannabinoids.
To verify the specificity of CB2R-mediated effects; SR144528 antagonized JWH133's protective effects and exacerbated PA-induced lung injury and inflammation
Respir Res. 2022 Dec 3;23(1):326
Mice
Chemotherapy-induced peripheral neuropathy model
Intraperitoneal injection
2.1 mg/kg
Once daily for 8 days
SR144528 blocked the antiallodynic effects of AM1710, indicating that the antiallodynic effects of AM1710 are mediated by peripheral CB2 receptors.
Pain. 2022 May 1;163(5):834-851
Mice
Carrageenan-induced inflammatory pain model
Intraperitoneal injection
3 mg/kg
Single administration
To evaluate the role of CB2 receptors in the anti-edematous and anti-allodynic effects of JZL184. Results showed that SR144528 completely blocked the anti-edematous effects of JZL184, indicating that CB2 receptors are necessary for the anti-edematous effects.
Life Sci. 2013 Mar 19;92(8-9):498-505
Mice
Chronic constriction injury (CCI) model
Intraperitoneal injection
3 mg/kg
Single administration
To evaluate the effect of the CB2 receptor antagonist SR144528 on the analgesic effects of the combination of JZL184 and diclofenac. Results showed that SR144528 did not block the analgesic effects of the combination on mechanical allodynia, indicating that CB1 receptors, not CB2 receptors, were primarily responsible for the anti-allodynia.
Br J Pharmacol. 2015 Apr;172(7):1700-12
Mice
Wild-type mice and CB2R knockout mice
Intraperitoneal injection
3 mg/kg
Single dose, 30 minutes prior
SR144528 significantly increased seizure susceptibility to PTZ-induced seizures in wild-type mice but had no effect in CB2R knockout mice.
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