BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist. BD-1063 dose dependently reduced ethanol self-administration in sP rats (3.3-11 mg/kg) and withdrawn, dependent Wistar rats (4-11 mg/kg) at doses that did not modify mean ethanol self-administration in nondependent Wistar controls. BD-1063 also reduced the breakpoints of sP rats to work for ethanol under a progressive-ratio reinforcement schedule[1]. BD-1063 dose-dependently reduced binge-like eating and the regularity of food responding, and blocked the increased eating rate in Palatable rats. In the light/dark conflict test, BD-1063 antagonized the increased time spent in the aversive compartment and the increased intake of the palatable diet, without affecting motor activity[2]. In endothelial cells, 10-100 μM of the Sig1R antagonist BD1063 inhibited sustained but not transient calcium responses evoked by histamine[3]. BD1063 treatment was able to preserve neuromuscular function of the hindlimbs and increased the number of surviving MNs (motoneurons) in the treated female SOD1G93A mice[4].
BD1063 dHCl 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HEK 293 cells expressing TRPM3
100 μM
1 hour
BD1047, BD1063, and 4-IBP inhibited TRPM3 channel activity, while SKF10047 had no effect.
Br J Pharmacol. 2013 Mar;168(6):1445-55
HEK 293 cells expressing TRPC5
100 μM
1 hour
BD1047, BD1063, and 4-IBP inhibited TRPC5 channel activity, and SKF10047 also showed inhibitory effects.
Br J Pharmacol. 2013 Mar;168(6):1445-55
human saphenous vein endothelial cells (SVECs)
10–100 μM
30 min
BD1063 inhibited sustained calcium responses evoked by histamine, VEGF, or hydrogen peroxide but not transient calcium responses.
Br J Pharmacol. 2013 Mar;168(6):1445-55
NG108 cells
100 nM
BD-1063 significantly reduced METH-induced dopamine release and efflux
Neuropsychopharmacology. 2018 May;43(6):1405-1414
Retinal microglia cells
10 μM
30 min
BD1063 blocked the (+)-pentazocine-mediated inhibition of LPS-induced morphologic changes, cytokine release, and ROS generation.
Invest Ophthalmol Vis Sci. 2014 May 8;55(6):3375-84
BD1063 dHCl 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Prenatal stress model
Intraperitoneal injection
10 mg/kg
Single administration, 20 minutes before
BD1063 alone did not affect performance but blocked the effect of igmesine, confirming the involvement of the σ1 receptor.
Br J Pharmacol. 2004 Jun;142(4):689-700
Male Wistar rats
Binge-like eating model
Subcutaneous injection
0, 3.75, 7.5, 15, 30 mg/kg
15 min pretreatment, 1 h testing
BD-1063 dose-dependently reduced binge-like eating and the regularity of food responding, and blocked the increased eating rate in Palatable rats.
Neuropsychopharmacology. 2012 Nov;37(12):2593-604
Rats
Sardinian alcohol-preferring rats and ethanol-dependent Wistar rats
Subcutaneous injection
3.3–11 mg/kg (sP rats) and 4–11 mg/kg (Wistar rats)
Single dose, 15 min before testing
BD-1063 dose-dependently reduced ethanol self-administration in sP rats and ethanol-dependent Wistar rats, but had no significant effect on non-dependent Wistar controls. BD-1063 also reduced the breakpoints of sP rats to work for ethanol under a progressive-ratio reinforcement schedule.
Neuropsychopharmacology. 2009 May;34(6):1482-93
Male Wistar-Harlan rats
TNBS-induced colitis model
Intracolonic administration
0.1 mg/kg
Once daily for three days
BD1063 as a σ1R antagonist exacerbated colonic inflammation when used alone and counteracted the beneficial effects of FLV when co-administered.
搜索
