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BD1063 dHCl

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Chemical Structure| 206996-13-6 同义名 : BD1063 dihydrochloride;BD1063 dhydrochloride;BD 1063 (hydrochloride);BD1063 2HCL
CAS号 : 206996-13-6
货号 : A725023
分子式 : C13H20Cl4N2
纯度 : 98%
分子量 : 346.123
MDL号 : MFCD00792740
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 100 mg/mL(288.91 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 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 BD-1063 dose dependently reduced ethanol self-administration in sP rats (3.3-11 mg/kg) and withdrawn, dependent Wistar rats (4-11 mg/kg) at doses that did not modify mean ethanol self-administration in nondependent Wistar controls.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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.89mL

0.58mL

0.29mL

14.45mL

2.89mL

1.44mL

28.89mL

5.78mL

2.89mL
参考文献

[1]Sabino V, Cottone P, Zhao Y, Iyer MR, Steardo L Jr, Steardo L, Rice KC, Conti B, Koob GF, Zorrilla EP. The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking. Neuropsychopharmacology. 2009 May;34(6):1482-93

[2]Cottone P, Wang X, Park JW, Valenza M, Blasio A, Kwak J, Iyer MR, Steardo L, Rice KC, Hayashi T, Sabino V. Antagonism of sigma-1 receptors blocks compulsive-like eating. Neuropsychopharmacology. 2012 Nov;37(12):2593-604

[3]Amer MS, McKeown L, Tumova S, Liu R, Seymour VA, Wilson LA, Naylor J, Greenhalgh K, Hou B, Majeed Y, Turner P, Sedo A, O'Regan DJ, Li J, Bon RS, Porter KE, Beech DJ. Inhibition of endothelial cell Ca²⁺ entry and transient receptor potential channels by Sigma-1 receptor ligands. Br J Pharmacol. 2013 Mar;168(6):1445-55

[4]Gaja-Capdevila N, Hernández N, Navarro X, Herrando-Grabulosa M. Sigma-1 Receptor is a Pharmacological Target to Promote Neuroprotection in the SOD1G93A ALS Mice. Front Pharmacol. 2021 Dec 10;12:780588