|1-(3,4-二氯苯乙基)-4-甲基哌嗪二盐酸盐|CsnPharm

CAS No.: 206996-13-6

BD1063 dHCl/1-[2-(3,4-二氯苯基)乙基]-4-甲基哌嗪二盐酸盐 Catalog No. CSN24789

Synonyms: BD1063 dihydrochloride;,

BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.

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技术信息

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 BD-1063 dose dependently reduced ethanol self-administration in sP rats (3.3-11 mg/kg) and withdrawn, dependent Wistar rats (4-11 mg/kg) at doses that did not modify mean ethanol self-administration in nondependent Wistar controls.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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8891 mL
- 14.4457 mL
- 28.8914 mL
- 5 mM
- 0.5778 mL
- 2.8891 mL
- 5.7783 mL
- 10 mM
- 0.2889 mL
- 1.4446 mL
- 2.8891 mL

技术信息

CAS号

206996-13-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H20Cl4N2

运输

蓝冰

分子量

346.12

别名

BD1063 dihydrochloride;,

溶解度

DMSO	10.0 mg/mL (28.9 mM)
Water	68.0 mg/mL (196.5 mM)
Ethanol	2.0 mg/mL (5.8 mM)

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BD1063 dHCl/1-[2-(3,4-二氯苯基)乙基]-4-甲基哌嗪二盐酸盐 Catalog No. CSN24789

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