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BD 1063 dihydrochloride Sale

(Synonyms: BD1063(盐酸盐)) 目录号 : GC15838

An antagonist of σ1 receptors

BD 1063 dihydrochloride Chemical Structure

Cas No.:206996-13-6

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10mg
¥990.00
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50mg
¥3,870.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

Rats: BD1063 is solubilized in isotonic saline and injected subcutaneously (s.c. 1 ml/kg), 15 min before testing. Rats are pretreated with BD1063 (0, 4.4, 7 and 11 mg/kg of body weight, free base weights, s.c.) using a within-subject Latin square design. sP rats: Rats are pretreated with BD1063 (0, 3, 4.4, 7 and 11 mg/kg of body weight, free base basis, s.c.) using a within-subject Latin square design[1].

References:

[1]. Sabino V, et al. 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, et al. Antagonism of sigma-1 receptors blocks compulsive-like eating. Neuropsychopharmacology. 2012 Nov;37(12):2593-604.
[3]. Nieto FR, et al. Role of sigma-1 receptors in paclitaxel-induced neuropathic pain in mice. J Pain. 2012 Nov;13(11):1107-21.

产品描述

BD 1063 dihydrochloride is an antagonist of σ-1 receptor with Ki value of 9.15 nM [1].

σ-receptor is a type of opioid receptor. There are two subtypes of σ-receptor: σ-1 and σ-2.σ-1 receptor plays an important role in stimulating dopamine release and modulating the actions of cocaine [2].

BD 1063 dihydrochloride is a σ-1 receptor antagonist with Ki values of 9.15 and 449 nM for σ-1 receptor and σ-2 receptor, respectively. BD1063 reduced the dystonia induced by haloperidol and di-o-tolylguanidine (DTG) in a dose-dependent way [1].

In mice, BD1063 inhibited up-regulation of fra-2 and σ-1 receptor induced by cocaine in whole brain, cortex and striatum [2]. In mice, BD1063 significantly inhibited convulsions, lethality and locomotor stimulatory effects induced by cocaine [3]. In two excessive drinking rat models, BD-1063 reduced ethanol self-administration in a dose-dependent way and inhibited the expression of σ-1 receptor in the nucleus accumbens [4]. In mice, BD-1063 reversed thermal (radiant heat) hyperalgesia and inflammatory mechanical (paw pressure) in a dose-dependent way. However, BD-1063 had no effect on thermal hyperalgesia in σ1 knockout (σ1-KO) mice. These results suggested that σ1 receptor played an important role in inflammatory hyperalgesia [5].

References:
[1].  Matsumoto RR, Bowen WD, Tom MA, et al. Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism. Eur J Pharmacol, 1995, 280(3): 301-310.
[2].  Liu Y, Chen GD, Lerner MR, et al. Cocaine up-regulates Fra-2 and sigma-1 receptor gene and protein expression in brain regions involved in addiction and reward. J Pharmacol Exp Ther, 2005, 314(2): 770-779.
[3].  Matsumoto RR, McCracken KA, Friedman MJ, et al. Conformationally restricted analogs of BD1008 and an antisense oligodeoxynucleotide targeting sigma1 receptors produce anti-cocaine effects in mice. Eur J Pharmacol, 2001, 419(2-3): 163-174.
[4].  Sabino V, Cottone P, Zhao Y, et al. The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking. Neuropsychopharmacology, 2009, 34(6): 1482-1493.
[5].  Tejada MA, Montilla-García A, Sánchez-Fernández C, et al. Sigma-1 receptor inhibition reverses acute inflammatory hyperalgesia in mice: role of peripheral sigma-1 receptors. Psychopharmacology (Berl), 2014, 231(19): 3855-3869.

Chemical Properties

Cas No. 206996-13-6 SDF
别名 BD1063(盐酸盐)
化学名 1-(3,4-dichlorophenethyl)-4-methylpiperazine dihydrochloride
Canonical SMILES CN(CC1)CCN1CCC2=CC(Cl)=C(Cl)C=C2.Cl.Cl
分子式 C13H18Cl2N2.2HCl 分子量 346.13
溶解度 DMF: 11 mg/ml,DMSO: 16 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 10 mg/ml 储存条件 Store at RT
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1 mM 2.8891 mL 14.4454 mL 28.8909 mL
5 mM 0.5778 mL 2.8891 mL 5.7782 mL
10 mM 0.2889 mL 1.4445 mL 2.8891 mL
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