BD 1063 dihydrochloride

BD 1063 dihydrochloride

Catalog Number:
L002371732APE
Mfr. No.:
APE-B6489
Price:
$274
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Categories
          σ1 receptor antagonist, potent and selective
          Alternative Name
          1-(3,4-dichlorophenethyl)-4-methylpiperazine dihydrochloride
          CAS Number
          206996-13-6
          Molecular Formula
          C13H18Cl2N2·2HCl
          Molecular Weight
          346.13
          Appearance
          White solid
          Purity
          98.00%
          Solubility
          Soluble to 100 mM in sterile water
          Storage
          Store at RT
          SMILES
          CN(CC1)CCN1CCC2=CC(Cl)=C(Cl)C=C2.Cl.Cl

          * For Research Use Only

      • Reference
        • 1. Zhu J, Zang S, et al. "Involvement of the delayed rectifier outward potassium channel Kv2.1 in methamphetamine-induced neuronal apoptosis via the p38 mitogen-activated protein kinase signaling pathway." J Appl Toxicol. 2018 Jan 3. PMID:29297590

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