BD 1063 dihydrochloride |
| Katalog-Nr.GC15838 |
BD 1063 Dihydrochlorid ist ein potenter und selektiver Sigma-1-Rezeptorantagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 206996-13-6
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 206996-13-6 | SDF | |
| Chemical Name | 1-(3,4-dichlorophenethyl)-4-methylpiperazine dihydrochloride | ||
| Canonical SMILES | CN(CC1)CCN1CCC2=CC(Cl)=C(Cl)C=C2.Cl.Cl | ||
| Formula | C13H18Cl2N2.2HCl | M.Wt | 346.13 |
| Löslichkeit | DMF: 11 mg/ml,DMSO: 16 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 10 mg/ml | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8891 mL | 14.4454 mL | 28.8909 mL |
| 5 mM | 577.8 μL | 2.8891 mL | 5.7782 mL |
| 10 mM | 288.9 μL | 1.4445 mL | 2.8891 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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