| Identification | Back Directory | [Name]
1-[2-(3,4-Dichlorophenyl)ethyl]-4-Methylpiperazine Dihydrochloride | [CAS]
206996-13-6 | [Synonyms]
BD1063 HCl
BD1063 (dhydrochloride)
BD 1063 (hydrochloride)
BD-1063 DHYDROCHLORIDE; BD 1063 DHYDROCHLORIDE | [Molecular Formula]
C13H20Cl4N2 | [MDL Number]
MFCD00792740 | [MOL File]
206996-13-6.mol | [Molecular Weight]
346.123 |
| Chemical Properties | Back Directory | [storage temp. ]
room temp | [solubility ]
H2O: >15mg/mL | [form ]
powder | [color ]
white to beige | [Water Solubility ]
Soluble to 100 mM in water | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
BD1063 (206996-13-6) is potent and selective sigma-1 antagonist (IC50’s: σ1 = 9nM, σ2 = 449nM).1?BD1063 abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute inflammation by enhancing the action of endogenous opioid peptides of immune origin in a σ1 dependent manner.2?BD1063 potentiated μ-opioid antinociception in mice in a sigma-dependent manner.3?BD-1063 has been used in animal models to successfully treat compulsive eating4?and excessive ethanol drinking5. | [Chemical Properties]
White Solid | [Uses]
The novel σ receptor ligands | [Biochem/physiol Actions]
BD 1063 is a potent sigma(1) receptor antagonist; approximately 50-fold selective for sigma-1 over sigma-2 and 100-fold or more selective over 9 other tested neurotransmitter receptors. BD 1063 has been shown to antagonize cocaine efffects. | [in vivo]
BD1063 dose-dependently reduces ethanol self-administration in sP rats (3.3-11 mg/kg) and withdrawn, dependent Wistar rats (4-11 mg/kg) at doses that does not modify mean ethanol self-administration in non-dependent Wistar controls. BD1063 also reduces the breakpoints of sP rats to work for ethanol under a progressive-ratio reinforcement schedule. BD1063 dose-dependently reduces binge-like eating and the regularity of food responding, and blocks the increased eating rate in Palatable rats. In the light/dark conflict test, BD1063 antagonizes the increased time spent in the aversive compartment and the increased intake of the palatable diet, without affecting motor activity. The administration of BD1063 30 minutes before each paclitaxel dose prevents the development of cold and mechanical allodynia in WT mice. Moreover, the acute administration of BD1063 dose dependently reverses both types of paclitaxel-induced allodynia. | [storage]
Store at RT | [References]
1) Matsumoto?et al.?(1995),?Characterization of two novel σ receptor ligands: antidystonic effects in rats suggest &sigma receptor antagonism; Eur. J. Pharmacol.?280?301
2) Tejada?et al.?(2017),?Sigma-1 receptors control immune-driven peripheral opioid analgesia during inflammation in mice; Proc. Natl. Acad. Sci. USA?114?8396
3) Sanchez-Fernandez?et al.?(2014),?Modulation of peripheral μ-opioid analgesia by σ1 receptors; J. Pharmacol. Exp. Ther.?348?32
4) Cottone?et al.?(2012),?Antagonism of sigma-1 receptors blocks compulsive-like eating; Neuropsychopharmaology?37?2593
5) Sabino?et al.?(2009),?The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking; Neuropsychopharmaology?34?1482 |
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| Company Name: |
Sigma-Aldrich
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021-61415566 800-8193336 |
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https://www.sigmaaldrich.cn |
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