BD1063 dhydrochloride - CAS 206996-13-6
Category: Inhibitor
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Sigma Receptor
BD1063 dhydrochloride is a potent and selective antagonist of sigma 1 receptor(Ki= 9.15 nM)with 50-fold more selective over sigma-2(Ki= 449 nM) and >100-fold more selective over 9 other tested neurotransmitter receptors.
Brife Description:
A potent and selective antagonist of sigma 1 receptor (Ki= 9.15 nM)
BD1063 dhydrochloride; BD 1063 dhydrochloride; BD-1063 dhydrochloride1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine;dihydrochloride
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.Modulation of peripheral μ-opioid analgesia by σ1 receptors.
Sánchez-Fernández C;Montilla-García Á;González-Cano R;Nieto FR;Romero L;Artacho-Cordón A;Montes R;Fernández-Pastor B;Merlos M;Baeyens JM;Entrena JM;Cobos EJ J Pharmacol Exp Ther. 2014 Jan;348(1):32-45. doi: 10.1124/jpet.113.208272. Epub 2013 Oct 23.
We evaluated the effects of σ1-receptor inhibition on μ-opioid-induced mechanical antinociception and constipation. σ1-Knockout mice exhibited marked mechanical antinociception in response to several μ-opioid analgesics (fentanyl, oxycodone, morphine, buprenorphine, and tramadol) at systemic (subcutaneous) doses that were inactive in wild-type mice and even unmasked the antinociceptive effects of the peripheral μ-opioid agonist loperamide. Likewise, systemic (subcutaneous) or local (intraplantar) treatment of wild-type mice with the selective σ1 antagonists BD-1063 [1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine dihydrochloride] or S1RA [4-[2-[[5-methyl-1-(2-naphthalenyl)1H-pyrazol-3-yl]oxy]ethyl] morpholine hydrochloride] potentiated μ-opioid antinociception; these effects were fully reversed by the σ1 agonist PRE-084 [2-(4-morpholinethyl)1-phenylcyclohexanecarboxylate) hydrochloride], showing the selectivity of the pharmacological approach. The μ-opioid antinociception potentiated by σ1 inhibition (by σ1-receptor knockout or σ1-pharmacological antagonism) was more sensitive to the peripherally restricted opioid antagonist naloxone methiodide than opioid antinociception under normal conditions, indicating a key role for peripheral opioid receptors in the enhanced antinociception.
2.A presynaptic action of the neurosteroid pregnenolone sulfate on GABAergic synaptic transmission.
Mtchedlishvili Z;Kapur J Mol Pharmacol. 2003 Oct;64(4):857-64.
The endogenous neurosteroid pregnenolone sulfate (PS) is known to enhance memory and cognitive function at nanomolar concentrations. However, the effect of these low concentrations on synaptic transmission has not been previously studied. The effects of PS on GABAA receptor-mediated inhibitory postsynaptic currents were studied in cultured hippocampal pyramidal neurons. Concentrations of PS similar to those endogenous in the hippocampus (10-30 nM) reduced the frequency of both action potential-dependent (spontaneous inhibitory postsynaptic current) and -independent (miniature inhibitory postsynaptic current; mIPSC) inhibitory postsynaptic currents. This effect of PS was mimicked by the selective sigma1 receptor agonist [2S-(2alpha,6alpha,11R]-1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(2-propenyl)-2,6-methano-3-benzazocin-8-ol hydrochloride [(+)-SKF 10047] and blocked the specific sigma1 receptor antagonists 1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine dihydrochloride (BD-1063) and haloperidol and by pertussis toxin. The GABAB antagonist baclofen and the metabotropic glutamate receptor antagonist (R,S)-a-cyclopropyl-4-phosphonophenylglycine had no effect on the PS-mediated inhibition of mIPSC frequency.
3.Sigma-1 receptor antagonism restores injury-induced decrease of voltage-gated Ca2+ current in sensory neurons.
Pan B;Guo Y;Kwok WM;Hogan Q;Wu HE J Pharmacol Exp Ther. 2014 Aug;350(2):290-300. doi: 10.1124/jpet.114.214320. Epub 2014 Jun 2.
Sigma-1 receptor (σ1R), an endoplasmic reticulum-chaperone protein, can modulate painful response after peripheral nerve injury. We have demonstrated that voltage-gated calcium current is inhibited in axotomized sensory neurons. We examined whether σ1R contributes to the sensory dysfunction of voltage-gated calcium channel (VGCC) after peripheral nerve injury through electrophysiological approach in dissociated rat dorsal root ganglion (DRG) neurons. Animals received either skin incision (Control) or spinal nerve ligation (SNL). Both σ1R agonists, (+)pentazocine (PTZ) and DTG [1,3-di-(2-tolyl)guanidine], dose dependently inhibited calcium current (ICa) with Ba(2+) as charge carrier in control sensory neurons. The inhibitory effect of σ1R agonists on ICa was blocked by σ1R antagonist, BD1063 (1-[2-(3,4-dichlorophenyl)ethyl]-4-m​ethylpiperazine dihydrochloride) or BD1047 (N-[2-(3,4-dichlorophenyl)ethyl]-N-m​ethyl-2-(dimethylamino)ethylamine dihydrobromide). PTZ and DTG showed similar effect on ICa in axotomized fifth DRG neurons (SNL L5). Both PTZ and DTG shifted the voltage-dependent activation and steady-state inactivation of VGCC to the left and accelerated VGCC inactivation rate in both Control and axotomized L5 SNL DRG neurons.
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CAS 206996-13-6 BD1063 dhydrochloride

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