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BD 1047 dihydrobromide structure, CAS 138356-21-5

BD 1047 dihydrobromide

CAS Number138356-21-5

SynonymsN'-[2-(3,4-dichlorophenyl)ethyl]-N,N,N'-trimethylethane-1,2-diamine,dihydrobromide; BD1047.2HBr; BD-1047 (dihydrobromide)

Molecular FormulaC13H22Br2Cl2N2

Molecular Weight437.04100

Purity

Density

Boiling Point

Melting Point

Flash Point

Appearancewhite powder

EINECS

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Cat. No.: 2A-1170348 Purity:
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Chemical & Physical Properties
CAS Number138356-21-5
Catalog No.2A-1170348
Chinese NameBD-1047
SynonymsN'-[2-(3,4-dichlorophenyl)ethyl]-N,N,N'-trimethylethane-1,2-diamine,dihydrobromide; BD1047.2HBr; BD-1047 (dihydrobromide)
Molecular FormulaC13H22Br2Cl2N2
Molecular Weight437.04100
Appearancewhite powder
Storage Condition2-8°C
ApplicationBD-1047 dihydrobromide is a sigma receptor selective antagonist that acts on animal models of schizophrenia and has antipsychotic activity.
PubChem ID91746260
SMILESBr.Br.CN(C)CCN(C)CCc1ccc(Cl)c(Cl)c1
InChIInChI=1S/C13H20Cl2N2.2BrH/c1-16(2)8-9-17(3)7-6-11-4-5-12(14)13(15)10-11;;/h4-5,10H,6-9H2,1-3H3;2*1H
InChI KeyWOALTFHGLDVJHK-UHFFFAOYSA-N
MSDSmsds/170499_2_138356_21_5.pdf
BioactivityBD-1047 dihydrobromide is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. IC50 value: Target: sigma receptorin vitro: Moreover, Progesterone and BD 1047 (a sigma 1 receptor antagonist) counteracted the antidepressant-like effect induced by co-administration of Pramipexole and Sertraline (but not Pramipexole and Fluoxetine). [2] This increased pNR1 expression is significantly reduced by pretreatment with the specific Sig-1 R antagonist, BD-1047. In another set of experiments Sig-1 R agonists further potentiated NMDA-induced pain behaviour and pNR1 immunoreactivity and this is also reversed with BD-1047. [3]in vivo: BD 1047 does not decrease amphetamine-induced hyperactivity in mice in a statistically significant manner. BD 1047 does not modify the hyperactivity induced by NMDA receptor antagonists. BD 1047 shows a moderate activity in models used in this study suggesting that its usefulness as an antipsychtic drug is doubtful. [1] Related Catalog Signaling Pathways >> GPCR/G Protein >> Sigma Receptor Research Areas >> Neurological Disease References [1]. Skuza G, et al. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep. 2006 Sep-Oct;58(5):626-635. [2]. Rogóz Z, et al. Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats. Pharmacol Rep. 2006 Jul-Aug;58(4):493-500. [3]. Kim HW, et al. Activation of the spinal sigma-1 receptor enhances NMDA-induced pain via PKC- and PKA-dependent phosphorylation of the NR1 subunit in mice. Br J Pharmacol. 2008 Jul;154(5):1125-1134. Chemical & Physical Properties Molecular Formula C13H22Br2Cl2N2 Molecular Weight 437.04100 Exact Mass 433.95300 PSA 6.48000 LogP 4.94550 InChIKey WOALTFHGLDVJHK-UHFFFAOYSA-N SMILES Br.Br.CN(C)CCN(C)CCc1ccc(Cl)c(Cl)c1 Storage condition 2-8°C
Use ofBD-1047 dihydrobromide is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. IC50 value: Target: sigma receptorin vitro: Moreover, Progesterone and BD 1047 (a sigma 1 receptor antagonist) counteracted the antidepressant-like effect induced by co-administration of Pramipexole and Sertraline (but not Pramipexole and Fluoxetine). [2] This increased pNR1 expression is significantly reduced by pretreatment with the specific Sig-1 R antagonist, BD-1047. In another set of experiments Sig-1 R agonists further potentiated NMDA-induced pain behaviour and pNR1 immunoreactivity and this is also reversed with BD-1047. [3]in vivo: BD 1047 does not decrease amphetamine-induced hyperactivity in mice in a statistically significant manner. BD 1047 does not modify the hyperactivity induced by NMDA receptor antagonists. BD 1047 shows a moderate activity in models used in this study suggesting that its usefulness as an antipsychtic drug is doubtful. [1] Properties Name BD 1047 dihydrobromide Synonym More Synonyms BD 1047 dihydrobromide Biological Activity Description BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. IC50 value: Target: sigma receptorin vitro: Moreover, Progesterone and BD 1047 (a sigma 1 receptor antagonist) counteracted the antidepressant-like effect induced by co-administration of Pramipexole and Sertraline (but not Pramipexole and Fluoxetine). [2] This increased pNR1 expression is significantly reduced by pretreatment with the specific Sig-1 R antagonist, BD-1047. In another set of experiments Sig-1 R agonists further potentiated NMDA-induced pain behaviour and pNR1 immunoreactivity and this is also reversed with BD-1047. [3]in vivo: BD 1047 does not decrease amphetamine-induced hyperactivity in mice in a statistically significant manner. BD 1047 does not modify the hyperactivity induced by NMDA receptor antagonists. BD 1047 shows a moderate activity in models used in this study suggesting that its usefulness as an antipsychtic drug is doubtful. [1] Related Catalog Signaling Pathways >> GPCR/G Protein >> Sigma Receptor Research Areas >> Neurological Disease References [1]. Skuza G, et al. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep. 2006 Sep-Oct;58(5):626-635. [2]. Rogóz Z, et al. Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats. Pharmacol Rep. 2006 Jul-Aug;58(4):493-500. [3]. Kim HW, et al. Activation of the spinal sigma-1 receptor enhances NMDA-induced pain via PKC- and PKA-dependent phosphorylation of the NR1 subunit in mice. Br J Pharmacol. 2008 Jul;154(5):1125-1134. Chemical & Physical Properties Exact Mass 433.95300 PSA 6.48000 LogP 4.94550 InChIKey WOALTFHGLDVJHK-UHFFFAOYSA-N
Transport InfoProduct name: BD 1047 dihydrobromide
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