ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors BD 1047 dihydrobromide

BD 1047 dihydrobromide

Product NameBD 1047 dihydrobromide
CAS138356-21-5
MFC13H22Br2Cl2N2
MW437.04118
EINECS
MOL File138356-21-5.mol

Chemical Properties

storage temp.	Inert atmosphere,2-8°C
solubility	H2O: >5mg/mL
form	powder
color	white
Water Solubility	H2O: >5mg/mL
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
InChI	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
InChIKey	WOALTFHGLDVJHK-UHFFFAOYSA-N
SMILES	Br.Br.CN(C)CCN(C)CCc1ccc(Cl)c(Cl)c1

Safety Information

Hazard Codes	Xi
Risk Statements	37/38-41
Safety Statements	26-36/37
WGK Germany	3
Storage Class	11 - Combustible Solids
Hazard Classifications	Eye Dam. 1 Skin Irrit. 2 STOT SE 3

Usage And Synthesis

Description

BD 1047 is a selective antagonist of sigma-1 (σ₁) receptors (K_i = 0.9 nM in a radioligand binding assay). It is selective for σ₁ receptors with binding affinity values greater than 10,000 nM for human recombinant dopamine, opioid, PCP, and serotonin receptors in vitro. In vivo, pretreatment with BD 1047 protects against convulsions and lethality induced by cocaine (Item Nos. 16186 | ISO60176) and reduces cocaine-induced locomotor activity. It reduces dystonias induced by the σ receptor agonists haloperidol and di-o-tolylguanidine (DTG) in rats in a dose-dependent manner. In vivo administration of BD 1047 also attenuates mechanical allodynia and microglial activation in a rat model of bone cancer pain.

Uses

BD 1047 dihydrobromide is an σ1 receptor antagonist with higher affinity than BD 1063.

in vivo

BD-1047 (dihydrobromide) (1-10 mg/kg; i.p.) decreases the Apomorphine (APO)-induced climbing behavior at the dose of 10 mg/kg in mice^[1].
BD-1047 (dihydrobromide) counteracts the antidepressant-like effect induced by co-administration of pramipexole and sertraline (but not pramipexole and fluoxetine)^[3].
BD-1047 (dihydrobromide) reduces the increasing expression of pNR1, and reverses the Sig-1 R agonists potentiated NMDA-induced pain behaviour and pNR1 immunoreactivity^[4].

Animal Model:	Male Albino Swiss mice (50 days old, 25–28 g)^[1]
Dosage:	1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:	Intraperitoneal injection
Result:	Decreased the APO-induced climbing at the dose of 10 mg/kg in mice.

IC 50

Sigma 1 Receptor

storage

Desiccate at +4°C

References

[1] RAE R. MATSUMOTO . Characterization of two novel σ receptor ligands: antidystonic effects in rats suggest σ receptor antagonism[J]. European journal of pharmacology, 1995, 280 3: Pages 301-310. DOI:10.1016/0014-2999(95)00208-3
[2] KARI A. MCCRACKEN . Two novel σ receptor ligands, BD1047 and LR172, attenuate cocaine-induced toxicity and locomotor activity[J]. European journal of pharmacology, 1999, 370 3: Pages 225-232. DOI:10.1016/s0014-2999(99)00113-2
[3] TIEYING SONG. Role of sigma 1 receptor in high fat diet-induced peripheral neuropathy.[J]. Biological Chemistry, 2017, 398 10: 1141-1149. DOI:10.1515/hsz-2017-0117
[4] YOUNG CHAN JEONG Young B K Ji Seon Son. The spinal antinociceptive mechanism determined by systemic administration of BD1047 in zymosan-induced hyperalgesia in rats[J]. Brain Research Bulletin, 2015, 119: Pages 93-100. DOI:10.1016/j.brainresbull.2015.07.006
[5] DAE-HYUN ROH S Y Y. Sigma-1 receptor antagonist, BD1047 reduces nociceptive responses and phosphorylation of p38 MAPK in mice orofacial formalin model.[J]. Accounts of Chemical Research, 2014: 145-151. DOI:10.1248/bpb.b13-00690
[6] SHANSHAN ZHU. Sigma-1 Receptor Antagonist BD1047 Reduces Mechanical Allodynia in a Rat Model of Bone Cancer Pain through the Inhibition of Spinal NR1 Phosphorylation and Microglia Activation.[J]. Mediators of Inflammation, 2015, 2015 1: 265056. DOI:10.1155/2015/265056

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