Description
BRL 52537 hydrochloride is a potent and selective agonist of κ/μ-opioid receptor with Ki value of 0.24 nM for κ-opioid receptor . The κ-opioid receptor (KOR) is a type of opioid receptor for opioid peptide dynorphin and controls addiction. Also, KOR plays an important role in stress, anxiety, anhedonia, depression and increased drug-seeking behavior. BRL 52537 hydrochloride is a potent and selective κ/μ-opioid receptor agonist. In the mouse tail flick model, BRL 52537 showed antinociception with ED50 value of 0.05 mg/kg, which was 25 times more potent than morphine . In WT male mice with middle cerebral artery occlusion, BRL 52537 significantly decreased infarct volumes at 72 h of reperfusion. However, BRL 52537 had no effect in neuronal NO synthase null mutants (nNOS-/-) mice or in the WT female mice. These results suggested that BRL 52537 exhibited neuroprotection through inhibition of ischemia-evoked NO production and nNOS activity . In adult rat dorsal root ganglia (DRGs), BRL 52537 inhibited tetrodotoxin-resistant (TTX-r) sodium currents in an opioid receptor-independent way, which also contributed to the antinociceptive effects . In rats with cerebral ischemia/reperfusion (I/R) injury, BRL52537 inhibited neuronal apoptosis and brain damage. Also, BRL52537 increased the level of phosphorylated STAT3 and reduced caspase-3 expression .
Product information
CAS Number: 112282-24-3
Molecular Weight: 391.76
Formula: C18H25Cl3N2O
Chemical Name: 2-(3,4-dichlorophenyl)-1-{2-[(pyrrolidin-1-yl)methyl]piperidin-1-yl}ethan-1-one hydrochloride
Smiles: Cl.O=C(CC1=CC(Cl)=C(Cl)C=C1)N1CCCCC1CN1CCCC1
InChiKey: NGVLSOWJSUUYDE-UHFFFAOYSA-N
InChi: InChI=1S/C18H24Cl2N2O.ClH/c19-16-7-6-14(11-17(16)20)12-18(23)22-10-2-1-5-15(22)13-21-8-3-4-9-21;/h6-7,11,15H,1-5,8-10,12-13H2;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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