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BRL-52537
- Development stage
- Discontinued
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Intravenous, Intrathecal
01
Overview
BRL-52537 is a potent and highly selective small molecule agonist of the κ-opioid receptor (KOR). Developed by GSK, it exhibits exceptional selectivity for κ-receptors over μ- and δ-opioid receptors, with a Ki of 0.24 nM for the κ subtype. In preclinical research, BRL-52537 has been investigated for its neuroprotective potential in models of ischemic stroke and cerebral ischemia, where it has demonstrated the ability to reduce infarct volume and attenuate ischemia-evoked nitric oxide production. Furthermore, studies have explored its impact on renal function, specifically its role in podocyte calcium handling and the potential for KOR/TRPC6 signaling to exacerbate kidney injury in hypertensive conditions. BRL-52537 is used exclusively as a pharmacological tool in research and is not approved for human therapeutic use.
- Other names
- (+/-)-1-(3,4-dichlorophenyl)acetyl-2-(1-pyrrolidinyl)methylpiperidineBRL-52537ABRL52537ABRL 52537A
02
Targets
KOR (Kappa opioid receptor)
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