BRL-52537

BRL-52537
Systematic (IUPAC) name
2-(3,4-dichlorophenyl)-1-[(2S)-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethanone
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 130497-33-5
ATC code  ?
PubChem CID 6603740
Chemical data
Formula C18H24Cl2N2O 
Mol. mass 355.301 g/mol
SMILES eMolecules & PubChem
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BRL-52537 is a drug which acts as a potent and highly selective κ-opioid agonist.[1] It has neuroprotective effects in animal studies,[2][3] and is used for research into potential treatments for stroke and heart attack as well as more general brain research.[4][5][6]

References

  1. ^ Vecchietti V, Giordani A, Giardina G, Colle R, Clarke GD (January 1991). "(2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics". Journal of Medicinal Chemistry 34 (1): 397–403. doi:10.1021/jm00105a061. PMID 1846921. 
  2. ^ Goyagi T, Toung TJ, Kirsch JR, Traystman RJ, Koehler RC, Hurn PD, Bhardwaj A (June 2003). "Neuroprotective kappa-opioid receptor agonist BRL 52537 attenuates ischemia-evoked nitric oxide production in vivo in rats". Stroke; a Journal of Cerebral Circulation 34 (6): 1533–8. doi:10.1161/01.STR.0000072512.30658.E7. PMID 12738895. 
  3. ^ Zhang Z, Chen TY, Kirsch JR, Toung TJ, Traystman RJ, Koehler RC, Hurn PD, Bhardwaj A (December 2003). "Kappa-opioid receptor selectivity for ischemic neuroprotection with BRL 52537 in rats". Anesthesia and Analgesia 97 (6): 1776–83. PMID 14633559. 
  4. ^ Chen TY, Goyagi T, Toung TJ, Kirsch JR, Hurn PD, Koehler RC, Bhardwaj A (May 2004). "Prolonged opportunity for ischemic neuroprotection with selective kappa-opioid receptor agonist in rats". Stroke; a Journal of Cerebral Circulation 35 (5): 1180–5. doi:10.1161/01.STR.0000125011.93188.c6. PMID 15031456. 
  5. ^ Peart JN, Gross ER, Gross GJ (March 2004). "Effect of exogenous kappa-opioid receptor activation in rat model of myocardial infarction". Journal of Cardiovascular Pharmacology 43 (3): 410–5. PMID 15076225. 
  6. ^ Britt JP, McGehee DS (February 2008). "Presynaptic opioid and nicotinic receptor modulation of dopamine overflow in the nucleus accumbens". Journal of Neuroscience 28 (7): 1672–81. doi:10.1523/JNEUROSCI.4275-07.2008. PMID 18272687.