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BRL-52537

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
BRL-52537
Identifiers
  • 2-(3,4-dichlorophenyl)-1-[(2S)-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethanone
CAS Number
PubChemCID
ChemSpider
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC18H24Cl2N2O
Molar mass355.30 g·mol−1
3D model (JSmol)
  • C1CCN([C@@H](C1)CN2CCCC2)C(=O)CC3=CC(=C(C=C3)Cl)Cl
  • InChI=1S/C18H24Cl2N2O/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/t15-/m0/s1 ☒N
  • Key:GHCCBWMZKJQGLS-HNNXBMFYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

BRL-52537 is a drug which acts as a potent and highly selectiveκ-opioidagonist.[1] It hasneuroprotective effects in animal studies,[2][3] and is used for research into potential treatments forstroke andheart attack as well as more general brain research.[4][5][6]

References

[edit]
  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.doi:10.1213/01.ane.0000087800.56290.2e.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.doi:10.1097/00005344-200403000-00012.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.PMC 6671549.PMID 18272687.
μ-opioid
(MOR)
Agonists
(abridged;
full list)
Antagonists
δ-opioid
(DOR)
Agonists
Antagonists
κ-opioid
(KOR)
Agonists
Antagonists
Nociceptin
(NOP)
Agonists
Antagonists
Others


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