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GR 89696 fumarate (CAS 126766-32-3)

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Alternate Names:
GR 89696
Application:
GR 89696 fumarate is a subtype-selective KOR (κ-opioid receptor) agonist
CAS Number:
126766-32-3
Molecular Weight:
530.4
Molecular Formula:
C19H25Cl2N3O3•C4H4O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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GR 89696 fumarate is a highly potent subtype-selective KOR (κ-opioid receptor) agonist with an IC50 = 0.04 nM.


GR 89696 fumarate (CAS 126766-32-3) References

  1. Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functional studies.  |  Soukara, S., et al. 2001. J Med Chem. 44: 2814-26. PMID: 11495592
  2. GR89,696: a potent kappa-opioid agonist with subtype selectivity in rhesus monkeys.  |  Butelman, ER., et al. 2001. J Pharmacol Exp Ther. 298: 1049-59. PMID: 11504802
  3. Induction of bladder sphincter dyssynergia by kappa-2 opioid receptor agonists in the female rat.  |  Gu, B., et al. 2004. J Urol. 171: 472-7. PMID: 14665958
  4. Sex related differences in analgesia in sheep (Ovis ovis).  |  Cook, CJ. 1997. N Z Vet J. 45: 169-70. PMID: 16031979
  5. Steroidal hormones determine sex-related differences in opioid-induced elevation of nociceptive threshold in sheep (Ovis aries).  |  Cook, CJ. 1998. N Z Vet J. 46: 68-71. PMID: 16032019
  6. Neuroprotective actions of GR89696, a highly potent and selective kappa-opioid receptor agonist.  |  Birch, PJ., et al. 1991. Br J Pharmacol. 103: 1819-23. PMID: 1657267
  7. [Role of kappa-opioid receptors in the regulation of cardiac resistance to arrhythmogenic effects of ischemia and reperfusion].  |  Lishmanov, AIu., et al. 2006. Ross Fiziol Zh Im I M Sechenova. 92: 1419-28. PMID: 17523463
  8. Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates.  |  Ko, MC. and Husbands, SM. 2009. J Pharmacol Exp Ther. 328: 193-200. PMID: 18842704
  9. Myocardial resistance to ischemic and reperfusion injuries under conditions of chronic administration of opioid receptor agonists and antagonists.  |  Lishmanov, YB., et al. 2008. Bull Exp Biol Med. 145: 696-9. PMID: 19110553
  10. Comparative analysis of the cardioprotective properties of opioid receptor agonists in a rat model of myocardial infarction.  |  Maslov, LN., et al. 2010. Acad Emerg Med. 17: 1239-46. PMID: 21175523
  11. Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.  |  Molenveld, P., et al. 2015. Bioorg Med Chem Lett. 25: 5326-30. PMID: 26411794
  12. Dynorphin-Dependent Reduction of Excitability and Attenuation of Inhibitory Afferents of NPS Neurons in the Pericoerulear Region of Mice.  |  Jüngling, K., et al. 2016. Front Cell Neurosci. 10: 61. PMID: 27013974
  13. Role of dorsal hippocampus κ opioid receptors in contextual aversive memory consolidation in rats.  |  Vanz, F., et al. 2018. Neuropharmacology. 135: 253-267. PMID: 29499274
  14. Comparative Analysis of Infarct Size Limiting Activity of κ-Opioid Receptor Agonists in In Vivo Reperfused Heart.  |  Mukhomedzyanov, AV., et al. 2021. Bull Exp Biol Med. 170: 594-597. PMID: 33792817
  15. A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.  |  Naylor, A., et al. 1993. J Med Chem. 36: 2075-83. PMID: 8393489

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

GR 89696 fumarate, 10 mg

sc-203982
10 mg
$188.00

GR 89696 fumarate, 50 mg

sc-203982A
50 mg
$774.00