GR-89696

GR-89696
Systematic (IUPAC) name
methyl 4-[2-(3,4-dichlorophenyl)acetyl]-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 126766-32-3 Y
ATC code  ?
PubChem CID 3505
ChEMBL CHEMBL277863 N
Chemical data
Formula C19H25Cl2N3O3 
Mol. mass 414.325 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

GR-89696 is a drug which acts as a highly selective κ-opioid agonist.[1] It shows selective effects in different animal models and it is thought it may be a subtype-selective agonist for the κ2 subtype.[2][3][4] Recent studies have suggested that GR-89696 and related κ2-selective agonists may be useful for preventing the itching which is a common side effect of conventional opioid analgesic drugs, without the additional side effects of non-selective kappa agonists.[5]

References

  1. ^ Naylor A, Judd DB, Lloyd JE, Scopes DI, Hayes AG, Birch PJ (July 1993). "A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines". Journal of Medicinal Chemistry 36 (15): 2075–83. doi:10.1021/jm00067a004. PMID 8393489. 
  2. ^ Herrero JF, Headley PM (September 1993). "Functional evidence for multiple receptor activation by kappa-ligands in the inhibition of spinal nociceptive reflexes in the rat". British Journal of Pharmacology 110 (1): 303–9. PMC 2176008. PMID 8220893. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2176008. 
  3. ^ Ho J, Mannes AJ, Dubner R, Caudle RM (April 1997). "Putative kappa-2 opioid agonists are antihyperalgesic in a rat model of inflammation". The Journal of Pharmacology and Experimental Therapeutics 281 (1): 136–41. PMID 9103490. 
  4. ^ Butelman ER, Ko MC, Traynor JR, Vivian JA, Kreek MJ, Woods JH (September 2001). "GR89,696: a potent kappa-opioid agonist with subtype selectivity in rhesus monkeys". The Journal of Pharmacology and Experimental Therapeutics 298 (3): 1049–59. PMID 11504802. 
  5. ^ Ko MC, Husbands SM (January 2009). "Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates". The Journal of Pharmacology and Experimental Therapeutics 328 (1): 193–200. doi:10.1124/jpet.108.143925. PMC 2719014. PMID 18842704. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2719014.