GR-89696

GR-89696
IUPAC ime
methyl 4-[2-(3,4-dichlorophenyl)acetyl]-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate
Identifikatori
CAS broj126766-32-3 ДаY
PubChemCID 3505
Hemijski podaci
FormulaC19H25Cl2N3O3
Molarna masa414.325 g/mol
  • Clc1ccc(cc1Cl)CC(=O)N2CCN(C(=O)OC)CC2CN3CCCC3

GR-89696 je lek koji deluje kao visoko selektivni κ-opioidni agonist.[1] On pokazuje selektivno dejstvo u različitim životinjskim modelima, i smatra se da je on selektivan za κ2 tip receptora.[2][3][4] Nedavne studije indiciraju da su GR-89696 i srodni κ2-selektivni agonisti korisni u sprečavanju svrabeža koji je uobičajena nuspojava konvencionalnih opioidnih analgetika, bez dodatnih nuspojava ne-selektivnih kapa agonista.[5]

Reference

  1. ^ Naylor A, Judd DB, Lloyd JE, Scopes DI, Hayes AG, Birch PJ (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. PMID 8393489. 
  2. ^ Herrero JF, Headley PM (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 Слободан приступ. PMID 8220893. 
  3. ^ Ho J, Mannes AJ, Dubner R, Caudle RM (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 (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 (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. PMC 2719014 Слободан приступ. PMID 18842704. doi:10.1124/jpet.108.143925. 

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