GR-89696

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GR-89696
(IUPAC) ime
methyl 4-[2-(3,4-dichlorophenyl)acetyl]-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate
Klinički podaci
Identifikatori
CAS broj 126766-32-3
ATC kod  ?
PubChem[1][2] 3505
Hemijski podaci
Formula C19H25Cl2N3O3 
Mol. masa 414.325 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

GR-89696 je lek koji deluje kao visoko selektivni κ-opioidni agonist.[3] On pokazuje selektivno dejstvo u različitim životinjskim modelima, i smatra se da je on selektivan za κ2 tip receptora.[4][5][6] 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.[7]

Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. 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. PMID 8393489. 
  4. 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. 
  5. 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. 
  6. 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. 
  7. 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. PMC 2719014. PMID 18842704. doi:10.1124/jpet.108.143925. 

Spoljašnje veze[uredi - уреди | uredi izvor]


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