GR-89696

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	3505
Hemijski podaci
Formula	C19H25Cl2N3O3
Mol. masa	414.325 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H25Cl2N3O3/c1-27-19(26)23-8-9-24(15(13-23)12-22-6-2-3-7-22)18(25)11-14-4-5-16(20)17(21)10-14/h4-5,10,15H,2-3,6-9,11-13H2,1H3 ; Key: HJUAKZYKCANOOZ-UHFFFAOYSA-N
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

↑ 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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. 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.

[pmid8393489-3] 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.

[pmid8220893-4] 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.

[pmid9103490-5] 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.

[pmid11504802-6] 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.

[pmid18842704-7] 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. DOI:10.1124/jpet.108.143925. PMC 2719014. PMID 18842704.

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