RWJ-394,674

RWJ-394,674
(IUPAC) ime
	N,N-dietil-4-((8-fenetil-8-azabiciklo[3.2.1]okt-3-iliden)fenilmetil)benzamid
Klinički podaci
Identifikatori
ATC kod	nije dodeljen
PubChem	10205965
Hemijski podaci
Formula	C33H38N2O
Mol. masa	478,667 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C33H38N2O/c1-3-34(4-2)33(36)28-17-15-27(16-18-28)32(26-13-9-6-10-14-26)29-23-30-19-20-31(24-29)35(30)22-21-25-11-7-5-8-12-25/h5-18,30-31H,3-4,19-24H2,1-2H3 ; Key: ZJOPBPNTQRUJNM-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	Legalan

RWJ-394674 je lek koji se koristi u naučnim istraživanjima. On je potentan, oralno aktivan analgetik, koji uzrokuje neznatnu hipoventilaciju. RWJ-394674 je potentan i selektivan agonist δ-opioidnih receptora, sa Ki vrednošću od 0.24 nM na δ i 72 nM na μ. U telu se RWJ-394674 dealkilira do monodesetil metabolita RWJ-413216, koji je potentan agonist μ-opioidnog receptora i koji ima manji afinitet za δ (Ki 0.26 nM na μ, 46.7 nM na δ). RWJ-394674 in vivo proizvodi potentne agonistske efekte na oba, μ i δ, receptore putem kombinovanog dejstva leka i njegovog aktivnog metabolita, pri čemu δ-agonistni efekti suzbijaju hipoventilacione μ-opioidne efekte, i jedina značajna nuspojava je sedacija.^[3]

Literatura

↑ 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.
↑ Codd EE, Carson JR, Colburn RW, Dax SL, Desai-Krieger D, Martinez RP, McKown LA, Neilson LA, Pitis PM, Stahle PL, Stone DJ, Streeter AJ, Wu WN, Zhang SP. The novel, orally active, delta opioid RWJ-394674 is biotransformed to the potent mu opioid RWJ-413216. Journal of Pharmacology and Experimental Therapeutic. 2006 Sep;318(3):1273-9. PMID 16766719

Vanjske 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.

[3] Codd EE, Carson JR, Colburn RW, Dax SL, Desai-Krieger D, Martinez RP, McKown LA, Neilson LA, Pitis PM, Stahle PL, Stone DJ, Streeter AJ, Wu WN, Zhang SP. The novel, orally active, delta opioid RWJ-394674 is biotransformed to the potent mu opioid RWJ-413216. Journal of Pharmacology and Experimental Therapeutic. 2006 Sep;318(3):1273-9. PMID 16766719

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