Naloksazon

Naloksazon
	(5α)-17-Alil-3,14-dihidroksi-4,5-epoksimorfinan-6-on hidrazon
Drugi nazivi	Nalokson- 6-hidrazon
Identifikacija
CAS registarski broj	73674-85-8
PubChem	9576788
ChEMBL	CHEMBL354010
Jmol-3D slike	Slika 1
SMILES
	C=CCN1CCC23C4C(=NN)CCC2(C1CC5=C3C(=C(C=C5)O)O4)O
Svojstva
Molekulska formula	C19H23N3O3
Molarna masa	341.4 g mol−1
	(šta je ovo?) (verifikuj) ; Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje (25 °C, 100 kPa) materijala
	Infobox references

Naloksazon je ireverzibilni antagonist μ opioidnog receptora, koji je selektivan za μ₁ receptorski podtip.^[4] Naloksazon ima dugotrajno antagonističko dejstvo, jer formira kovalentnu vezu na aktivnom mestu mi-opioidnog receptora,^[5] čime onemogućava drugim molekulima da se vežu za receptor, dok se konačno receptor ne reciklira putem endocitoze.

Poznato je da je naloksazon nestabilan u kiselim rastvorima, u kojima dolazi do dimerizacije u stabilniji i potentniji antagonist naloksonazin.^[6] U uslovima pod kojim dolazi do formiranja naloksonazina, naloksazon ne deluje kao ireverzibilni antagonist μ opioidnog receptora.^[6]

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.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ Pasternak GW, Childers SR, Snyder SH. "Opiate analgesia: evidence for mediation by a subpopulation of opiate receptors." Science. 1980 May 2; 208(4443):514-6. PMID 6245448. DOI:10.1126/science.6245448
↑ Ling, G. S.; Simantov, R.; Clark, J. A.; Pasternak, G. W. (1986-09-23). „Naloxonazine actions in vivo”. European Journal of Pharmacology 129 (1-2): 33–38. DOI:10.1016/0014-2999(86)90333-X. PMID 3021478. Pristupljeno 2011-10-18.
↑ ^6,0 ^6,1 Hahn, E. F.; Pasternak, G. W. (1982). „Naloxonazine, a potent, long-lasting inhibitor of opiate binding sites”. Life Sciences 31 (12-13): 1385–1388. DOI:10.1016/0024-3205(82)90387-3. PMID 6292633. Pristupljeno 2011-10-18.

Povezano

Hlornaltreksamin, ireverzibilni mešoviti agonist-antagonist
Oksimorfazon, ireverzibilni μ-opioidni pun agonist

[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] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[4] Pasternak GW, Childers SR, Snyder SH. "Opiate analgesia: evidence for mediation by a subpopulation of opiate receptors." Science. 1980 May 2; 208(4443):514-6. PMID 6245448. DOI:10.1126/science.6245448

[Ling-5] Ling, G. S.; Simantov, R.; Clark, J. A.; Pasternak, G. W. (1986-09-23). „Naloxonazine actions in vivo”. European Journal of Pharmacology 129 (1-2): 33–38. DOI:10.1016/0014-2999(86)90333-X. PMID 3021478. Pristupljeno 2011-10-18.

[Hahn-6] 6,0 ^6,1 Hahn, E. F.; Pasternak, G. W. (1982). „Naloxonazine, a potent, long-lasting inhibitor of opiate binding sites”. Life Sciences 31 (12-13): 1385–1388. DOI:10.1016/0024-3205(82)90387-3. PMID 6292633. Pristupljeno 2011-10-18.

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