Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
SYNTHESIS AND BIOLOGICAL-ACTIVITY OF THE PHOSPHATE AND SULFATE ESTERSOF NALOXONE AND NALTREXONE
Autore:
LAZAR S; JABBOURI S; MOISAND C; NOELHOCQUET S; MEUNIER JC; ROPARS C; GUILLAUMET G;
Indirizzi:
UNIV ORLEANS,CNRS,URA 499,CHIM BIOORGAN & ANALYT LAB,BP 6759 F-45067 ORLEANS 2 FRANCE NOVACELL,RECH & DEV PHARMACEUT F-37000 TOURS FRANCE CNRS,PHARMACOL & TOXICOL FONDAMENTALES LAB F-31077 TOULOUSE FRANCE
Titolo Testata:
European journal of medicinal chemistry
fascicolo: 1, volume: 29, anno: 1994,
pagine: 45 - 53
SICI:
0223-5234(1994)29:1<45:SABOTP>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG CEREBELLUM; OPIOID RECEPTOR; BINDING-SITES; SYSTEM; RABBIT; DRUGS; CELLS;
Keywords:
PHOSPHATE AND SULFATE ESTERS OF NALOXONE AND NALTREXONE; OPIATE ANTAGONISTS; MU- DELTA- AND KAPPA-OPIOID RECEPTORS; EQUILIBRIUM BINDING; ENCAPSULATION; RED BLOOD CELLS; METABOLIC STABILITY;
Tipo documento:
Note
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
S. Lazar et al., "SYNTHESIS AND BIOLOGICAL-ACTIVITY OF THE PHOSPHATE AND SULFATE ESTERSOF NALOXONE AND NALTREXONE", European journal of medicinal chemistry, 29(1), 1994, pp. 45-53

Abstract

Prodrugs of the two opiate antagonists naloxone and naltrexone, in particular the 3-monophosphate, 3-triphosphate, 9-monosulfate and 3,l4-disulfate eaters, have been synthesized and evaluated for: i) their ability to bind opioid receptors in vitro; and ii) their stability in both space and time upon entrapment into ex vivo human red blood cells (RBC). We find that, unlike the other esters, the mono- and triphosphateeaters of naloxone and naltrexone retain high (in the nmol range) affinities especially for mu- and kappa-opioid receptors. Owing to their hydrophilic nature, the two esters could possibly help in certain types of pharmacological experiments. Moreover, upon entrapment into humanRBC, the triphosphate esters of naloxone and naltrexone display considerable ex vivo intracellular stability.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/07/20 alle ore 00:41:23