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Titolo:
PHARMACOLOGICAL PROFILE OF ANTIDEPRESSANTS AND RELATED-COMPOUNDS AT HUMAN MONOAMINE TRANSPORTERS
Autore:
TATSUMI M; GROSHAN K; BLAKELY RD; RICHELSON E;
Indirizzi:
MAYO CLIN JACKSONVILLE,4500 SAN PABLO RD JACKSONVILLE FL 32224 MAYO CLIN JACKSONVILLE JACKSONVILLE FL 32224 SHOWA UNIV,SCH MED,DEPT PSYCHIAT TOKYO 142 JAPAN VANDERBILT UNIV,SCH MED,DEPT PHARMACOL NASHVILLE TN 37232
Titolo Testata:
European journal of pharmacology
fascicolo: 2-3, volume: 340, anno: 1997,
pagine: 249 - 258
SICI:
0014-2999(1997)340:2-3<249:PPOAAR>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN DOPAMINE TRANSPORTER; RAT-BRAIN SYNAPTOSOMES; HUMAN SEROTONIN TRANSPORTER; BIOGENIC-AMINE UPTAKE; NOREPINEPHRINE UPTAKE; BINDING; COCAINE; CLONING; CELLS; NORADRENALINE;
Keywords:
5-HT (5-HYDROXYTRYPTAMINE, SEROTONIN) TRANSPORTER, HUMAN; NOREPINEPHRINE TRANSPORTER, HUMAN; DOPAMINE TRANSPORTER, HUMAN; ANTIDEPRESSANT; RADIOLIGAND BINDING ASSAY;
Tipo documento:
Article
Natura:
Periodico
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
M. Tatsumi et al., "PHARMACOLOGICAL PROFILE OF ANTIDEPRESSANTS AND RELATED-COMPOUNDS AT HUMAN MONOAMINE TRANSPORTERS", European journal of pharmacology, 340(2-3), 1997, pp. 249-258

Abstract

Using radioligand binding assays, we determined the equilibrium dissociation constants (K-D's) for 37 antidepressants, three of their metabolites (desmethylcitalopram, desmethylsertraline, and norfluoxetine), some mood stabilizers, and assorted other compounds (some antiepileptics, Ca2+ channel antagonists, benzodiazepines, psychostimulants, antihistamines, and monoamines) for the human serotonin, norepinephrine, and dopamine transporters. Among the compounds that we tested, mazindol was the most potent at the human norepinephrine and dopamine transporters with K-D's of 0.45 +/- 0.03 nM and 8.1 +/- 0.4 nM, respectively. Sertraline (K-D = 25 +/- 2 nM) and nomifensine (56 +/- 3 nM) were the two most potent antidepressants at the human dopamine transporter. We showed significant correlations for antidepressant affinities at binding to serotonin (R = 0.93), norepinephrine (R = 0.97), and dopamine (R = 0.87) transporters in comparison to their respective values for inhibiting uptake of monoamines into rat brain synaptosomes. These data are useful in predicting some possible adverse effects and drug-drug interactions of antidepressants and related compounds. (C) 1997 Elsevier Science B.V.

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Documento generato il 15/07/20 alle ore 07:45:33