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Titolo:
Thiophene analogs of naphthoxazines and 2-aminotetralins: bioisosteres with improved relative oral bioavailability, as compared to 5-OH-DPAT
Autore:
Rodenhuis, N; Timmerman, W; Wikstrom, HV; Dijkstra, D;
Indirizzi:
Univ Groningen, Ctr Pharm, Dept Med Chem, NL-9713 AV Groningen, Netherlands Univ Groningen Groningen Netherlands NL-9713 AV V Groningen, Netherlands
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 2-3, volume: 394, anno: 2000,
pagine: 255 - 263
SICI:
0014-2999(20000414)394:2-3<255:TAONA2>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
DOPAMINE-RECEPTOR AGONISTS; STRUCTURAL REQUIREMENTS; D-4 RECEPTORS; D2 RECEPTOR; BINDING; SERIES; RELEASE; BRAIN; RAT; MONOHYDROXYAMINOTETRALINS;
Keywords:
dopamine receptor agonist; microdialysis; bioavailability; striatum; bioisosteric replacement; thiophene analog;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
34
Recensione:
Indirizzi per estratti:
Indirizzo: Rodenhuis, N Univ Groningen, Ctr Pharm, Dept Med Chem, A Deusinglaan 1, NL-9713 AV Groningen, Netherlands Univ Groningen A Deusinglaan 1 Groningen Netherlands NL-9713 AV
Citazione:
N. Rodenhuis et al., "Thiophene analogs of naphthoxazines and 2-aminotetralins: bioisosteres with improved relative oral bioavailability, as compared to 5-OH-DPAT", EUR J PHARM, 394(2-3), 2000, pp. 255-263

Abstract

In the present study, a series of thiophene analogs of 2-aminotetralins and hexahydronaphthoxazines were studied in vivo for their ability to decrease striatal dopamine release, their effects on locomotor activity, and theirbehavioral characteristics in reserpinized rats, in order to investigate whether a thiophene moiety can act as a bioisostere for the phenol moiety. In general, the new compounds showed lower in vivo activities than 5-hydroxy-2-(N, N,-di-n-propylamino)tetralin (5-OH-DPAT). However, the introduction of the thiophene moiety gave a significant improvement of the relative oralbioavailability, compared to 5-OH-DPAT. Our results suggest that the thiophene moiety can act as a bioisostere for a phenol group in hydroxylated 2-aminotetralins. For the thianaphthoxazines it was not possible to discriminate between bioisosterism for a phenyl or a phenol moiety. The tetrahydrobenzo[b]thiophenes could be used as lead compounds for the development of novel dopamine receptor ligands with improved relative oral bioavailability. (C) 2000 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/03/20 alle ore 12:12:02