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Titolo:
TRANSCRIPTIONAL MECHANISMS INVOLVED IN THE RELAXANT EFFECT OF ZERANOLON ISOLATED RAT UTERUS
Autore:
REVUELTA MP; CANTABRANA B; HIDALGO A;
Indirizzi:
FAC MED C JULIAN CLAVERIA,DEPT MED,PHARMACOL LAB OVIEDO 33006 SPAIN FAC MED C JULIAN CLAVERIA,DEPT MED,PHARMACOL LAB OVIEDO 33006 SPAIN
Titolo Testata:
General pharmacology
fascicolo: 4, volume: 28, anno: 1997,
pagine: 561 - 565
SICI:
0306-3623(1997)28:4<561:TMIITR>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
SMOOTH-MUSCLE CONTRACTION; CALCIUM-FREE SOLUTION; UTERINE CONTRACTION; PARTIAL AGONIST; IN-VITRO; DIETHYLSTILBESTROL; ESTROGENS; PHARMACOLOGY; POLYAMINES; ANTIESTROGENS;
Keywords:
RAT UTERUS; CALCIUM; ZERANOL; TRANSCRIPTIONAL MECHANISMS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
39
Recensione:
Indirizzi per estratti:
Citazione:
M.P. Revuelta et al., "TRANSCRIPTIONAL MECHANISMS INVOLVED IN THE RELAXANT EFFECT OF ZERANOLON ISOLATED RAT UTERUS", General pharmacology, 28(4), 1997, pp. 561-565

Abstract

1. The effect of zeranol (3-100 mu M) on rat uterus contractions induced by KCl (60 mM) and CaCl2 (30 mu M-10 mM) has been assayed. 2. Zeranol relaxed the tonic contraction induced by KCl in a concentration-dependent manner (IC50 15.62+/-2.66 mu M), CaCl2 (0.1-10 mM) did not counteract the relaxing effect of zeranol. 3. CaCl2 (30 mu M-10 mM) produced a concentration-dependent contraction of rat uterus in medium lacking calcium plus KCl (60 mM) (EC(50) 0.34+/-0.03 mM). Zeranol (8 mu M)displaced the CaCl2 concentration-response curve to the right and increased the EC(50) to 1.27+/-0.57 mM (P<0.05) without modifying the E(max). 4. The antiestrogen tamoxifen (1 mu M) and the inhibitor of cAMP-dependent protein kinase TPCK (3 mu M) did not modify the effect of zeranol. However, the inhibitors of transcription (actinomycin D, 4 mu M), protein synthesis (cycloheximide, 100 mu M), and ornithine-decarboxilase (alpha-difluoromethyl ornithine, 10 mM)) antagonized the effect of zeranol, increasing the IC50 to 50.2+/-6.2 mu M, 122+/-6.9 mu M, and 23.51+/-1.14 mu M, respectively. 5. Our results suggest that the relaxing effect of zeranol on rat uterus smooth muscle is produced by mechanisms unrelated to cAMP and estrogen receptors, but involves transcriptional effects and polyamine synthesis. (C) 1997 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/11/20 alle ore 19:54:16