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Titolo:
EFFECTS OF JTV-506, A NEW K-MUSCLE CONTRACTION AND SYSTEMIC BLOOD-PRESSURE( CHANNEL ACTIVATOR, ON AIRWAY SMOOTH)
Autore:
ANDO T; KUME H; URATA Y; TAKAGI K;
Indirizzi:
NAGOYA UNIV,SCH MED,DEPT INTERNAL MED 2,SHOWA KU,65 TSURUMA CHO NAGOYA AICHI 466 JAPAN NAGOYA UNIV,SCH MED,DEPT INTERNAL MED 2,SHOWA KU NAGOYA AICHI 466 JAPAN JAPAN TOBACCO INC,CENT PHARMACEUT RES INST TAKATSUKI OSAKA JAPAN
Titolo Testata:
Clinical and experimental allergy
fascicolo: 6, volume: 27, anno: 1997,
pagine: 705 - 713
SICI:
0954-7894(1997)27:6<705:EOJANK>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
PIG ISOLATED TRACHEALIS; GUINEA-PIG; POTASSIUM CHANNELS; INDUCED BRONCHOCONSTRICTION; RELAXANT ACTION; RO 31-6930; CROMAKALIM; MEMBRANE; OPENER; BRONCHODILATOR;
Keywords:
ATP-SENSITIVE POTASSIUM CHANNELS; K+ CHANNEL ACTIVATORS; TRACHEAL SMOOTH MUSCLE; BRONCHODILATORS; RESPIRATORY RESISTANCE; DYNAMIC COMPLIANCE; BLOOD PRESSURE; CROMAKALIM;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
41
Recensione:
Indirizzi per estratti:
Citazione:
T. Ando et al., "EFFECTS OF JTV-506, A NEW K-MUSCLE CONTRACTION AND SYSTEMIC BLOOD-PRESSURE( CHANNEL ACTIVATOR, ON AIRWAY SMOOTH)", Clinical and experimental allergy, 27(6), 1997, pp. 705-713

Abstract

Background ATP-sensitive K+ (K-ATP) channel activators produce relaxation of smooth muscle in many tissues. However, this wide range of effects restricts their clinical usefulness in bronchial asthma because of a reduction in systemic blood pressure. Methods We have now examinedthe effects of JTV-506, a new benzopyran derivative, on airway smoothmuscle contraction and systemic blood pressure and have compared thiscompound with cromakalim. We measured isometric tension records from guinea-pig isolated trachea, as well as the respiratory resistance (R-rs) and systemic blood pressure in anesthetized guinea-pigs. Results JTV-506 caused a concentration-dependent inhibition of histamine-induced contraction in guinea-pig isolated tracheal smooth muscle, and was antagonized by glibenclamide. JTV-506 was 7.6-fold mon potent than cromakalim. In anesthetized animals the intravenous injection of JTV-506 reduced the increase in R-rs induced by intravenous application of 5 mug/kg of histamine in a dose-dependent manner. 10 mu g/kg of JTV-506 resulted in 57.0 +/- 17.9% inhibition of the increase in R-rs at 10 min. The inhibitory action on R-rs disappeared after 60 min. 10 mu g/kg of cromakalim caused 25.4 +/- 5.8% inhibition of the increase in R-rs induced by histamine at 1 min. The ED50 values for JTV-506 and cromakalim were 6.7 +/- 3.5 mu g/kg and 60.1 +/- 15.8 mu g/kg, respectively (P<0.05). Cromakalim was approximate to 9-fold less potent in inhibitingthe increased R-rs by histamine, and the inhibitory action lasted less than 10 min. The reduction of systemic blood pressure by JTV-506 andcromakalim (each at a dose of 10 mu g/kg iv) was 11.3% and 21.5%, respectively (P < 0.05). Conclusion JTV-506 inhibits histamine-induced contraction of tracheal smooth muscle by activation of K-ATP channels. This compound is more potent and longer-lasting in the suppression of histamine-induced increases in R-rs, and is less hypotensive than cromakalim. Our results suggest that this compound merits further investigation for utility as a bronchodilator in the clinic.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 08:27:32