Influence of Endothelin1131on Smooth Muscle Tone and Cholinergic NerveMediated Contraction in Rat Isolated Trachea

Autor: Goldie, Roy G., D'Aprile, Angela C., Self, Glenn J., Rigby, Paul J., Henry, Peter J.
Zdroj: Journal of Cardiovascular Pharmacology; January 2000, Vol. 36 Issue: Supplement 1 pS228S231-S228S231, 1p
Abstrakt: Endothelin1121ET1121is a strong candidate as a significant mediator in asthma, in part because of its powerful spasmogenic actions and its ability to enhance cholinergic nervemediated contraction in human and animal airway smooth muscle. In the study reported here, we have demonstrated that 125IET1131binds specifically to BQ123sensitive sites presumably ETAreceptors and to sarafotoxin S6c S6csensitive sites presumably ETBreceptors in rat tracheal and pulmonary airways, as well as in lung alveoli. These sites coexist in tracheal airway smooth muscle and in alveolar tissue in approximately equal proportions. ET1121and ET1131were equipotent and approximately equally active as spasmogens in rat tracheal smooth muscle. Importantly, both peptides were shown to potentiate cholinergic nervemediated rat tracheal contraction, although ET1131was less active in this regard. These data are consistent with the idea that ET1131could play a significant mediator role in obstructive airway diseases such as asthma.
Databáze: Supplemental Index