کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
9894438 1542459 2005 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Endothelin receptors in lower esophageal sphincter circular smooth muscle
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شیمی
پیش نمایش صفحه اول مقاله
Endothelin receptors in lower esophageal sphincter circular smooth muscle
چکیده انگلیسی
To characterize endothelin (ET) receptors in the lower esophageal sphincter, we measured contraction of transverse strips from the guinea-pig lower esophageal sphincter induced by ET-related peptides and binding of 125I-ET-1 to cell membranes prepared from the lower esophageal sphincter circular muscle. Visualization of 125I-ET-1 binding sites in tissue was performed by autoradiography. ET-1 or ET-2 alone did not cause contraction or relaxation in resting strips. However, in carbachol precontracted lower esophageal sphincter strips, ET-1 and ET-2 caused marked, tetrodotoxin-insensitive relaxation. The ET-1-induced relaxation was abolished by BQ-123, an ETA receptor selective antagonist, but not inhibited by BQ-788, an ETB receptor selective antagonist. ET-3 and sarafotoxin S6c, a selective ETB receptor agonist, did not cause relaxation in the carbachol precontracted muscle strips. These clearly indicate that ETA receptors mediate relaxation. On the other hand, ET-3 and sarafotoxin S6c caused tetrodotoxin and atropine-insensitive contraction in the resting strips. The sarafotoxin S6c-induced contraction was inhibited by BQ-788, but not by BQ-123. Furthermore, ET-1 and ET-2 caused contraction of the resting muscle strips after pretreatment with BQ-123. This ET-1-induced contraction was also inhibited by BQ-788. Taken together, these indicate that ETB receptors mediate contraction. Autoradiography localized 125I-ET-1 binding to the lower esophageal sphincter circular muscle as well as longitudinal muscle of the esophagus. Binding of 125I-ET-1 to cell membranes prepared from the circular smooth muscle was saturable and specific. Analysis of dose-inhibition curves indicated the presence of two classes of receptors, ETA and ETB receptors. These results demonstrate that the guinea-pig lower esophageal sphincter possesses ETA receptors mediating relaxation and ETB receptors mediating contraction.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Regulatory Peptides - Volume 127, Issues 1–3, 15 April 2005, Pages 27-35
نویسندگان
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