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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
3
|
| pubmed:dateCreated |
1995-4-14
|
| pubmed:abstractText |
Endothelin (ET) has been previously demonstrated to be a potent intestinal secretory stimuli and to elicit intestinal smooth muscle contractions. In rat distal colon, the ETA receptor antagonist cyclo[D-Asp-L-Pro-D-Val-L-Leu-D-Trp] abolishes the changes in ion transport (as measured by short-circuit current) elicited by ET-1. In this study, effects of ET-1, sarafotoxin 6c and "big" ET in the absence and presence of the endothelin receptor antagonists cyclo [D-Asp-L-Pro-D-Val-L-Leu-D-Trp] and (+/-)-3-[2-(carboxymethoxy)-4-methoxyphenyl]-1-[3,4- (methylenedioxy)phenyl]-5-(prop-1-yloxy)indan-2-carboxylic acid on ion transport in rabbit distal colon were assessed through measurement of short-circuit current changes in segments of muscle-stripped mucosa in Ussing chambers. In addition, changes in smooth muscle contraction in response to acetylcholine, ET-1, ET-3 and sarafotoxin 6c in the absence and presence of (+/-)-3-[2-(carboxymethoxy)-4-methoxyphenyl]-1-[3,4- (methylenedioxy)phenyl]-5-(prop-1-yloxy)indan-2-carboxylic acid and of cyclo [D-Asp-L-Pro-D-Val-L-Leu-D-Trp] were measured in mucosa-free preparations oriented along their longitudinal axes. Receptor binding studies with mucosal or smooth muscle homogenates were conducted with [125I]ET-1, with [125I]ET-3 and with [125I]Tyr13Suc-[Glu9,Ala11,15]-endothelin-1(8-21 ) to identify the subtypes of ET receptors present in these preparations. From studies with rabbit colonic mucosa, both binding studies and measurement of short-circuit current confirm that the ETB receptor subtype is the predominant subtype and is responsible for the changes observed in ion transport.(ABSTRACT TRUNCATED AT 250 WORDS)
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Mar
|
| pubmed:issn |
0022-3565
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
272
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1204-10
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| pubmed:dateRevised |
2003-11-14
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| pubmed:meshHeading |
pubmed-meshheading:7891334-Amino Acid Sequence,
pubmed-meshheading:7891334-Animals,
pubmed-meshheading:7891334-Colon,
pubmed-meshheading:7891334-Endothelins,
pubmed-meshheading:7891334-Gastrointestinal Motility,
pubmed-meshheading:7891334-Intestinal Mucosa,
pubmed-meshheading:7891334-Ion Transport,
pubmed-meshheading:7891334-Membranes,
pubmed-meshheading:7891334-Molecular Sequence Data,
pubmed-meshheading:7891334-Muscle, Smooth,
pubmed-meshheading:7891334-Muscle Contraction,
pubmed-meshheading:7891334-Rabbits,
pubmed-meshheading:7891334-Radioligand Assay,
pubmed-meshheading:7891334-Receptors, Endothelin,
pubmed-meshheading:7891334-Viper Venoms
|
| pubmed:year |
1995
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| pubmed:articleTitle |
Nonpeptide endothelin receptor antagonists: IV. Identification of receptors in rabbit colonic mucosa and smooth muscle and correlation with physiological effects.
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| pubmed:affiliation |
Department of Drug Delivery, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania.
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| pubmed:publicationType |
Journal Article
|