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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6 Pt 1
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pubmed:dateCreated |
1994-2-8
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pubmed:abstractText |
In the estrogen-treated rat myometrium, bombesin (Bn) and related agonists triggered contraction and the increased generation of inositol phosphates. The relative order of potencies was identical for both responses: Bn = gastrin releasing peptide (GRP) = litorin = neuromedin C >> neuromedin B. Two specific GRP-preferring receptor antagonists, namely [D-Phe6]Bn-(6-13) methyl ester and [Leu14,psi 13-14]Bn were inhibitory for both Bn-mediated tension and generation of inositol phosphates. [125I-Tyr4]Bn bound to myometrial membranes with high affinity (Kd = 104 pM) to a single class of sites in a saturable and reversible manner. The relative potencies for inhibiting binding were GRP = litorin = [Tyr4]Bn (Ki = 0.4 to 0.6 nM) >> neuromedin B (Ki = 10.3 nM). The high affinity displayed by [D-Phe6]Bn-(6-13) methyl ester (Ki = 2.8 nM) and [Leu14,psi 13-14]Bn (Ki = 35 nM) for competing for [Tyr4]Bn binding supported the involvement of a GRP-preferring Bn receptor. Guanine nucleotides decreased the binding of [125I-Tyr4]Bn and accelerated the rate of ligand dissociation, reflecting the coupling of receptors to guanine nucleotide regulatory proteins (G proteins). The results demonstrate that rat myometrium expresses functional GRP-preferring Bn receptors whose activation stimulates the phospholipase C pathway, pertussis toxin-insensitive event that contributes to Bn-mediated uterine contractions.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine Triphosphate,
http://linkedlifedata.com/resource/pubmed/chemical/Bombesin,
http://linkedlifedata.com/resource/pubmed/chemical/GTP-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Gastrin-Releasing Peptide,
http://linkedlifedata.com/resource/pubmed/chemical/Guanosine 5'-O-(3-Thiotriphosphate),
http://linkedlifedata.com/resource/pubmed/chemical/Guanylyl Imidodiphosphate,
http://linkedlifedata.com/resource/pubmed/chemical/Inositol Phosphates,
http://linkedlifedata.com/resource/pubmed/chemical/Neurokinin B,
http://linkedlifedata.com/resource/pubmed/chemical/Oligopeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Peptide Fragments,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Pertussis Toxin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Bombesin,
http://linkedlifedata.com/resource/pubmed/chemical/Virulence Factors, Bordetella,
http://linkedlifedata.com/resource/pubmed/chemical/adenosine 5'-O-(3-thiotriphosphate),
http://linkedlifedata.com/resource/pubmed/chemical/litorin,
http://linkedlifedata.com/resource/pubmed/chemical/neuromedin B,
http://linkedlifedata.com/resource/pubmed/chemical/neuromedin C
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0002-9513
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
265
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
C1579-87
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8279518-Adenosine Triphosphate,
pubmed-meshheading:8279518-Animals,
pubmed-meshheading:8279518-Binding, Competitive,
pubmed-meshheading:8279518-Bombesin,
pubmed-meshheading:8279518-Cell Membrane,
pubmed-meshheading:8279518-Chromatography, High Pressure Liquid,
pubmed-meshheading:8279518-Female,
pubmed-meshheading:8279518-GTP-Binding Proteins,
pubmed-meshheading:8279518-Gastrin-Releasing Peptide,
pubmed-meshheading:8279518-Guanosine 5'-O-(3-Thiotriphosphate),
pubmed-meshheading:8279518-Guanylyl Imidodiphosphate,
pubmed-meshheading:8279518-Inositol Phosphates,
pubmed-meshheading:8279518-Kinetics,
pubmed-meshheading:8279518-Muscle, Smooth,
pubmed-meshheading:8279518-Myometrium,
pubmed-meshheading:8279518-Neurokinin B,
pubmed-meshheading:8279518-Oligopeptides,
pubmed-meshheading:8279518-Peptide Fragments,
pubmed-meshheading:8279518-Peptides,
pubmed-meshheading:8279518-Pertussis Toxin,
pubmed-meshheading:8279518-Rats,
pubmed-meshheading:8279518-Rats, Wistar,
pubmed-meshheading:8279518-Receptors, Bombesin,
pubmed-meshheading:8279518-Signal Transduction,
pubmed-meshheading:8279518-Uterine Contraction,
pubmed-meshheading:8279518-Virulence Factors, Bordetella
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pubmed:year |
1993
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pubmed:articleTitle |
GRP-preferring bombesin receptors increase generation of inositol phosphates and tension in rat myometrium.
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pubmed:affiliation |
Laboratoire d'Endocrinologie et Régulations Cellulaires, Centre National de la Recherche Scientifique, Unité de Recherche Associée 1131, Université Paris Sud, Orsay, France.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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