rdf:type |
|
lifeskim:mentions |
umls-concept:C0034791,
umls-concept:C0038351,
umls-concept:C0064465,
umls-concept:C0109741,
umls-concept:C0205314,
umls-concept:C0243076,
umls-concept:C0679622,
umls-concept:C0999699,
umls-concept:C1267092,
umls-concept:C1521827,
umls-concept:C1524063,
umls-concept:C1880022
|
pubmed:issue |
4
|
pubmed:dateCreated |
1993-11-2
|
pubmed:abstractText |
1. The cholecystokinin receptors mediating motor responses in a novel smooth muscle preparation from the corpus region of the guinea-pig stomach have been characterized by use of five agonist peptides and the antagonists CI-988, L-365,260 and devazepide. 2. Mucosa-denuded strips of circular muscle were contracted in a concentration-dependent manner by the five cholecystokinin (CCK)-related peptides CCK-8S, pentagastrin, gastrin-I, CCK-8US and CCK-4. 3. CI-988 was a powerful antagonist of the response to pentagastrin with an affinity (pKB = 9.49) similar to that obtained in CCKB receptor binding assays. With CCK-8S as the agonist, CI-988 was approximately 1000 fold less powerful as an antagonist. 4. Devazepide powerfully blocked responses to CCK-8S with an affinity (pKB = 9.54) that was in agreement with reported functional data obtained in pancreatic amylase secretion studies, a system exhibiting CCKA receptor activity. Devazepide displayed lower affinity against pentagastrin than against CCK-8S. 5. CI-988 blocked responses to pentagastrin in an insurmountable manner in the presence of 3 nM devazepide; a concentration previously shown to block the CCKA receptor. The nature of the antagonism observed with L-365,260 was unaltered by the presence of devazepide. 6. The guinea-pig stomach corpus smooth muscle preparation contains both subtypes of CCK receptor and will be useful as a pharmacological tool for investigating the functional effects of novel CCK ligands.
|
pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-13651579,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-1393262,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-1504734,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-1704435,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-1881532,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-1975695,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2064383,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2262906,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2382717,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2473653,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2549666,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2573403,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2721567,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2748418,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2758237,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2831729,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-2873044,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-3014520,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-3658220,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-3781185,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-6093075,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-6256771,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-6278962,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-6293316,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8401944-7013499
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Benzodiazepinones,
http://linkedlifedata.com/resource/pubmed/chemical/Carbachol,
http://linkedlifedata.com/resource/pubmed/chemical/Cholecystokinin,
http://linkedlifedata.com/resource/pubmed/chemical/Devazepide,
http://linkedlifedata.com/resource/pubmed/chemical/Gastrins,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/L 365260,
http://linkedlifedata.com/resource/pubmed/chemical/Meglumine,
http://linkedlifedata.com/resource/pubmed/chemical/PD 134308,
http://linkedlifedata.com/resource/pubmed/chemical/Phenylurea Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cholecystokinin
|
pubmed:status |
MEDLINE
|
pubmed:month |
Aug
|
pubmed:issn |
0007-1188
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
109
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
913-7
|
pubmed:dateRevised |
2009-11-18
|
pubmed:meshHeading |
pubmed-meshheading:8401944-Animals,
pubmed-meshheading:8401944-Benzodiazepinones,
pubmed-meshheading:8401944-Carbachol,
pubmed-meshheading:8401944-Cholecystokinin,
pubmed-meshheading:8401944-Devazepide,
pubmed-meshheading:8401944-Gastric Mucosa,
pubmed-meshheading:8401944-Gastrins,
pubmed-meshheading:8401944-Guinea Pigs,
pubmed-meshheading:8401944-Indoles,
pubmed-meshheading:8401944-Male,
pubmed-meshheading:8401944-Meglumine,
pubmed-meshheading:8401944-Muscle, Smooth,
pubmed-meshheading:8401944-Muscle Contraction,
pubmed-meshheading:8401944-Phenylurea Compounds,
pubmed-meshheading:8401944-Receptors, Cholecystokinin,
pubmed-meshheading:8401944-Stomach
|
pubmed:year |
1993
|
pubmed:articleTitle |
Characterization of CCK receptors in a novel smooth muscle preparation from the guinea-pig stomach by use of the selective antagonists CI-988, L-365,260 and devazepide.
|
pubmed:affiliation |
Parke-Davis Neuroscience Research Centre, Addenbrookes Hospital Site, Cambridge.
|
pubmed:publicationType |
Journal Article,
In Vitro
|