Linked Life Data

2463767

Source:http://linkedlifedata.com/resource/pubmed/id/2463767

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1 Pt 1
pubmed:dateCreated
1989-2-21
pubmed:abstractText
The present experiments evaluate in vivo effects of recently described cholecystokinin (CCK) receptor antagonists on rat pancreatic secretion. Pancreaticobiliary secretion was studied after bile duct cannulation in anesthetized rats. After two basal 10-min fractions were selected, secretion was stimulated by intravenous caerulein (0.1-30.0 micrograms/kg) or secretin, and collected for seven further 10-min fractions. Peptide antagonists (CR 1409, CR 1392, and CR 1505) and nonpeptide antagonists (asperlicin and L364,718) were given intravenously 10 min before agonists. Increasing doses of antagonists gradually reduced secretion of protein and enzymes stimulated by submaximal and maximal doses of caerulein. The antagonists did not alter nonstimulated or secretin-stimulated secretion, indicating their specificity for the CCK receptor. Except for proglumide and asperlicin, all antagonists were able to abolish caerulein-stimulated pancreatic secretion, as evaluated by the mean integrated 1-h response to a near-maximal dose of caerulein. The caerulein dose-response curve was gradually shifted to the right by increasing doses of CR 1409, indicating competitive-like kinetics. Inhibition of secretion due to supramaximal doses of caerulein, however, could be reversed by doses of CR 1409 smaller than expected from extrapolating truely competitive kinetics from an in vitro situation to the in vivo situation. The rank order of potency of the compounds to antagonize caerulein-stimulated secretion in vivo agreed with their relative potencies to antagonize caerulein-stimulated amylase secretion from pancreatic acini in vitro as well as with their affinity to bind to peripheral CCK receptors in vitro.(ABSTRACT TRUNCATED AT 250 WORDS)
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/Amylases, http://linkedlifedata.com/resource/pubmed/chemical/Benzodiazepinones, http://linkedlifedata.com/resource/pubmed/chemical/Caerulein, http://linkedlifedata.com/resource/pubmed/chemical/Cholecystokinin, http://linkedlifedata.com/resource/pubmed/chemical/Chymotrypsinogen, http://linkedlifedata.com/resource/pubmed/chemical/Devazepide, http://linkedlifedata.com/resource/pubmed/chemical/Proglumide, http://linkedlifedata.com/resource/pubmed/chemical/Proteins, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cholecystokinin, http://linkedlifedata.com/resource/pubmed/chemical/Secretin, http://linkedlifedata.com/resource/pubmed/chemical/asperlicin, http://linkedlifedata.com/resource/pubmed/chemical/lorglumide, http://linkedlifedata.com/resource/pubmed/chemical/loxiglumide
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0002-9513
pubmed:author
pubmed:issnType
Print
pubmed:volume
256
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
G150-7
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Comparative effects of CCK receptor antagonists on rat pancreatic secretion in vivo.
pubmed:affiliation
Medizinische Klinik und Poliklinik, Universität Düsseldorf, Federal Republic of Germany.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't