Involvement of cholecystokinin receptor in the inhibition of gastrointestinal motility by estradiol in ovariectomized rats.
BACKGROUND
The effects of estradiol benzoate (EB) on gastric emptying, gastrointestinal transit and plasma levels of cholecystokinin (CCK) were studied in ovariectomized rats.


METHODS
Gastrointestinal motility was assessed in rats 15 min after intragastric instillation of a test meal containing charcoal and Na2 51CrO4. Gastric emptying was determined by measuring the amount of radiolabeled chromium contained in the small intestine as a percentage of the initial amount received. Gastrointestinal transit was evaluated by calculating the geometric center of distribution of the radiolabeled marker. Blood samples were collected for E2 and CCK radioimmunoassay.


RESULTS
After treatment of EB (4-25 microg/kg), gastric emptying and gastrointestinal transit were inhibited, whereas plasma concentrations of E2 and CCK were increased in a dose-dependent manner. The selective CCK(A) receptor antagonists, devazepide and lorglumide, effectively attenuated the EB-induced inhibition of gastric emptying and gastrointestinal transit. L-365,260, a selective CCK(B) receptor antagonist, did not alter the EB-induced inhibition of gastric emptying and gastrointestinal transit.


CONCLUSIONS
The results suggest that EB inhibits gastric emptying and gastrointestinal transit in ovariectomized rats via a mechanism involving CCK stimulation and CCK(A) receptor activation.
Wu
C L
CL
Dept of Physiology, School of Medicine, National Yang-Ming University, Taipei, Taiwan, ROC.
Hung
C R
CR
Chang
F Y
FY
Pau
K Y F
KY
Wang
P S
PS
D000818:Animals; D001570:Benzodiazepinones / Q000494:pharmacology; D002766:Cholecystokinin / Q000097:blood*; D020109:Devazepide / Q000494:pharmacology; D004195:Disease Models, Animal; D004958:Estradiol / Q000031:analogs & derivatives* / Q000097:blood / Q000494:pharmacology*; D005260:Female; D005746:Gastric Emptying / Q000187:drug effects* / Q000502:physiology*; D005772:Gastrointestinal Transit / Q000187:drug effects* / Q000502:physiology*; D006727:Hormone Antagonists / Q000494:pharmacology; D010052:Ovariectomy; D010671:Phenylurea Compounds / Q000494:pharmacology; D011377:Proglumide / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors / Q000187:drug effects* / Q000502:physiology*; D013997:Time Factors
D001570:Benzodiazepinones; D006727:Hormone Antagonists; D010671:Phenylurea Compounds; D011949:Receptors, Cholecystokinin; C074283:estradiol 3-benzoate; C058121:L 365260; D004958:Estradiol; D002766:Cholecystokinin; D011377:Proglumide; D020109:Devazepide; C048181:lorglumide