Duration of anti-cholecystokinin (CCK) action on the rat exocrine pancreas of new CCK receptor antagonist FK480 administered orally.
We assessed the duration of the anti-cholecystokinin (CCK) action of FK480, a new non-peptide CCK-A receptor antagonist developed in Japan, in an in vivo study in rats, comparing it with CR 1505. Pancreatic exocrine secretion stimulated by intravenous infusion of CCK-8 (0.06 microgram/kg per h) was measured at intervals of 0-24 h after the oral administration of FK480 (1.5 mg/kg) and CR 1505 (30 mg/kg). FK480 significantly inhibited both CCK-stimulated pancreatic juice volume flow and amylase output 0, 4, 8, and 12 h after oral administration, whereas the inhibitory effect of CR 1505 had completely disappeared by 8 h after oral administration. It was concluded that orally administered FK480 has a prolonged anti-CCK action.
Moriyoshi
Y
Y
Department of Internal Medicine, Tokyo Women's Medical College, Japan.
Shiratori
K
K
Iwabe
C
C
Watanabe
S
S
Takeuchi
T
T
D000284:Administration, Oral; D000818:Animals; D001570:Benzodiazepinones / Q000008:administration & dosage / Q000494:pharmacology*; D006727:Hormone Antagonists / Q000008:administration & dosage / Q000494:pharmacology*; D007211:Indoles / Q000008:administration & dosage / Q000494:pharmacology*; D007262:Infusions, Intravenous; D008297:Male; D010179:Pancreas / Q000187:drug effects* / Q000378:metabolism; D010189:Pancreatic Juice / Q000187:drug effects / Q000378:metabolism; D011377:Proglumide / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors*
D001570:Benzodiazepinones; D006727:Hormone Antagonists; D007211:Indoles; D011949:Receptors, Cholecystokinin; C082966:FR 120480; C053737:loxiglumide; D011377:Proglumide