Effects of CCK-receptor antagonist on colonic motor activity in dogs. 1995

M Karaus, and C Niederau
Department of Internal Medicine, Heinrich-Heine-University of Düsseldorf, Germany.

This study employed a cholecystokinin (CCK) antagonist to evaluate whether endogenous CCK regulates fasted and fed motor patterns of the colon. Experiments were performed in six conscious dogs, each in duplicate. Motor activity was recorded by four strain gauge transducers implanted on the colon. The effects of the CCK-analogue caerulein and the CCK-antagonist loxiglumide (Rotta, Italy) were studied in fasted and fed states. The motor activity was computed for the area under contractions. Caerulein given as an intravenous bolus of 50 ng kg-1 during a quiescent state caused a burst of phasic and tonic contractions resembling a regular non-migrating motor complex. Physiological doses of 10 ng kg-1 caerulein, which increases plasma CCK-immunoreactivity to postprandial levels, had no effect. Continuous intravenous infusion of 10 mg kg-1 h-1 loxiglumide completely abolished the effects of 50 ng kg-1 caerulein. The motor activity stimulated by the cholinesterase inhibitor neostigmine (10 micrograms kg-1) was not altered by loxiglumide. Loxiglumide given in the fasted state reduced the area under contractions in the proximal colon by 26.8 +/- 12.8% compared to the control without loxiglumide (P < 0.05). The postprandial increase in motor activity in the distal colon, the gastrocolonic response, was significantly inhibited by loxiglumide. Moreover, loxiglumide reduced the area under contractions in the fed state by 25.4 +/- 10.7% and 19 +/- 7.2% in the proximal and distal colon, respectively (P < 0.05). The present results show that loxiglumide acts as a specific antagonist of the actions of CCK on colonic motor activity in the dog.(ABSTRACT TRUNCATED AT 250 WORDS)

UI MeSH Term Description Entries
D008297 Male Males
D009388 Neostigmine A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier. Synstigmin,Neostigmine Bromide,Neostigmine Methylsulfate,Polstigmine,Proserine,Prostigmin,Prostigmine,Prozerin,Syntostigmine,Bromide, Neostigmine,Methylsulfate, Neostigmine
D011377 Proglumide A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers. Xylamide,Milid,Xilamide
D011949 Receptors, Cholecystokinin Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood. CCK Receptors,Caerulein Receptors,Cholecystokinin Octapeptide Receptors,Cholecystokinin Receptors,Pancreozymin Receptors,Receptors, CCK,Receptors, Caerulein,Receptors, Pancreozymin,Receptors, Sincalide,Sincalide Receptors,CCK Receptor,CCK-4 Receptors,CCK-8 Receptors,Cholecystokinin Receptor,Receptors, CCK-4,Receptors, CCK-8,Receptors, Cholecystokinin Octapeptide,CCK 4 Receptors,CCK 8 Receptors,Octapeptide Receptors, Cholecystokinin,Receptor, CCK,Receptor, Cholecystokinin,Receptors, CCK 4,Receptors, CCK 8
D002108 Ceruletide A specific decapeptide obtained from the skin of Hila caerulea, an Australian amphibian. Caerulein is similar in action and composition to CHOLECYSTOKININ. It stimulates gastric, biliary, and pancreatic secretion; and certain smooth muscle. It is used in paralytic ileus and as diagnostic aid in pancreatic malfunction. Caerulein,Cerulein,Ceruletid,FI-6934,Takus,FI 6934,FI6934
D003106 Colon The segment of LARGE INTESTINE between the CECUM and the RECTUM. It includes the ASCENDING COLON; the TRANSVERSE COLON; the DESCENDING COLON; and the SIGMOID COLON. Appendix Epiploica,Taenia Coli,Omental Appendices,Omental Appendix,Appendices, Omental,Appendix, Omental
D003864 Depression, Chemical The decrease in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical. Chemical Depression,Chemical Depressions,Depressions, Chemical
D004285 Dogs The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065) Canis familiaris,Dog
D005215 Fasting Abstaining from FOOD. Hunger Strike,Hunger Strikes,Strike, Hunger,Strikes, Hunger
D005260 Female Females

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