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The actions of caerulein on the smooth muscle of the gastrointestinal tract and the gall bladder
Author(s) -
BERTACCINI G.,
CARO G.,
ENDEAN R.,
ERSPAMER V.,
IMPICCIATORE M.
Publication year - 1968
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1968.tb07052.x
Subject(s) - tachyphylaxis , atropine , gastrointestinal tract , cholecystokinin , endocrinology , medicine , ileum , chemistry , pharmacology , receptor
1 In the intact conscious dog, caerulein causes emesis and evacuation of the bowel. The mean effective dose by the intravenous route is 0.4–0.5 μg/kg, and by the subcutaneous route 3–4 μg/kg. 2 The gall bladder in situ or as an isolated preparation is highly sensitive to caerulein. A few ng/kg injected intravenously are sufficient to stimulate the gall bladder in situ and less than 1 ng/kg per min is effective when infused intravenously. The isolated gall bladder is contracted by caerulein in concentrations as low as 0.03–2 ng/ml. Krebs solution. There is no tachyphylaxis but, generally, a good dose‐response relationship. Hence the gall bladder, especially that of the guinea‐pig, appears to be very suitable for the bioassay of caerulein and related peptides. 3 In situ , the musculature of the gastrointestinal tract is also highly sensitive to caerulein. Doses as low as 1–5 ng/kg, administered intravenously, have a spasmogenic action on jejunal loops of the dog, and slightly larger doses contract the small intestine of the cat. The stomach and the large intestine seem to be somewhat less sensitive to the polypeptide. Caerulein has a considerable spasmogenic action on the rat pylorus but relaxes the sphincter of Oddi of the guinea‐pig. 4 Isolated preparations of the gastrointestinal tract are relatively insensitive to caerulein and tachyphylaxis occurs readily. 5 Blockade with atropine produces different effects in different intestinal segments and in different animal species. The spasmogenic action of caerulein on the gall bladder is atropine‐resistant. 6 The effects of caerulein are similar to those of cholecystokinin‐pancreozymin in the organs tested in situ or as isolated preparations. Caerulein, however, is always more potent than cholecystokinin‐pancreozymin, even on a molar basis. Compared with caerulein, human gastrin I has negligible activity. 7 The possible use of caerulein in cholecystography is discussed.