In vivo identification of muscarinic receptors on rat colonic epithelial cells binding of [3H]-quinuclidinyl benzilate
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We have demonstrated that intravenously administered [3H]-quinuclidinyl benzilate binds to rat colonic and ileal epithelial cells. The binding was prevented by pretreatment with atropine and QNB.
Binding was stereoselective in favor of dexetimide, the biologically more active optical isomer of benzetimide.
The results with intestinal epithelial cells were qualitatively the same as those obtained using heart and gut muscle as controls.
QNB inhibited pilocarpine-induced fluid accumulation in ligated gut segments.
The results support the concept that cholinergic receptors, which mediate intestinal secretion, exist on rat intestinal epithelial cell membranes.
Key wordsColon Isolated enterocytes Muscarinic receptors In vivo binding
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- Aronstam RS, Abood LG, Baumgold J (1977) Role of phospholipids in muscarinic binding by neural membranes. Biochem Pharmacol 26:1689–1695Google Scholar
- Blickenstaff DD, Lewis LJ (1952) Effect of atropine on intestinal absorption of water and chloride. Am J Physiol 170:17–23Google Scholar
- Browning JG, Hardcastle J, Hardcastle PT, Redfern JS (1978) Localization of the effects of acetylcholine in regulating intestinal ion transport. J Physiol 281:15–27Google Scholar
- Fields JZ, Roeske WR, Morkin E, Yamamura HI (1978) Cardiac muscarinic cholinergic receptors. J Biol Chem 253:3251–3258Google Scholar
- Gaginella TS, Haddad AC, Go VLW, Phillips SF (1977) Cytotoxicity of ricinoleci acid (castor oil) and other intestinal secretagogues on isolated intestinal epithelial cells. J Pharmacol Exp Ther 201:259–266Google Scholar
- Hardcastle PT, Eggenton J (1973) The effect of acetylcholine on the electrical activity of intestinal epithelial cells. Biochim Biophys Acta 298:95–100Google Scholar
- Hubel KA (1976) Intestinal ion transport: effect of norepinephrine, pilocarpine and atropine. Am J Physiol 231:252–257Google Scholar
- Hubel KA (1977) Effects of bethanechol on intestinal ion transport in the rat. Proc Soc Exp Biol Med 154:41–44Google Scholar
- Lowry OH, Rosebrough NJ, Farr AL, Randall J (1951) Protein measurements with the Folin phenol reagent. J Biol Chem 193:265–275Google Scholar
- Powell DW, Tapper EJ (1979a) Intestinal ion transport: cholinergic-adrenergic interactions. In: Binder HJ (ed) Mechanisms of intestinal secretion. Kroc Foundation Symp, vol 12. Alan R. Liss, Inc., New York, pp 175–192Google Scholar
- Powell DW, Tapper EJ (1979b) Autonomic control of intestinal electrolyte transport. In: Janowitz HD, Sachar DB (eds) Frontiers of knowledge in the diarrheal diseases. Projects in Health, Inc., Upper Montclair, NJ, pp 37–52Google Scholar
- Racusen LC, Binder HJ (1979) Adrenergic interaction with ion transport across colonic mucosa: Role of both α and β adrenergic agonists. In: Binder HJ (ed) Mechanisms of intestinal secretion. Kroc Foundation Symp, vol 12. Alan R. Liss, Inc., New York, pp 201–215Google Scholar
- Rimele TJ, Rogers WA, Gaginella TS (1979) Characterization of muscarinic cholinergic receptors in the lower esophageal sphincter of the cat: Binding of [3H]-quinuclidinyl benzilate. Gastroenterology 77:1225–1234Google Scholar
- Rimele TJ, O'Dorisio MS, Gaginella TS (1981) Evidence for muscarinic receptors on rat colonic epithelial cells: Binding of [3H]-quinuclidinyl benzilate. J Pharmacol Exp Ther 218:426–434Google Scholar
- Sokal RR, Rohlf FT (1969) Biometry: The principles and practice of statistics in biological research. Freeman, San FranciscoGoogle Scholar
- Soudijn W, Van Wijngaarden I, Ariens EJ (1973) Dexetimide, a useful tool in acetylcholine-receptor localization. Eur J Pharmacol 24:43–48Google Scholar
- Steel RGD, Torrie JH (1960) Principles and procedures of statistics. McGraw-Hill, New YorkGoogle Scholar
- Tapper EJ, Powell DW, Morris SM (1978) Cholinergic-adrenergic interactions on intestinal ion transport. Am J Physiol 235:E402-E409Google Scholar
- Tidball CS (1961) Active chloride transport during intestinal secretion. Am J Physiol 200:309–312Google Scholar
- Tidball CS, Tidball ME (1958) Changes in intestinal net absorption of a sodium chloride solution produced by atropine in normal and vagotomized dogs. Am J Physiol 193:25–28Google Scholar
- Turnheim K, Lauterbach F (1977) Secretion of monoquaternary ammonium compounds by guinea pig small intestine in vivo. Naunyn-Schmiedeberg's Arch Pharmacol 299:201–205Google Scholar
- Turnheim K, Lauterbach F (1980) Interaction between intestinal absorption and secretion of monoquaternary ammonium compounds in guinea pigs — a concept for the absorption kinetics of organic cations. J Pharmacol Exp Ther 212:418–424Google Scholar
- Ussing HH, Windhager EE (1964) Nature of shunt path and active sodium transport path through frog skin epithelium. Acta Physiol Scand 61:484–504Google Scholar
- Wright RD, Jennings MA, Florey HW, Lium R (1940) The influence of nerves and drugs on secretion by the small intestine and an investigation of the enzymes in intestinal juice. Q J Exp Physiol 30:73–120Google Scholar
- Yamamura HI, Kuhar MJ, Snyder SH (1974) In vivo identification of muscarinic cholinergic receptor binding in rat brain. Brain Res 80:170–176Google Scholar