Synergistic opioid inhibition of colonic Cl- secretion by kappa-opioid receptor agonism plus mu-opioid receptor antagonism.
On the basis of the novel concept of a dual prosecretory/antisecretory intestinal opioid system, a voltage-clamp experiment was performed with guinea-pig colonic mucosa, and net anion (Cl-) secretion was measured after stimulation with prostaglandin E1 (PGE1) plus theophylline. Synergism between kappa-opioid receptor agonism by U69593 and mu-opioid receptor antagonism by CTOP-NH2 (D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2) was observed.
Kromer
W
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Department of Pharmacology, Byk Gulden Pharmaceuticals, Konstanz, Germany.
D000584:Amiloride / Q000494:pharmacology; D000595:Amino Acid Sequence; D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D044482:Benzeneacetamides; D002712:Chlorides / Q000378:metabolism*; D003106:Colon / Q000187:drug effects* / Q000378:metabolism; D004357:Drug Synergism; D006168:Guinea Pigs; D008297:Male; D008969:Molecular Sequence Data; D009092:Mucous Membrane / Q000187:drug effects / Q000378:metabolism; D011759:Pyrrolidines / Q000494:pharmacology*; D017473:Receptors, Opioid, kappa / Q000187:drug effects; D017450:Receptors, Opioid, mu / Q000037:antagonists & inhibitors*; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000494:pharmacology
D000700:Analgesics; D044482:Benzeneacetamides; D002712:Chlorides; D011759:Pyrrolidines; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; C049352:phenylalanyl-cyclo(cysteinyltyrosyl-tryptophyl-ornithyl-threonyl-penicillamine)threoninamide; D013004:Somatostatin; D000584:Amiloride; C045444:U 69593