Summary
(1) Reflex peristalsis in the circular muscle of the guinea pig ileum was elicited in vitro by sustained luminal distension of the intestinal wall according to 2 cm H2O and evaluated in terms of the number of peristaltic waves within 15 min intervals. (2) The poorly μ-selective opioid antagonist naloxone at concentrations of 10−7 and 10−6 mol/l increased the frequency of peristaltic contractions within the first 15 min interval, and thereafter in a declining fashion, by 68 and 88%, respectively. The highly κ-selective opioid antagonist nor-binaltorphimine behaved similarly. It was, by one order of magnitude, more potent but a little less effective than naloxone, i.e., the maximum effect was 57% increase in peristaltic frequency at 10−8 mol/l. Concentrations of 10−7 and 10−6 mol/l had the same effect as 10−8 mol/l, and 10−9 mol/l were ineffective. The highly μ-selective antagonist CTOP-NH2 and the highly δ-selective antagonist ICI 174,864 were ineffective up to 10−6 mol/l. (3) It is concluded that predominantly ξ opioid receptors are used by endogenous opioids under the present conditions to inhibit reflex peristalsis.
Similar content being viewed by others
References
Barnard EA, Demoliou-Mason C (1983) Molecular properties of opioid receptors. Br Med Bulletin 39:37–45
Chavkin Ch, Goldstein A (1981) Demonstration of a specific dynorphin receptor in guinea pig ileum myenteric plexus. Nature 291:591–593
Chavkin Ch, Goldstein A (1982) Reduction in opiate receptor reserve in morphine tolerant guinea pig ilea. Life Sci 31:1687–1690
Clark SJ, Smith TW (1981) Peristalsis abolishes the release of methionine-enkephalin from guinea-pig ileum in vitro. Eur J Pharmacol 70:421–424
Cotton R, Giles MG, Miller L, Shaw JS, Timms D (1984) ICI 174864: A highly selective antagonist for the opioid δ-receptor. Eur J Pharmacol 97:331–332
Gulya K, Pelton JT, Hruby VJ, Yamamura HI (1986) Cyclic somatostatin octapeptide analogues with high affinity and selectivity toward mu opioid receptors. Life Sci 38:2221–2229
Johnson SM, Costa M, Humphreys CMS (1988) Opioid mu and kappa receptors on axons of cholinergic excitatory motor neurons supplying the circular muscle of guinea-pig ileum. Naunyn-Schmiedeberg's Arch Pharmacol 338:397–400
Kachur JF, Miller RJ, Field M (1980) Control of guinea pig intestinal electrolyte secretion by a δ-opiate receptor. Proc Natl Acad Sci USA 77:2753–2756
Kosterlitz HW, Pirie VW, Robinson JA (1956) The mechanism of the peristaltic reflex in the isolated guinea-pig ileum. J Physiol 133:681–694
Kramer TH, Shook JE, Kazmierski W, Ayres EA, Wire WS, Hruby VJ, Burks TF (1989) Novel peptidic mu opioid antagonists: Pharmacologic characterization in vitro and in vivo. J Pharmacol Exp Ther 249:544–551
Kromer W (1988) Endogenous and exogenous opioids in the control of gastrointestinal motility and secretion. Pharmacol Rev 40:121–162
Kromer W (1989) The current status of opioid research on gastrointestinal motility. Life Sci 44:579–589
Kromer W (1990) Regulation of intestinal motility by peripheral opioids: Facts and hypotheses. In: OFX Almeida and TS Shippenberg (eds) Opioid peptides and receptors. Biochemistry, physiology and pharmacology. Springer, Berlin (in press)
Kromer W, Pretzlaff W (1979) In vitro evidence for the participation of intestinal opioids in the control of peristalsis in the guinea pig small intestine. Naunyn-Schmiedeberg's Arch Pharmacol 309:153–157
Kromer W, Höllt V, Schmidt H, Herz A (1981a) Release of immunoreactive-dynorphin from the isolated guinea-pig small intestine is reduced during peristaltic activity. Neurosci Letters 25:53–56
Kromer W, Pretzlaff W, Woinoff R (1980) Opioids modulate periodicity rather than efficacy of peristaltic waves in the guinea pig ileum in vitro. Life Sci 26:1857–1865
Kromer W, Pretzlaff W, Woinoff R (1981b) Regional distribution of an opioid mechanism in the guinea-pig isolated intestine. J Pharm Pharmacol 33:98–101
Kromer W, Steigemann N, Shearman GT (1982) Differential effects of SKF 10,047 (N-Allyl-Normetazocine) on peristalsis and longitudinal muscle contractions of the isolated guinea-pig ileum. Naunyn-Schmiedeberg's Arch Pharmacol 321:218–222
Lord JAH, Waterfield AA, Hughes J, Kosterlitz HW (1977) Endogenous opioid peptides: multiple agonists and receptors. Nature 267:495–499
Miller L, Shaw JS, Whiting EM (1986) The contribution of intrinsic activity to the action of opioids in vitro. Br J Pharmac 87:595–601
Portoghese PS, Nagase H, Lipowski AW, Larson DL, Takemori AE (1988) Binaltorphimine-related bivalent ligands and their κ opioid receptor antagonist selectivity. J Med Chem 31:836–841
Ramabadran K, Bansinath M, Turndorf H, Puig MM (1988) Stereospecific inhibition of gastrointestinal transit by κ opioid agonists in mice. Eur J Pharmacol 155:329–331
Schulz R, Wüster M, Rubini P, Herz A (1981) Functional opiate receptors in the guinea-pig ileum: Their differentiation by means of selective tolerance development. J Pharmacol Exp Ther 219:547–550
Smith TW, Hughes J, Kosterlitz HW, Sosa RP (1976) Enkephalins: Isolation, distribution and function. In: HW Kosterlitz (ed) Opiates and endogenous opioid peptides. Elsevier, Amsterdam 1976
Tortella FC (1988) Endogenous opioid peptides and epilepsy: quieting the seizing brain? Trends Pharmacol Sci 9:366–372
Zukin RS, Zukin SR (1984) The case for multiple opiate receptors. Trends Neurosci 7:160–164
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Kromer, W. Reflex peristalsis in the guinea pig isolated ileum is endogenously controlled by kappa opioid receptors. Naunyn-Schmiedeberg's Arch Pharmacol 341, 450–454 (1990). https://doi.org/10.1007/BF00176339
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00176339