Endomorphin-1 and endomorphin-2 activate μ-opioid receptors in myenteric neurons of the guinea-pig small intestine

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 358, Issue 6, 1998, Pages 686-689

  Tonini, M ^a   Fiori, E ^a   Balestra, B ^a   Spelta, V ^a   D'Agostino, G ^a   Di Nucci, A ^a   Brecha, N C ^b   Sternini, C ^b  

^a UNIVERSITY OF PAVIA   (Italy)

^b UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

Endomorphin 2; Endomorphin l; Guinea pig ileum; Longitudinal muscle myenteric plexus preparation; Opioid receptor antagonists; Opioid receptors

Indexed keywords

ACETYLCHOLINE; DEXTRO PHENYLALANYLCYSTEINYLTYROSYL DEXTRO TRYPTOPHYLORNITHYLTHREONYLPENICILLAMINYLTHREONINAMIDE 2,7 DISULFIDE; ENDOMORPHIN 1; ENDOMORPHIN 2; MU OPIATE RECEPTOR; NALTRINDOLE; NORBINALTORPHIMINE;

ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; FEMALE; GUINEA PIG; ILEUM; MALE; MUSCLE TWITCH; MYENTERIC PLEXUS; NONHUMAN;

EID: 0031671970     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/PL00005313     Document Type: Article

References (18)

1. Arunlakshana O, Schild HO (1959) Some quantitative uses of drug antagonists. Br J Pharmacol Chemother 14:48-58
2. Corbett AD, Kosterlitz HW, McKnight AT, Paterson SJ, Robson LE (1985) Pre-incubation of guinea-pig myenteric plexus with β-funaltrexamine: discrepancy between binding assays and bioassays. Br J Pharmacol 85:665-673
3. Dhawan BN, Cesselin F, Raghubir R, Reisine T, Bradley PB, Portoghese PS, Hamon M (1996) International Union of Pharmacology. XII. Classification of opioid receptors. Pharmacol Rev 48:567-592
4. Galligan JJ (1993) Differential inhibition of cholinergic and noncholinergic neurogenic contractions by mu opioid and alpha-2 adrenergic agonists in guinea pig ileum. J Pharmacol Exp Ther 264:375-383
5. Goldstein A, Naidu A (1989) Multiple opioid receptors: ligands selectivity profiles and binding site signature. Mol Pharmacol 36:265-272
6. Hackler L, Zadina JE, Ge L-J, Kastin AJ (1997) Isolation of relatively large amounts of endomorphin-1 and endomorphin-2 from human brain cortex. Peptides 18:1635-1639
7. Hahn A, Allescher D (1998) Effect of endomorphin-1 and endomorphin-2 on the ascending and descending reflex pathway in rat intestine. Gastroenterology 114:A759
8. Hosohata K, Burkey TH, Alfaro-Lopez J, Varga E, Hruby VJ, Roeske WR, Yamamura HI (1998) Endomorphin-1 and endomorphin-2 are partial agonists at the human μ-opioid receptor. Eur J Pharmacol 346:111-114
9. Kenakin T (1995) Efficacy as the molecular property of ligand. Trends Pharmacol Sci 16:84-85
10. Kilbinger H (1982) The myenteric plexus-longitudinal muscle preparation. In: Hanin I, Goldberg AM (eds) Progress in cholinergic biology: model of cholinergic synapses. Raven Press, New York, pp 147-167
11. 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
12. McConalogue K, Grady EF, Minnis J, Balestra B, Tonini M, Brecha NC, Bunnet NW, Sternini C (1998) Activation and internalization of the μ-opioid receptor by the newly discovered endogenous agonists, endomorphin-1 and endomorphin-2. Neuroscience (in press)
13. Mulder AH, Wardeh G, Hogenboom F, Kazmierski W, Hruby VJ, Schoffelmeer ANM (1991) Cyclic somatostatin analogues as potent antagonists at μ-, but not δ- and κ-opioid receptors mediating presynaptic inhibition of neurotransmitter release in the brain. Eur J Pharmacol 205:1-6
14. Paton WDM, Zar A (1968) The origin of acetylcholine released from guinea-pig intestine and longitudinal muscle strips. J Physiol (Lond) 194:13-33
15. 35S]GTPγS binding in rat brain: evidence for partial agonist activity at μ-opioid receptor. J Neurochem 70:1567-1576
16. Tallarida RJ, Murray RB (1986) Manual of pharmacologic calculations with computer programs, 2nd edn. Springer, Berlin Heidelberg New York
17. Toll L (1992) Comparison of mu opioid receptor binding on intact neuroblastoma cells with guinea pig brain and neuroblastoma cell membranes. J Pharmacol Exp Ther 260:9-15
18. Zadina JE, Hackler L, Ge L-J, Kastin AJ (1997) A potent and selective endogenous agonist for the μ-opiate receptor. Nature 386:499-502