[3H]Alvimopan binding to the μ opioid receptor: Comparative binding kinetics of opioid antagonists

European Journal of Pharmacology

Volumn 520, Issue 1-3, 2005, Pages 29-36

  Cassel, Joel A ^a   Daubert, Jeffrey D ^a   DeHaven, Robert N ^a  

^a ADOLOR CORPORATION   (United States)

Author keywords

Alvimopan; Kinetics; N methylnaltrexone; Opioid antagonist; Opioid receptor

Indexed keywords

17 METHYLNALTREXONE; ALVIMOPAN; BUPRENORPHINE; MU OPIATE RECEPTOR; NALOXONE; OPIATE ANTAGONIST; PARTIAL AGONIST; TRITIUM;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING KINETICS; CHO CELL; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG MECHANISM; DRUG POTENCY; FEMALE; INCUBATION TIME; NONHUMAN; PRIORITY JOURNAL;

ANALGESICS, OPIOID; ANIMALS; BINDING, COMPETITIVE; BUPRENORPHINE; CHO CELLS; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HUMANS; KINETICS; NALOXONE; PIPERIDINES; RECEPTORS, OPIOID, MU; TIME FACTORS; TRANSFECTION; TRITIUM;

EID: 25444478115     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2005.08.008     Document Type: Article

References (29)

1. R.A. Boas, and J.W. Villiger Clinical actions of fentanyl and buprenorphine: the significance of receptor binding Br. J. Anaesth. 57 1985 192 196
2. D.R. Brown, and L.I. Goldberg The use of quaternary narcotic antagonists in opiate research Neuropharmacology 24 1985 181 191
3. R.E. Bullingham, H.J. McQuay, and R.A. Moore Clinical pharmacokinetics of narcotic agonist-antagonist drugs Clin. Pharmacokinet. 8 1983 332 343
4. A. Cowan, J.W. Lewis, and I.E. MacFarlane Agonist and antagonist properties of buprenorphine, a new antinociceptive agent Br. J. Pharmacol. 60 1977 537 545
5. J.A. Culpepper-Morgan, C.E. Inturrisi, R.K. Portenoy, K. Foley, R.W. Houde, F. Marsh, and M.-J. Kreek Treatment of opioid-induced constipation with oral naloxone: a pilot study Clin. Pharmacol. Ther. 52 1992 90 95
6. J.D. Daubert, J.A. Cassel, D. Guo, E.K. Gauntner, V. Kumar, E. Mansson, and R.N. DeHaven Inhibition of opioid receptor-mediated [35S]GTPγS binding by ADL 8-2698, a potent opioid receptor antagonist Soc. Neurosci. Abstr. 26 2000 635
7. DeHaven, R.N., Little, P.J., Cassel, J.A., Gottshall, S.L., Koblish, M., Long, S., Wiant, D.D., Guo, D., Mansson, E., Daubert, J.D., DeHaven-Hudkins, D., in preparation. In vitro and in vivo pharmacology of alvimopan, a novel, peripherally acting opioid antagonist.
8. C.P. Delaney, J.L. Weese, N.H. Hyman, J. Bauer, L. Techner, K. Gabriel, W. Du, W.K. Schmidt, and B.A. Wallin Phase III trial of alvimopan, a novel, peripherally acting, mu opioid antagonist, for postoperative ileus after major abdominal surgery Dis. Colon Rectum 48 2005 1114 1129
9. J.R. Fricke, D. Linquist, and R.L. Carpenter ADL 8-2698 does not antagonize opioid analgesia Clin. Pharmacol. Ther. 67 2000 93
10. J.F. Foss A review of the potential role of methylnaltrexone in opioid bowel dysfunction Am. J. Surg. 182 2001 19S 26S
11. S. Kim, H.N. Wagner Jr., V.L. Villemagne, P.F. Kao, R.F. Dannals, H.T. Ravert, T. Joh, R.B. Dixon, and A.C. Civelek Longer occupancy of opioid receptors by nalmefene compared to naloxone as measured in vivo by a dual-detector system J. Nucl. Med. 38 1997 1726 1731
12. M.-J. Kreek, R.A. Schaefer, E.F. Hahn, and J. Fishman Naloxone, a specific opioid antagonist, reverses chronic idiopathic constipation Lancet 1 1983 261 262
13. L.E. Limbird Cell Surface Receptors: A Short Course on Theory and Methods second ed. 1996 Kulwer Academic Publishers Norwell, MA
14. P.J. Little, M. Koblish, D.L. DeHaven-Hudkins, M.R. Pietras, and A. Cowan ADL 8-2698, a GI restricted opioid antagonist, blocks the antisecretory and colorectal transit effects of morphine and loperamide Soc. Neurosci. Abstr. 27 2001 907.2
15. S.L. Long, P.J. Little, F. Gaul, D. Guo, M. Koblish, and D.L. DeHaven-Hudkins Effects of novel μ opioid antagonists on gastrointestinal (GI) transit in mice Soc. Neurosci. Abstr. 25 1999 1706
16. L. Manara, G. Bianchi, P. Ferretti, and A. Tavani Inhibition of gastrointestinal transit by morphine in rats results primarily from direct drug action on gut opioid sites J. Pharmacol. Exp. Ther. 237 1986 945 949
17. H.J. Motulsky Analyzing Data with GraphPad Prism 1999 GraphPad Software Inc. San Diego, CA
18. H.J. Motulsky, and L.C. Mahan The kinetics of competitive radioligand binding predicted by the law of mass action Mol. Pharmacol. 25 1984 1 9
19. D.B. Murphy, J.A. Sutton, L.F. Prescott, and M.B. Murphy Opioid-induced delay in gastric emptying: a peripheral mechanism in humans Anesthesiology 87 1997 765 770
20. D.M. Paulson, D.T. Kennedy, R.A. Donovick, R.L. Carpenter, M. Cherubini, L. Techner, W. Du, Y. Ma, W.K. Schmidt, B.A. Wallin, and D. Jackson Alvimopan: an oral, peripherally acting, μ-opioid receptor antagonist for the treatment of opioid-induced bowel dysfunction - a 21 day treatment-randomized clinical trial J. Pain 6 2005 184 192
21. T. Reisine, and G. Pasternak Opioid analgesics and antagonists J.G. Hardman L.E. Limbird P.G. Molinoff R.W. Ruddon A.G. Gilman Goodman and Gilman's The Pharmacological Basis of Therapeutics ninth ed. 1996 McGraw-Hill New York 521 555
22. W.K. Schmidt Alvimopan (ADL 8-2698) is a novel peripheral opioid antagonist Am. J. Surg. 182 2001 27S 38S
23. A. Taguchi, N. Sharma, R.M. Saleem, D.I. Sessler, R.L. Carpenter, M. Seyedsadr, and A. Kurz Selective postoperative inhibition of gastrointestinal opioid receptors N. Engl. J. Med. 345 2001 935 940
24. A. Tavani, G. Bianchi, P. Ferretti, and L. Manara Morphine is most effective on gastrointestinal propulsion in rats by intraperitoneal route: evidence for local action Life Sci. 27 1980 2211 2217
25. B.G. Wolff, F. Michelassi, T.M. Gerkin, L. Techner, K. Gabriel, W. Du, and B.A. Wallin Alvimopan, a novel, peripherally acting μ opioid antagonist Ann. Surg. 240 2004 728 735
26. C.-S. Yuan, J.F. Foss, M. O'Connor, A. Toledano, M.F. Roizen, and J. Moss Methylnaltrexone prevents morphine-induced delay in oral-cecal transit time without affecting analgesia: a double-blind randomized placebo-controlled trial Clin. Pharmacol. Ther. 59 1996 469 475
27. C.-S. Yuan, J.F. Foss, M. O'Connor, T. Karrison, J. Osinski, M.F. Roizen, and J. Moss Effects of enteric-coated methylnaltrexone in preventing opioid-induced delay in oral-cecal transit time Clin. Pharmacol. Ther. 67 2000 398 404
28. D.M. Zimmerman, J.S. Gidda, B.E. Cantrell, D.D. Schoepp, B.G. Johnson, and J.D. Leander Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders J. Med. Chem. 37 1994 2262 2265
29. D.M. Zimmerman, J.S. Gidda, B.E. Cantrell, J.A. Werner, C.J. Parli, R.B. Franklin, P.C. Francis, and J.D. Leander LY246736 dihydrate: μ opioid receptor antagonist Drugs Future 19 1994 1078 1083