Agonist activity of N-desmethylclozapine at δ-opioid receptors of human frontal cortex

European Journal of Pharmacology

Volumn 607, Issue 1-3, 2009, Pages 96-101

  Olianas, Maria C ^a   Dedoni, Simona ^a   Ambu, Rossano ^a   Onali, Pierluigi ^a  

^a UNIVERSITY OF CAGLIARI   (Italy)

Author keywords

opioid receptor; Cyclic AMP; G protein activation; Human frontal cortex; N desmethylclozapine; Receptor binding

Indexed keywords

ACETYLCHOLINE; ATROPINE; CARBACHOL; CLOZAPINE; CLOZAPINE N OXIDE; CYCLIC AMP; DELTA OPIATE RECEPTOR; DEXTRO PHENYLALANYLCYSTEINYLTYROSYL DEXTRO TRYPTOPHYLARGINYLTHREONYLPENICILLAMINYLTHREONINAMIDE 2,7 DISULFIDE; DOPAMINE 2 RECEPTOR; GUANINE NUCLEOTIDE; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); HALOPERIDOL; LEUCINE ENKEPHALIN; NALTRINDOLE; NORBINALTORPHIMINE; NORCLOZAPINE; QUINPIROLE; RADIOLIGAND; SEROTONIN 1A RECEPTOR; UNCLASSIFIED DRUG; WAY100135;

ADULT; AGED; ARTICLE; AUTOPSY; BINDING ASSAY; BRAIN; CLINICAL FEATURE; CONTROLLED STUDY; DRUG BINDING; DRUG EFFICACY; DRUG POTENCY; FRONTAL CORTEX; HUMAN; MALE; MEMBRANE; METABOLITE; PRIORITY JOURNAL;

ADULT; AGED; BINDING, COMPETITIVE; CLOZAPINE; CYCLIC AMP; FRONTAL LOBE; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HUMANS; MALE; MIDDLE AGED; PROTEIN BINDING; RADIOLIGAND ASSAY; RECEPTORS, OPIOID, DELTA;

EID: 62249162153     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2009.02.025     Document Type: Article

References (49)

1. Ackenheil M. Clozapine-pharmacokinetic investigations and biochemical effects in man. Psychopharmacology 99 (1989) S32-S37
2. Aravagiri M., and Marder S.R. Simultaneous determination of clozapine and its N-desmethyl and N-oxide metabolites in plasma by liquid chromatography/electrospray tandem mass spectrometry and its application to plasma level monitoring in schizophrenic patients. J. Pharm. Biomed. Anal 26 (2001) 301-311
3. Bradford M.M. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem 72 (1976) 248-254
4. Broom D.C., Jutkiewicz E.M., Folk J.E., Traynor J.R., Rice K.C., and Woods J.H. Nonpeptidic δ-opioid receptor agonists reduce immobility in the forced swim assay in rats. Neuropsychopharmacology 26 (2002) 744-755
5. 3 partial agonist. J. Pharmacol. Exp. Ther 315 (2005) 1278-1287
6. Centorrino F., Baldessarini R.J., Kando J.C., Frankenburg F.R., Volpicelli S.A., and Flood J.G. Clozapine and metabolites: concentrations in serum and clinical findings during treatment of chronically psychotic patients. J. Clin. Psychopharmacol 14 (1994) 119-125
7. 50) of an enzymatic reaction. Biochem. Pharmacol 22 (1973) 3099-3102
8. Comer S.D., Hoenicke E.M., Sable A.I., McNutt R.W., Chang K.-J., DeCosta B.R., Mosberg H.I., and Woods J.H. Convulsive effects of systemic administration of the delta opioid agonist BW373U86 in mice. J. Pharmacol. Exp. Ther 267 (1993) 888-895
9. 1 agonism a pre-requisite for mimicking clozapine's actions ?. Psychopharmacology 178 (2005) 451-460
10. Farde L. A PET-study of extrastriatal D2-dopamine receptors. Eur. Neuropsychopharmacol. 7 Supp.2 (1997) 129-130
11. Filliol D., Ghozland S., Chluba J., Martin M., Matthes H.W.D., Simonin F., Befort K., Gaveriaux-Ruff C., Dierich A., LeMeur M., Valverde O., Maldonado R., and Kieffer D.L. Mice deficient for δ- and μ-opioid receptors exhibit opposing alterations of emotional responses. Nat. Genet 25 (2000) 195-200
12. Frazier J.A., Cohen L.G., Jacobson L., Grothe D., Flood J., Baldessarini J., Piscitelli S., Kim G.S., and Rapoport J.L. Clozapine pharmacokinetics in children and adolescents with childhood-onset schizophrenia. J. Clin. Psychopharmacol. 23 (2003) 87-91
13. Green A.I., Noordsy D.L., Brunette M.F., O, and Keefe C. Substance abuse and schizophrenia: pharmacotherapeutic intervention. J. Subst. Abuse Treat 34 (2008) 61-71
14. Gulya K. The opioid system in neurologic and psychiatric disorders and their experimental models. Pharmacol. Ther 46 (1990) 395-428
15. Hiller J.M., and Fan L.Q. Laminar distribution of the multiple opioid receptors in the human cerebral cortex. Neurochem. Res 21 (1996) 1333-1345
16. Jann M.W., Grimsley S.R., Gray E.C., and Chang W.H. Pharmacokinetics and pharmacodynamics of clozapine. Clin. Pharmacokinet 24 (1993) 161-176
17. Jutkiewicz E.M. The antidepressant-like effects of delta-opioid receptor agonists. Mol. Interv 6 (2006) 162-169
18. Konig M., Zimmer A.M., Steiner H., Holmes P.V., Crawley J.N., Brownstein M.J., and Zimmer A. Pain responses, anxiety and aggression in mice deficient in pre-proenkephalin. Nature 383 (1996) 535-538
19. Kraus J.E., and Sheitman B.B. Clozapine reduces violent behavior in heterogeneous diagnostic groups. J. Neuropsychiatry Clin. Neurosci 17 (2005) 36-44
20. 1c receptor antagonists. Eur. J. Pharmacol.-Mol. Pharmacol. Sect. 245 (1993) 179-182
21. Lameh J., Burstein E.S., Taylor E., Weiner D.M., Vanover K.E., and Bonhaus D.W. Pharmacology of N-desmethylclozapine. Pharmacol Ther. 115 (2007) 223-231
22. 1 muscarinic receptors. Neuropsychopharmacology 30 (2005) 1986-1995
23. 11C]methyl)naltrindole and PET. Synapse 24 (1996) 19-28
24. Marazziti D., Marracci S., Palego L., Rotondo A., Mozzanti C., Nardi I., Ladinsky H., Giraldo E., Borsini F., and Cassano G.B. Localization and gene expression of serotonin 1A (5HT1A) receptors in human brain postmortem. Brain Res 658 (1994) 55-59
25. Mas Nieto M., Guen S.L.E., Kieffer B.L., Roques B.P., and Noble F. Physiological control of emotion-related behaviors by endogenous encephalins involves essentially the delta opioid receptors. Neuroscience 135 (2005) 305-313
26. Masri B., Salahpour A., Didriksen M., Ghisi V., Beaulieu J.M., Gainetdinov R.R., and Caron M.G. Antagonism of dopamine D2 receptor/β-arrestin 2 interaction is a common property of clinically effective antipsychotics. Proc. Natl. Acad. Sci. USA 105 (2008) 13656-13661
27. Mauri M.C., Volontari L.S., Dell, Osso B., Regispani F., Papa P., Baldi M., and Bareggi S.R. Predictors of clinical outcome in schizophenic patients responding to clozapine. J Clin. Psychopharmacol. 23 (2003) 660-664
28. McElroy S.L., Dessain E.C., Pope Jr. H.G., Cole J.O., Keck Jr. P.E., Frankenberg F.R., Alzley N.G., O, and Brien S. Clozapine in the treatment of psychotic mood disorders, schizoaffective disorder, and schizophrenia. J. Clin. Psychiatry 52 (1991) 411-414
29. Meltzer H.Y., Alphs L., Green A.I., Altamura A.C., Anand R., Bertoldi A., Bourgeois M., Choulnard G., Islam M.Z., Kane J., Krishnan R., Lindenmayer J.P., and Potkin S. Clozapine treatment for suicidality in schizophrenia: International Suicide Prevention Trial (InterSePT). Arch. Gen. Psychiatry 60 (2003) 82-91
30. Metcalf M.D., and Coop A. Kappa opioid antagonists: past successes and future prospects. AAPS J 7 (2005) E704-E722
31. Munson P.J., and Rodbard D. Ligand: a versatile computerized approach for the characterization of ligand binding systems. Anal. Biochem 107 (1980) 220-239
32. Olesen O.V., Thomsen K., Jensen P.N., Wulff C.H., Rasmussen N.A., Refshammer C., Sorensen J., Bysted M., Christensen J., and Rosemberg R. Clozapine serum levels and side effects during steady state treatment of schizophrenic patients: a cross-sectional study. Psychopharmacology 117 (1995) 371-378
33. Olianas M.C., Concas D., and Onali P. Agonist activity of naloxone benzohylhydrazone at recombinant and native receptors. Br. J. Pharmacol 147 (2006) 360-370
34. Olianas M.C., Maullu C., and Onali P. Effects of clozapine on rat striatal muscarinic receptors coupled to inhibition of adenylyl cyclase activity and on the human cloned m4 receptor. Br. J. Pharmacol 122 (1997) 401-408
35. Olianas M.C., Maullu C., and Onali P. Mixed agonist-antagonist properties of clozapine at different human cloned muscarinic receptor subtypes expressed in Chinese hamster ovary cells. Neuropsychopharmacology 20 (1999) 263-270
36. 35S]thiotriphosphate) binding by cholinergic muscarinic receptors in membranes of rat olfactory bulb. J. Neurochem. 67 (1996) 2549-2556
37. Onali P., and Olianas M.C. N-desmethylclozapine, a major clozapine metabolite, acts as a selective and efficacious δ-opioid agonist at recombinant and native receptors. Neuropsychopharmacology 32 (2007) 773-785
38. 32P in situ hybridization study. Neuroscience 88 (1999) 1093-1135
39. Quock R.M., Burkey T.H., Varga E., Hosohata Y., Hosohata K., Cowell S.M., Slate C.A., Ehlert F.J., Roeske W.R., and Yamamura H.I. The delta-opioid receptor: molecular pharmacology, signal transduction, and the determination of drug efficacy. Pharmacol. Rev. 51 (1999) 503-532
40. 3H]ketanserin binding sites in autopsied brain tissue from cirrhotic patients with hepatic encephalopathy. Neurosci. Lett 182 (1994) 69-72
41. Roberts A.J., Gold L.H., Polls I., McDonald J.S., Filliol D., Kieffer B.L., and Koob G.F. Increased ethanol self-administration in δ-opioid receptor knockout mice. Alcohol Clin. Exp. Res 25 (2001) 1249-1256
42. Saito A., Yoshikawa Y., Onodera K., and Kamei J. Role of δ-opioid receptor subtypes in anxiety-related behaviours in the elevated plus-maze in rats. Psychopharmacology 182 (2005) 327-334
43. Sporn A.L., Vermani A., Greenstein D.K., Bobb A.J., Spencer E.P., Clasen L.S., Tossel J.W., Stayer C.C., Gochman P.A., Lenane M.C., Rapoport J.L., and Gogtay N. Clozapine treatment of childhood-onset schizophrenia: evaluation of effectiveness, adverse effects, and long-term outcome. J. Am. Acad. Child. Adolesc. Psychiatry 46 (2007) 1349-1356
44. Sur C., Mallorga P.J., Wittmann M., Jacobson M.A., Pescarella D., Williams J.B., Brandish P.E., Pettibone D.J., Scolnick E.M., and Conn P.J. N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. Proc. Natl. Acad. Sci. USA 100 (2003) 13674-13679
45. Toth P., and Frankenburg F.R. Clozapine and seizure: a review. Can. J. Psychiatry 39 (1994) 36-238
46. Weigmann H., Hartter S., Fischer V., Dahmen N., and Hiemke C. Distribution of clozapine and desmethylclozapine between blood and brain in rats. Eur. Neuropsychopharmacology 9 (1999) 253-256
47. 1 muscarinic receptor agonism of N-desmethylclozapine in the unique clinical effects of clozapine. Psychopharmacology 177 (2004) 207-216
48. Werling L.L., Puttfarcken P.S., and Cox B.M. Multiple agonist-affinity states of opioid receptors: regulation of binding by guanyl nucleotides in guinea pig cortical, NG108-15, and 7315c cell membranes. Mol. Pharmacol 33 (1988) 423-431
49. Zarate Jr. C.A., Tohen M., and Baldessarini R.J. Clozapine in severe mood disorders. J. Clin. Psychiatry 56 (1995) 411-417