An Index of Relative Central α-Adrenergic Receptor Antagonism by Antipsychotic Medications

Experimental and Clinical Psychopharmacology

Volumn 19, Issue 1, 2011, Pages 31-39

  Minzenberg, Michael J ^a   Yoon, Jong H ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

adrenergic; Antipsychotic; Atypical; Neuroleptic

Indexed keywords

ALPHA 1 ADRENERGIC RECEPTOR; ALPHA 2 ADRENERGIC RECEPTOR; ARIPIPRAZOLE; ATYPICAL ANTIPSYCHOTIC AGENT; CHLORPROMAZINE; CLOZAPINE; FLUPHENAZINE; HALOPERIDOL; LOXAPINE; MOLINDONE; NEUROLEPTIC AGENT; OLANZAPINE; PERPHENAZINE; PIMOZIDE; QUETIAPINE; RISPERIDONE; TIOTIXENE; TRIFLUOPERAZINE; ZIPRASIDONE;

ALPHA ADRENERGIC RECEPTOR BLOCKING; ARTICLE; COGNITION; HUMAN; NONHUMAN; RECEPTOR BINDING;

ADRENERGIC ALPHA-ANTAGONISTS; ANTIPSYCHOTIC AGENTS; BRAIN; HALOPERIDOL; HUMANS; RECEPTORS, ADRENERGIC, ALPHA; UNITED STATES;

EID: 79952086694     PISSN: 10641297     EISSN: 19362293     Source Type: Journal    
DOI: 10.1037/a0022258     Document Type: Article

References (60)

1. Andreasen N.C., Pressler M., Nopoulos P., Miller D., Ho B.-C. Antipsychotic dose equivalents and dose-years: A standardized method for comparing exposure to different drugs. Biological Psychiatry 2010, 67:255-262.
2. Arnsten A.F. Catecholamine and second messenger influences on prefrontal cortical networks of " representational knowledge": A rational bridge between genetics and the symptoms of mental illness. Cerebral Cortex 2007, 17(Suppl. 1):i6-i15.
3. Arnt J., Skarsfeldt T. Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence. Neuropsychopharmacology 1998, 18:63-101.
4. Berridge C.W., Abercrombie E.D. Relationship between locus coeruleus discharge rates and rates of norepinephrine release within neocortex as assessed by in vivo microdialysis. Neuroscience 1999, 93:1263-1270.
5. Blake T.J., Tillery C.E., Reynolds G.P. Antipsychotic drug affinities at alpha2-adrenoceptor subtypes in post-mortem human brain. Journal of Psychopharmacology 1998, 12:151-154.
6. Brea J., Castro M., Loza M.I., Masaguer C.F., Ravina E., Dezi C., Robledo P. QF2004B, a potential antipsychotic butyrophenone derivative with similar pharmacological properties to clozapine. Neuropharmacology 2006, 51:251-262.
7. Brooks K.M., Cai J., Sandrasagra A., Roehr J.E., Errazo R., Vargas H.M. Interaction of clozapine and other antipsychotic drugs with human alpha 1-adrenergic receptor subtypes. Proceedings of the Western Pharmacology Society 1999, 42:67-69.
8. Bylund D.B. Subtypes of alpha 2-adrenoceptors: Pharmacological and molecular biological evidence converge. Trends in Pharmacological Sciences 1988, 9:356-361.
9. Bylund D.B. Alpha-2 adrenoceptor subtypes: Are more better?. British Journal of Pharmacology 2005, 144:159-160.
10. Bymaster F.P., Calligaro D.O., Falcone J.F., Marsh R.D., Moore N.A., Tye N.C., Wong D.T. Radioreceptor binding profile of the atypical antipsychotic olanzapine. Neuropsychopharmacology 1996, 14:87-96.
11. Civantos Calzada B., de Artiñano A.A. Alpha-adrenoceptor subtypes. Pharmacological Research 2001, 44:195-208.
12. Cooper J.R., Bloom F.E., Roth R.H. The biochemical basis of neuropharmacology 2003, Oxford University Press, Oxford, England. 8th ed.
13. Creese I., Burt D.R., Snyder S.H. Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science 1976, April 30, 192:481-483.
14. Davis J.M. Dose equivalence of the antipsychotic drugs. Journal of Psychiatric Research 1974, 11:65-69.
15. Glick I.D., Murray S.R., Vasudevan P., Marder S.R., Hu R.J. Treatment with atypical antipsychotics: New indications and new populations. Journal of Psychiatric Research 2001, 35:187-191.
16. Green M.F. What are the functional consequences of neurocognitive deficits in schizophrenia?. The American Journal of Psychiatry 1996, 153:321-330.
17. Hals P.-A., Hall H., Dahl S.G. Phenothiazine drug metabolites: Dopamine D2 receptor, α2- and α2-adrenoceptor binding. European Journal of Pharmacology 1986, 125:373-381.
18. Hertel P., Didriksen M., Pouzet B., Brennum L.T., Soby K.K., Larsen A.K., Arnt J. Lu 35-138 ((+)-(S)-3-{1-[2- (1-acetyl-2,3-dihydro-1H-indol-3-yl)ethyl]-3,6-dihydro-2H-pyridin- 4-yl}-6-chloro-1H-indole), a dopamine D4 receptor antagonist and serotonin reuptake inhibitor: Characterisation of its in vitro profile and pre-clinical antipsychotic potential. European Journal of Pharmacology 2007, 573:148-160.
19. Kalkman H.O., Subramanian N., Hoyer D. Extended radioligand binding profile of iloperidone: A broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders. Neuropsychopharmacology 2001, 25(6):904-914.
20. Kroeze W.K., Hufeisen S.J., Popadak B.A., Renock S.M., Steinberg S., Ernsberger P., Roth B.L. H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology 2003, 28:519-526.
21. Lameh J., Burstein E.S., Taylor E., Weiner D.M., Vanover K.E., Bonhaus D.W. Pharmacology of N-desmethylclozapine. Pharmacy and Therapeutics 2007, 115:223-231.
22. Lange J.H., Reinders J.H., Tolboom J.T., Glennon J.C., Coolen H.K., Kruse C.G. Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. Journal of Medicinal Chemistry 2007, 50:5103-5108.
23. Leysen J.E., Gommeren W., Eens A., de Chaffoy de Courcelles D., Stoof J.C., Janssen P.A. Biochemical profile of risperidone, a new antipsychotic. Journal of Pharmacology and Experimental Therapeutics 1988, 247(2):661-670.
24. Leysen J.E., Janssen P.M., Gommeren W., Wynants J., Pauwels P.J., Janssen P.A. In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone. Molecular Pharmacology 1992, 41:494-508.
25. Leysen J.E., Janssen P.M., Schotte A., Luyten W.H., Megens A.A. Interaction of antipsychotic drugs with neurotransmitter receptor sites in vitro and in vivo in relation to pharmacological and clinical effects: Role of 5HT2 receptors. Psychopharmacology (Berl) 1993, 112(Suppl. 1):S40-S54.
26. Liao Y., Venhuis B.J., Rodenhuis N., Timmerman W., Wikstrom H., Meier E., Sundell S. New (sulfonyloxy) piperazinyldibenzazepines as potential atypical antipsychotics: Chemistry and pharmacological evaluation. Journal of Medicinal Chemistry 1999, 42:2235-2244.
27. Mackin P. Cardiac side effects of psychiatric drugs. Human Psychopharmacology 2008, 23(Suppl. 1):3-14.
28. Michelsen J.W., Meyer J.M. Cardiovascular effects of antipsychotics. Expert Review of Neurotherapeutics 2007, 7:829-839.
29. Millan M.J., Brocco M., Rivet J.M., Audinot V., Newman-Tancredi A., Maiofiss L., Peglion J.L. S18327 (1-[2-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)piperid-1-yl]ethyl]3-phenyl imidazolin-2-one), a novel, potential antipsychotic displaying marked antagonist properties at alpha(1)- and alpha(2)-adrenergic receptors: II. Functional profile and a multiparametric comparison with haloperidol, clozapine, and 11 other antipsychotic agents. Journal of Pharmacology and Experimental Therapeutics 2000, 292:54-66.
30. Minzenberg M.J., Laird A.R., Thelen S., Carter C.S., Glahn D.C. Meta-analysis of 41 functional neuroimaging studies of executive function in schizophrenia. Archives of General Psychiatry 2009, 66:811-822.
31. Minzenberg M.J., Poole J.H., Benton C., Vinogradov S. Association of anticholinergic load with impairment of complex attention and memory in schizophrenia. The American Journal of Psychiatry 2004, 161:116-124.
32. Minzenberg M.J., Watrous A.J., Yoon J.H., Ursu S., Carter C.S. Modafinil shifts human locus coeruleus to low-tonic, high-phasic activity during functional MRI. Science 2008, December 12, 322:1700-1702.
33. Morimoto T., Hashimoto K., Yasumatsu H., Tanaka H., Fujimura M., Kuriyama M., Yamagami K. Neuropharmacological profile of a novel potential atypical antipsychotic drug Y-931 (8-fluoro-12-(4-methylpiperazin-1-yl)- 6H-[1]benzothieno[2,3-b][1,5] benzodiazepine maleate). Neuropsychopharmacology 2002, 26:456-467.
34. Muller D.J., Kennedy J.L. Genetics of antipsychotic treatment emergent weight gain in schizophrenia. Pharmacogenomics 2006, 7:863-887.
35. Osman O.T., Becker R.E. Neuroleptics and their metabolites binding to alpha 1 and D2 receptors. Biological Psychiatry 1988, 24:815-818.
36. Peroutka S.J., Synder S.H. Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency. The American Journal of Psychiatry 1980, 137:1518-1522.
37. Peroutka S.J., U'Prichard D.C., Greenberg D.A., Snyder S.H. Neuroleptic drug interactions with norepinephrine alpha receptor binding sites in rat brain. Neuropharmacology 1977, 16:549-556.
38. Richelson E. Neuroleptic affinities for human brain receptors and their use in predicting adverse effects. Journal of Clinical Psychiatry 1984, 45:331-336.
39. Richelson E., Nelson A. Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro. European Journal of Pharmacology 1984, 103:197-204.
40. Richelson E., Souder T. Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sciences 2000, 68:29-39.
41. The roadmap for antipsychotic psychopharmacology: An overview. Journal of Clinical Psychiatry 2007, 68:1799-1806. Roadmap Editorial Board.
42. Robbins T.W., Roberts A.C. Differential regulation of fronto-executive function by the monoamines and acetylcholine. Cerebral Cortex 2007, 17(Suppl. 1):i151-i160.
43. Roth B.L., Sheffler D.J., Kroeze W.K. Magic shotguns versus magic bullets: Selectively non-selective drugs for mood disorders and schizophrenia. Nature Reviews Drug Discovery 2004, 3:353-359.
44. Sanchez C., Arnt J., Dragsted N., Hyttel J., Lembol H.L., Meier E., Skarsfeldt T. Neurochemical and in vivo pharmacological profile of sertindole, a limbic-selective neuroleptic compound. Drug Development Research 1991, 22:239-250.
45. Schmidt A.W., Lebel L.A., Howard H.R., Zorn S.H. Ziprasidone: A novel antipsychotic agent with a unique human receptor binding profile. European Journal of Pharmacology 2001, 425:197-201.
46. Schotte A., Bonaventure P., Janssen P.F., Leysen J.E. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: Risperidone compared with antipsychotics hitherto used. Japanese Journal of Pharmacology 1995, 69:399-412.
47. Schotte A., Janssen P.F., Gommeren W., Luyten W.H., Van Gompel P., Lesage A.S., Leysen J.E. Risperidone compared with new and reference antipsychotic drugs: In vitro and in vivo receptor binding. Psychopharmacology (Berl) 1996, 124:57-73.
48. Seeger T.F., Seymour P.A., Schmidt A.W., Zorn S.H., Schulz D.W., Lebel L.A., Lowe J.A. Ziprasidone (CP-88,059): A new antipsychotic with combined dopamine and serotonin receptor antagonist activity. Journal of Pharmacology and Experimental Therapeutics 1995, 275:101-113.
49. Seeman P., Lee T., Chau-Wong M., Wong K. Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature 1976, June 24, 261:717-719.
50. Sekine Y., Rikihisa T., Ogata H., Echizen H., Arakawa Y. Correlations between in vitro affinity of antipsychotics to various central neurotransmitter receptors and clinical incidence of their adverse drug reactions. European Journal of Clinical Pharmacology 1999, 55:583-587.
51. Shahid M., Walker G.B., Zorn S.H., Wong E.H.F. Asenapine: A novel psychopharmacologic agent with a unique human receptor signature. Journal of Psychopharmacology 2009, 23:65-73.
52. Sleight A.J., Koek W., Bigg D.C. Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: Risperidone is selective for the alpha 1B-adrenoceptors. European Journal of Pharmacology 1993, 238:407-410.
53. Subramanian N., Kalkman H.O. Receptor profile of P88-8991 and P95-12113, metabolites of the novel antipsychotic iloperidone. Progress in Neuro-Psychopharmacology and Biological Psychiatry 2002, 26:553-560.
54. Svensson T.H. Alpha-adrenoceptor modulation hypothesis of antipsychotic atypicality. Progress in Neuro-Psychopharmacology and Biological Psychiatry 2003, 27:1145-1158.
55. Szewczak M.R., Corbett R., Rush D.K., Wilmot C.A., Conway P.G., Strupczewski J.T., Cornfeldt M. The pharmacological profile of iloperidone, a novel atypical antipsychotic agent. Journal of Pharmacology and Experimental Therapeutics 1995, 274:1404-1413.
56. Testa R., Abbiati G., Ceserani R., Restelli G., Vanasia A., Barone D., Mennini T. Profile of in vitro binding affinities of neuroleptics at different rat brain receptors: Cluster analysis comparison with pharmacological and clinical profiles. Pharmaceutical Research 1989, 6:571-577.
57. Tsukamoto T., Asakura M., Hirata N., Imafuku J., Matsui H., Hasegawa K. Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: A possible relationship between alpha 2-receptor antagonism and antidepressant action. Biological Psychiatry 1984, 19:1283-1291.
58. Wang J.-F., Min J.-Y., Hampton T.G., Amende I., Yan X., Malek S., Morgan J.P. Clozapine-induced myocarditis: Role of catecholamines in a murine model. European Journal of Pharmacology 2008, 592:123-127.
59. Weiner D.M., Meltzer H.Y., Veinbergs I., Donohue E.M., Spalding T.A., Smith T.T., Brann M.R. The role of M1 muscarinic receptor agonism of N-desmethylclozapine in the unique clinical effects of clozapine. Psychopharmacology 2004, 177:207-216.
60. Woods S.W. Chlorpromazine equivalent doses for the newer atypical antipsychotics. Journal of Clinical Psychiatry 2003, 64:663-667.