Forty years of antipsychotic drug research - From haloperidol to paliperidone - with Dr. Paul Janssen

Arzneimittel-Forschung/Drug Research

Volumn 57, Issue 10, 2007, Pages 625-632

  Awouters, Frans H L ^a   Lewi, Paul J ^b,c,d  

^a University Hospital ^*  (Belgium)

^b UNIVERSITY OF LEUVEN   (Belgium)

^c VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

^d NONE   (Belgium)

Author keywords

Antipsychotics; Benzoxazolylpiperidines; Butyrophenones; Diphenylbutylpiperidines; Dopamine antagonism; Neuroleptics

Indexed keywords

AMBUCETAMIDE; ANALGESIC AGENT; ATYPICAL ANTIPSYCHOTIC AGENT; AZAPERONE; BENPERIDOL; BROMPERIDOL; BROMPERIDOL DECANOATE; BUTYROPHENONE DERIVATIVE; CHLORPROMAZINE; CHOLINERGIC RECEPTOR BLOCKING AGENT; DOPAMINE RECEPTOR; DROPERIDOL; FLUANISONE; FLUSPIRILENE; HALOPERIDOL; HALOPERIDOL DECANOATE; ISOPROPAMIDE IODIDE; MOPERONE; MORPHINE; NEUROLEPTIC AGENT; OCAPERIDONE; PALIPERIDONE; PENFLURIDOL; PETHIDINE; PIMOZIDE; PIPAMPERONE; R 1187; R 1472; RISPERIDONE; SEROTONIN; SEROTONIN 2 ANTAGONIST; SETOPERONE; SPASMOLYTIC AGENT; SPIPERONE; UNCLASSIFIED DRUG;

BELGIUM; DRUG EFFICACY; DRUG INDICATION; DRUG RESEARCH; EXTRAPYRAMIDAL SYMPTOM; HEBEPHRENIA; HUMAN; HYPOTENSION; NEGATIVE SYNDROME; NONHUMAN; PATIENT COMPLIANCE; RECEPTOR BINDING; REVIEW; SCHIZOPHRENIA; STEREOTYPY;

EID: 35948937147     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0031-1296660     Document Type: Review

References (67)

1. Janssen PAJ, Niemegeers CJ, Schellekens KH. Is it possible to predict the clinical effects of neuroleptic drugs (major tranquilizers) from animal data? Part I "Neuroleptic activity spectra" for rats. Arzneimittel- Forschung (Drug Research). 1965;15:104-117.
2. Janssen PAJ, Niemegeers CJ, Schellekens KH. Is it possible to predict the clinical effects of neuroleptic drugs (major tranquilizers) from animal data? Part II "Neuroleptic activity spectra" for dogs. Arzneimittel- Forschung (Drug Research). 1965;15:1196-1206.
3. Janssen PAJ, Niemegeers CJ, Schellekens KH. Is it possible to predict the clinical effects of neuroleptic drugs (major tranquilizers) from animal data? Part III The subcutaneous and oral activity in rats and dogs of 56 neuroleptic drugs in the jumping box test. Arzneimittel-Forschung (Drug Research). 1966;16:339-346.
4. Janssen PAJ, Niemegeers CJ, Schellekens KH, Lenaerts FM. Is it possible to predict the clinical effects of neuroleptic drugs (major tranquilizers) from animal data? Part IV An improved experimental design for measuring the inhibitory effects of neuroleptic drugs on amphetamine- or apomorphine-induced "chewing" and "agitation" in rats. Arzneimittel-Forschung (Drug Research). 1967;17:841-854.
5. Janssen PAJ, Awouters FHL. Is it possible to predict the clinical effects of neuroleptic drugs from animal data? Part V From haloperidol and pipamperone to risperidone. Arzneimittel-Forschung (Drug Research). 1994;44:269-277.
6. Smith A.The conductorless orchestra. Nat Rev Drug Disc. 2004;3:3.
7. Schwartz H. The discovery of modern medicines. Morris Plains NJ: Skyline Publ Group; 1989.
8. Curzon G. How reserpine and chlorpromazine act: the impact of key discoveries on the history of psychopharmacology. TiPS. 1990;11:61-63.
9. Courvoisier S, Fournet J, Ducrot R, Kolsky M, Koetschet P. Propriétés pharmacodynamiques du chlorhydrate de chloro-3-(dimethylamino-3′-propyl)-10-phenothiazine (4560 R.P.). Etude expérimentale d'un nouveau corps utilisee dans l'anesthésie potentialisée et dans l'hibernation artificielle. Arch Int Pharmacodyn. 1953;92:305-361.
10. Carlsson A, Lindqvist M. Effect of chlorpromazine or haloperidol on formation of 3-methoxytyramine and normetanephrine in mouse brain. Acta Pharmacol Toxicol. 1963;20:140-144.
11. Andén NE, Carlsson A, Dahlstroem A, Fuxe K, Hillarp NA, Larsson K. Demonstration and mapping out of nigro-neostriatal dopamine neurons. Life Sci. 1964;3:523-530.
12. Beckett AH, Casy AF. Synthetic analgesics: stereochemical considerations. J Pharm Pharmacol. 1954;6:986-1001.
13. Beckett AH, Casey AF, Harper NJ. Analgesics and their antagonists: some steric and chemical considerations. Part III The influence of the basic group on the biological response. J Pharm Pharmacol. 1956;8:874-883.
14. Costa E, Karczmar AG, Vessel ES. Bernard B. Brodie and the rise of chemical pharmacology. Ann Rev Pharmacol Toxicol. 1989;29:1-22.
15. Janssen PAJ. Haloperidol and the butyrophenones: the early years. In: Ban TA, Ray OS, eds. A history of the CINP. Brentwood TN: JM Productions; 1996. p. 440-450.
16. Janssen PAJ, Jageneau AH, Van Proosdij-Harzema EG, De Jongh DH. The pharmacology of a new potent analgesic, R951 2-(N-(4-carbethoxy-4-phenyl)- piperidino)-propiophenone HCl. Acta Physiol Pharmacol Neerland. 1958;7;373-402.
17. Granger B. La découverte de l'haloperidol. L'Encé phale. 1999;25:59-66.
18. Bett K, Janssen P. The decrease in the number of farmers led to less common sense. ECNP Matters. 2002; nr 2 January.
19. Granger B, Albu S. The haloperidol story. An Clin Psych. 2005;17:137-140.
20. Divry P, Bobon J, Collard J. Le 'R1625' nouvelle thérapeutique symptomatique de l'agitation psychomotrice. Acta Neurol Psychiatr Belg 1958;58:878-888.
21. Divry P, Bobon J, Lopez Ibor J, Pichot P, Ley RA, eds. Proceedings of the International Symposium on Haloperidol. Acta Med Belg. 1960;60:7, 21, 70, 108, 140, 145, 148.
22. Andreasen NC. Brave new brain. Conquering mental illness in the era of the genome. New York: Oxford Univ Press; 2001.
23. Janssen PAJ. Clinical significance and therapeutics of the neuroleptic syndrome. In: Divry P, Bobon J, Lopez Ibor J, Pichot P, R. Ley RA, eds. Proceedings of the International Symposium on Haloperidol. Acta Med Belg. 1960;60:149.
24. Seeman P, Lee T. Antipsychotic drugs: direct correlation between clinical potency and presynaptic action on dopamine neurons. Science. 1975;188:1217-1219.
25. Seeman P, Wong M, Lee T. Dopamine receptor-block and nigral fiber-impulse blockade by major tranquillizers. Fed Proc. 1974;33:246.
26. Snyder HHM. The dopamine hypothesis of schizophrenia: focus on the dopamine receptor. Am J Psych. 1976;133:197-202.
27. Creese I, Burt DR, Snyder SH. Dopamine receptor binding predicts clinical and pharmacological potencies of anti-schizophrenic drugs. Science. 1976;192:481-483.
28. Niemegeers CJE, Janssen PAJ, Minireview. A systematic study of the pharmacological activities of dopamine antagonists. Life Sci. 1979;24:2201-2216.
29. Janssen PAJ. The butyrophenone story In: Ayd FJ, Blackwell B, eds. Discoveries in biological psychiatry. Philadelphia PA: Lippincott; 1970.
30. Haase H-J, Janssen PAJ. The action of neuroleptic drugs. 2nd ed. Amsterdam: Elsevier; 1985.
31. 2 dopamine receptor occupancy during treatment with neuroleptic drugs. Psych Res: Neuroimag. 1999;90:31-39.
32. Janssen PAJ. The pharmacology of neuroleptanalgesia. Proceedings of dehydrobenzperidol - fentanyl. Moscow: Min Health USSR; 1967. p. 7-14.
33. Shale JH, Shale CM, Mastin WD. A review of the safety and efficacy of droperidol for the rapid sedation of severely agitated and violent patients. J Clin Psych. 2003;64:500-505.
34. De Castro J, Mundeleer P. Anesthesia without sleep: " neuroleptanalgesia". Acta Chir Belg. 1959;58:689-693.
35. Marsboom R, Symoens J. Azaperone (R1929) as a sedative for pigs. Neth J Vet Sci. 1968;1:124-131.
36. Leysen J, Laduron P. A serotonergic component of neuroleptic receptors. Arch Int Pharmacodyn Ther. 1977;230:337-339.
37. Sugerman AA. A pilot study of floropipamide (dipiperon). Dis Nerv Syst. 1964;25:355-358.
38. Schotte A, Janssen PFM, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, et al. Risperidone compared with new and reference antipsychotic drugs:in vitro and in vivo receptor binding. Psychopharmacol. 1996;124:57-73.
39. Janssen PAJ, Awouters FHL. Antipsychotic agents. In: Munson PL, Mueller RA, Breese GR, eds. Basic Concepts and Clinical Applications. New York: Chapman and Hall; 1995. p. 289-308.
40. Vranckx-Haenen J, De Munter W, Heykants J. Fluspirilene (IMAP) administered in a biweekly dose for the prevention of relapses in chronic schizophrenia. Acta Psych Belg. 1979;79:459-474.
41. Niemegeers CJE, Awouters F. Is there a biological basis for low dose application of some neuroleptics in anxiety? Proceedings of the VIII World Congress of Psychiatry. Athens;1989. p. 241-247.
42. Johnson DN, Funderburk WH, Ward JW. Neuropharmacology analysis of AHR-2277, a new psychotherapeutic agent. Arch Int Pharmacodyn. 1971;194:197-208.
43. 2-antagonists. Drug Dev Res. 1986;8:133-140.
44. 2 antagonist properties. J Pharmacol Exp Ther. 1988;244:685-693.
45. 2 neurotransmission as revealed by selective antagonism of hyper-reactivity to tryptamine and apomorphine. J Pharm Exp Therap.1990;254:945-951.
46. Megens AA, Kennis LE. Risperidone and related 5HT2/D2 antagonists: a new type of antipsychotic agent? Prog Med Chem. 1996;33:185-232.
47. 2-antagonist. Drug Dev Res. 1988;15:61-73.
48. Janssen P. Die Entwicklung neuartiger Antipsychotika - ein Schritt vorwärts in der Behandlung chronischer Psychosen. In: Bergener M, ed. Fortschritte in der Behandlung chronischer Psychosen. Erlangen: Perimed; 1988. p. 34-42.
49. Viola U, Brandenberger G, Toussaint M, Bouhours P, Macher J-P, Luthringer R. Ritanserin, a serotonin-2 receptor antagonist, improves ultradian sleep rhytmicity in young poor sleepers. Clin Neurophysiol. 2002;113:429-434.
50. Van Beijsterveldt LEC, Geerts RFJ, Leysen JE, Megens AA, Van den Eynde HM, Meuldermans WE. The regional brain distribution of risperidone and its active metabolite 9-hydroxy-risperidone in the rat. Psychopharmacol. 1994;114:53-62.
51. Leysen JE, Gommeren W, Eens A, de Chaffoy de Courcelles D, Stoof JC, Janssen PAJ. Biochemical profile of risperidone, a new antipsychotic. J Pharmacol Exp Ther.1988;247:661-670.
52. 2- receptors. In: Kane JMJM, Moeller H-J, Awouters F, eds. Serotonin in antipsychotic treatment. Mechanisms and clinical practice. New York: Marcel Dekker; 1996. p. 153-179.
53. Seeman P, Van Tol HHM. Dopamine receptor pharmacology. TiPS. 1994;15:264-269.
54. 2 receptors. Curr Drug Targets - CNS & Neurol Dis. 2004;3:11-26.
55. Leysen JE, Niemegeers CJE, Tollenaere JP, Laduron PM. Serotonergic component of neuroleptic receptors. Nature. 1978;272:168-171.
56. Meltzer HJ. Clinical studies on the mechanism of action of clozapine: the dopamine-serotonin hypothesis of schizophrenia. Psychopharmacol. 1989;99 Suppl: S18-S27.
57. Colpaert FC. Discovering risperidone: the LSD model of psychopathology. Nature Rev Drug Disc. 2003;2:315-320.
58. Snyder SH. Amphetamine psychosis: A "model' schizophrenia mediated by catecholamines. Am J Psych. 1973;130:61-67.
59. Freedman R, Olincy A, Ross RG, Waldo MC, Stevens KE, Adler LE, et al. The genetics of sensory gating deficits in schizophrenia. Curr Psych Rep. 2003;5:155-161.
60. Bleuler E. Dementia praecox oder Gruppe der Schizophrenien. In: Aschaffenburg G, ed. Handbuch der Psychiatrie. Leipzig: Franz Deuticke (neu verlegt); 1911.
61. Janssen PAJ, Awouters FHL. Introduction to internal inhibition. CINP In: Ban TA, Healy D, Shorter E,eds. Reflections on twentieth-century psychopharmacology. Budapest: Animula Publ House: 2004. p. 65-70.
62. Axmacher I, Bente D, Ferner U. Informationsstatistische Untersuchungen zur Struktur einfachen Handlungsfolgen bei endogenen Psychosen. Arzneimittel-Forschung (Drug Research). 1970;20:919-921.
63. Lewi PJ, Rogiers R, Janssen PAJ. Stereotypy Test Apparatus (STA), User Instruction Manual. Beerse: Janssen Pharmaceutica NV; 2001.
64. Hoffmann E, Servais L, Campanella S, Stillemans E, Lewi P, Janssen P. Use of the stereotypy test apparatus with juvenile offenders. Int. Congr. Schizophrenia Research, Colorado Springs, CO; March 29 - April 2, 2003.
65. Good KP, Wadhwa D, Choo S, Lewi P, Kopala LC, Janssen PAJ. An exploration of stereotypy and cognitive correlates in patients with first-episode psychosis. Int. Congr. Schizophrenia Research, Colorado Springs, CO; March 29 - April 2, 2003.
66. Shannon CE, A mathematical theory of communication. Bell Syst Techn J. 1948;27:379-423, 623-656.
67. Morrens M., Hustijn W, Lewi PJ, De Hert M, Sabbe BG, Stereotypy in Schizophrenia, Schizophr Res. 2006;84:397-404.