History of the discovery of the antipsychotic dopamine D2 receptor: A basis for the dopamine hypothesis of schizophrenia

Journal of the History of the Neurosciences

Volumn 22, Issue 1, 2013, Pages 62-78

  Madras, Bertha K ^a  

^a HARVARD MEDICAL SCHOOL   (United States)

Author keywords

antipsychotics; behavior; delusions; hallucinations; psychosis; schizophrenia; striatum

Indexed keywords

DOPAMINE 2 RECEPTOR; HALOPERIDOL; NEUROLEPTIC AGENT;

ARTICLE; DRUG DEVELOPMENT; HISTORY; HUMAN; NEUROBIOLOGY; SCHIZOPHRENIA;

ANTIPSYCHOTIC AGENTS; DRUG DISCOVERY; HALOPERIDOL; HISTORY, 20TH CENTURY; HUMANS; NEUROBIOLOGY; RECEPTORS, DOPAMINE D2; SCHIZOPHRENIA;

EID: 84872877090     PISSN: 0964704X     EISSN: 17445213     Source Type: Journal    
DOI: 10.1080/0964704X.2012.678199     Document Type: Article

References (57)

1. Agid O, Seeman P, Kapur S (2006): The "delayed onset" of antipsychotic action - An idea whosetime has come and gone. Journal of Psychiatry & Neuroscience 31: 93-100.
2. Andén N-E, Butcher SG, Corrodi H, Fuxe K, Ungerstedt U (1970): Receptor activity and turnover ofdopamine and noradrenaline after neuroleptics. European Journal of Pharmacology 11: 303-314.
3. Andén N-E, Roos B-E, Werdinius B (1964): Effects of chlorpromazine, haloperidol and reserpine onthe levels of phenolic acids in rabbit corpus striatum. Life Sciences 3: 149-158.
4. Baumeister AA, Francis JL (2002): Historical development of the dopamine hypothesis of schizophrenia. Journal of the History of the Neurosciences 11: 265-277. (Pubitemid 35415377)
5. Bloom FE, Costa E, Salmoiraghi GC (1965): Anesthesia and the responsiveness of individual neuronsof the caudate nucleus of the cat to acetylcholine, norepinephrine and dopamine administered by microelectrophoresis. Journal of Pharmacology and Experimental Therapeutics 150: 244-252.
6. Burt DR, Creese, I, Snyder SH (1976): Properties of [3H]haloperidol and [3H]dopamine bindingassociated with dopamine receptors in calf brain membranes. Molecular Pharmacology 12:800-812. (Pubitemid 8011598)
7. Carlsson A, Lindqvist M (1963): Effect of chlorpromazine or haloperidol on formation of 3- methoxytyramine and normetanephrine in mouse brain. Acta Pharmacologica et Toxicologica(Copenhagen) 20: 140-144.
8. Carlsson A, Lindqvist M, Magnusson T, Waldeck B (1958): On the presence of 3-hydroxytyraminein brain. Science 127: 471.
9. Clement-Cormier YC, Kebabian JW, Petzold GL, Greengard P (1974): Dopamine-sensitive adenylatecyclase in mammalian brain: A possible site of action of antipsychotic drugs. Proceedings of theNational Academy of Sciences, USA 71: 1113-1117.
10. Cools AR, Van Rossum JM (1976): Excitation-mediating and inhibition-mediating dopaminereceptors: A new concept towards a better understanding of electrophysiological, biochemical,pharmacological, functional and clinical data. Psychopharmacologia 45: 243-254.
11. Corripio I, Escartí MJ, Portella MJ, Pérez V, Grasa E, Sauras RB, Alonso A, Safont G, CamachoMV, Dueñas R, Arranz B, San L, Catafau AM, Carrió I, Alvarez E (2011): Density of striatal D2 receptors in untreated first-episode psychosis: An I(123)-IBZM SPECT study. EuropeanNeuropsychopharmacology 21: 861-866.
12. Curry SH (1970): Plasma protein binding of chlorpromazine. Journal of Pharmacy andPharmacology 22: 193-197.
13. Da Prada M, Pletscher A (1966): Acceleration of the cerebral dopamine turnover by chlorpromazine. Experientia 22: 465-466.
14. Delay J, Deniker P, Harl J-M (1952): Traitement des états d'excitation et d'agitation par une méthodemédicamenteuse dérivée de l'hibernithérapie [Therapeutic method derived from hiberno-therapyin excitation and agitation states]. Annales Medico-Psychologiques (Paris) 110: 267-273.
15. Ehringer H, Hornykiewicz O (1960): Distribution of noradrenaline and dopamine (3-hydroxytyramine) in the human brain and their behavior in diseases of the extrapyramidal system.Wiener Klinische Wochenschrift 38: 1236-1239.
16. Farde L, Wiesel FA, Halldin C, Sedvall G (1988): Central D2-dopamine receptor occupancy in schizophrenic patients treated with antipsychotic drugs. Archives of General Psychiatry 45: 71-76. (Pubitemid 18018572)
17. Forsman A, Öhman R (1977): Studies on serum protein binding of haloperidol. Current TherapeuticResearch, Clinical and Experimental 21: 245-255. (Pubitemid 8070835)
18. George SR, Watanabe M, Di Paolo T, Falardeau P, Labrie F, Seeman P (1985): The functional stateof the dopamine receptor in the anterior pituitary is in the high-affinity form. Endocrinology 117: 690-697. (Pubitemid 15237891)
19. Girgis RR, Phillips MR, Li X, Li K, Jiang H, Wu C, Duan N, Niu Y, Lieberman JA (2011): Clozapine v. chlorpromazine in treatment-naive, first-episode schizophrenia: 9-year outcomes of a randomised clinical trial. British Journal of Psychiatry 199: 281-288.
20. Graff-Guerrero A, Mizrahi R, Agid O, Marcon H, Barsoum P, Rusjan P, Wilson AA, Zipursky R, Kapur S (2009): The dopamine D2 receptors in high-affinity state and D3 receptors in schizophrenia: A clinical [11C]-(+)-PHNO PET study. Neuropsychopharmacology 34: 1078-1086.
21. Humber LG, Bruderlein FT, Philipp AH, Götz M (1979): Mapping the dopamine receptor. 1.Features derived from modifications in ring E of the neuroleptic butaclamol. Journal of MedicinalChemistry 22: 761-767. (Pubitemid 10234132)
22. Kapur S, Zipursky R, Jones C, Shammi CS, Remington, Seeman P (2000): A positron emissiontomography study of quetiapine in schizophrenia - A preliminary finding of an antipsychoticeffect with only transiently high dopamine D2 receptor occupancy. Archives of General Psychiatry57: 553-559. (Pubitemid 30349435)
23. Karobath M, Leitich H (1974): Antipsychotic drugs and dopamine-stimulated adenylate cyclase prepared from corpus striatum of rat brain. Proceedings of the National Academy of Sciences, USA 71: 2915-2918.
24. Kebabian JW, Calne DB (1979): Multiple receptors for dopamine. Nature 277: 93-96. (Pubitemid 9093798)
25. Kebabian JW, Petzold GL, Greengard P (1972): Dopamine-sensitive adenylate cyclase in caudate nucleus of rat brain, and its similarity to the "dopamine receptor." Proceedings of the NationalAcademy of Sciences, USA 69: 2145-2149.
26. Lacomme M, Laborit H, Le Lorier G, Pommier M (1952): [Obstetric analgesia potentiated by associated intravenous dolosal with RP 4560]. Bulletin de la Fédération des Sociétés de Gynécologie et Dóbstétrique de Langue Française 4: 558-562.
27. Lieberman JA, Kane JM, Alvir J (1987): Provocative tests with psychostimulant drugs in schizophrenia. Psychopharmacology (Berl) 91: 415-433. (Pubitemid 17038204)
28. Liu X, Van Natta K, Yeo H, Vilenski O, Weller PE, Worboys PD, Monshouwer M (2009): Unbound drug concentration in brain homogenate and cerebral spinal fluid at steady state as a surrogate for unbound concentration in brain interstitial fluid. Drug Metabolism and Disposition 37: 787-793.
29. Madras BK, Miller GM, Fischman AJ (2005): The dopamine transporter and attentiondeficit/ hyperactivity disorder. Biological Psychiatry 57: 1397-1409. (Pubitemid 40798561)
30. Montagu KA (1957): Catechol compounds in rat tissues and in brains of different animals. Nature180: 244-245.
31. Nordström AL, Farde L, Eriksson L, Halldin C (1995): No elevated D2 dopamine receptors in neuroleptic-naive schizophrenic patients revealed by positron emission tomography and [11C]Nmethylspiperone. Psychiatry Research 61: 67-83.
32. Seeman N, Seeman P, Watanabe M (2011): Psychosis: Discovery of the Antipsychotic Receptor. Japanese edition, Suginamiku, Tokyo 168, Seiwa Shoten Co., Ltd. Posted on Amazon Japan. Available by e-mail from ishizawa@seiwa-pb.co. jp
33. [English version: Seeman N, and Seeman P(2009): Psychosis: Discovery of the Antipsychotic Receptor. Toronto, SZ Publications. Available by e-mail from Philip.Seeman@utoronto.ca].
34. Seeman P (1966): Erythrocyte membrane stabilization by local anesthetics and tranquilizers. Biochemical Pharmacology 15: 1753-1766.
35. Seeman P (1972): The membrane actions of anesthetics and tranquilizers. Pharmacological Reviews 24: 583-655.
36. Seeman P (1987): Dopamine receptors and the dopamine hypothesis of schizophrenia. Synapse 1: 133-152. (Pubitemid 17119661)
37. Seeman P (1992): Dopamine receptor sequences: Therapeutic levels of neuroleptics occupy D2, clozapine occupies D4. Neuropsychopharmacology 7: 261-284.
38. Seeman P (2002): Atypical antipsychotics: Mechanism of action. Canadian Journal of Psychiatry 47: 27-38. (Pubitemid 34302921)
39. Seeman P (2012): Dopamine agonist radioligand binds to both D2High and D2Low receptors, explaining why alterations in D2High are not detected in human brain scans. Synapse 66: 88-93.
40. Seeman P, Bialy HS (1963): The surface activity of tranquilizers. Biochemical Pharmacology 12:1181-1191.
41. Seeman P, Chau-Wong M, Tedesco J, Wong K (1975): Brain receptors for antipsychotic drugs and dopamine: Direct binding assays. Proceedings of the National Academy of Sciences, USA 72: 4376-4380.
42. Seeman P, Lee T (1974): The dopamine-releasing actions of neuroleptics and ethanol. Journal Pharmacology Experimental Therapeutics 190: 131-140.
43. Seeman P, Lee T (1975): Antipsychotic drugs: Direct correlation between clinical potency and presynaptic action on dopamine neurons. Science 188: 1217-1219.
44. Seeman P, Lee T, Chau-Wong M, Wong K (1976): Antipsychotic drug doses andneuroleptic/dopamine receptors. Nature 261: 717-719.
45. Seeman P, Staiman A, Chau-Wong M (1974): The nerve impulse-blocking actions of tranquilizers,and the binding of neuroleptics to synaptosome membranes. Journal of Pharmacology andExperimental Therapeutics 190: 123-130.
46. Seeman P, Tallerico T (1999): Rapid release of antipsychotic drugs from dopamine D2 receptors:An explanation for low receptor occupancy and early clinical relapse upon drug withdrawal ofclozapine or quetiapine. American Journal of Psychiatry 156: 876-884. (Pubitemid 29260342)
47. Seeman P,Wong M, Tedesco J (1975): Tranquilizer receptors in rat striatum. Society for NeuroscienceAbstracts 1: 405.
48. Seeman P, Ulpian C, Wreggett KA, Wells J (1984): Dopamine receptor parameters detected by 3Hspiperonedepend on tissue concentration: Analysis and examples. Journal of Neurochemistry 43:221-235. (Pubitemid 14083338)
49. Seeman P, Weinshenker D, Quirion R, Srivastava LK, Bhardwaj SK, Grandy DK, Premont RT, Sotnikova TD, Boksa P, El-Ghundi M, O'dowd BF, George SR, Perreault ML, Männistö PT, Robinson S, Palmiter RD, Tallerico T (2005): Dopamine supersensitivity correlates with D2Highstates, implying many paths to psychosis. Proceedings of the National Academy of Sciences, USA 102: 3513-3518. (Pubitemid 40328076)
50. Skinbjerg M, Sibley DR, Javitch JA, Abi-Dargham A (2012): Imaging the high-affinity state of thedopamine D(2) receptor in vivo: Fact or fiction? Biochemical Pharmacology 83: 193-198.
51. Snyder SH, Creese I, Burt DR (1975): The brain's dopamine receptor: Labeling with [3H]dopamineand [3H]haloperidol. Psychopharmacology Communications 1: 663-673.
52. Spano PF, Govoni S, Trabucchi M (1978): Studies on the pharmacological properties of dopamine receptors in various areas of the central nervous system. Advances in BiochemicalPsychopharmacology 19: 155-165.
53. Szent-Györgyi A (1960): Introduction to a Submolecular Biology. New York, Academic Press.
54. Van Rossum JM(1966): The significance of dopamine-receptor blockade for the mechanism of actionof neuroleptic drugs. Archives Internationales de Pharmacodynamie et de Therapie 160: 92-94.
55. Van Rossum JM(1967): The significance of dopamine-receptor blockade for the action of neurolepticdrugs. In: Brill H, Cole JO, Deniker P, Hippius H, Bradley PB, eds., Neuro-Psycho-Pharmacology,Proceedings of the Fifth International Congress of the Collegium Internationale Neuro- Psychopharmacologicum, March 1966, Excerpta Medica Foundation, Amsterdam, pp. 321-329.
56. Wreggett KA, Seeman P (1984): Agonist high- and low-affinity states of the D2 dopamine receptorin calf brain: Partial conversion by guanine nucleotide. Molecular Pharmacology 25: 10-17. (Pubitemid 14223247)
57. Zingales IA (1971): A gas chromatographic method for the determination of haloperidol in human plasma. Journal of Chromatography 54: 15-24.