Dopamine D2 and D4 receptor ligands: Relation to antipsychotic action

European Journal of Pharmacology

Volumn 351, Issue 3, 1998, Pages 273-286

  Wilson, Julie M ^a,c   Sanyal, Suparna ^a,c   Van Tol, Hubert H M ^a,b,c  

^a CENTRE FOR ADDICTION AND MENTAL HEALTH   (Canada)

^b UNIVERSITY OF TORONTO   (Canada)

^c UNIVERSITY OF TORONTO   (Canada)

Author keywords

Antipsychotic; Clozapine; Dopamine D2 like receptor; Dopamine D4 receptor antagonist; Dopamine receptor; Extrapyramidal symptom; Neuroleptic loose; Schizophrenia

Indexed keywords

1,2,3,4,4A,5,10,10A OCTAHYDRO 6 HYDROXY 1 METHYL 3 [(2 PYRIDYLTHIO)METHYL]BENZO[G]QUINOLINE; 2 AMINO 4 (4 FLUOROPHENYL) 5 [1 [4 (4 FLUOROPHENYL) 4 OXOBUTYL] 3 PYRROLIDINYL]THIAZOLE; 3 [[4 (4 CHLOROPHENYL) 1 PIPERAZINYL]METHYL] 1H PYRROLO[2,3 B]PYRIDINE; 7 (4 FLUOROPHENOXYMETHYL) 2 (5 FLUORO 2 PYRIMIDINYL) 2,3,4,6,7,8,9,9A OCTAHYDROPYRIDO[1,2 A]PYRAZINE; APOMORPHINE; BENZAMIDE DERIVATIVE; BROMOCRIPTINE; CHLORPROMAZINE; DOPAMINE 2 RECEPTOR; DOPAMINE 2 RECEPTOR BLOCKING AGENT; DOPAMINE 4 RECEPTOR; DOPAMINE RECEPTOR BLOCKING AGENT; EMONAPRIDE; FLUPHENAZINE; HALOPERIDOL; LOXAPINE; MELPERONE; NEUROLEPTIC AGENT; NGD 0941; OLANZAPINE; PD 167021; PENTAZOCINE; QUETIAPINE; RACLOPRIDE; RECEPTOR SUBTYPE; REMOXIPRIDE; RO 616270; SONEPIPRAZOLE; SPIPERONE; SULPIRIDE; UNCLASSIFIED DRUG; DRD4 PROTEIN, HUMAN; LIGAND;

BINDING AFFINITY; DRUG ACTIVITY; DRUG RECEPTOR BINDING; HUMAN; NONHUMAN; PRIORITY JOURNAL; RECEPTOR OCCUPANCY; REVIEW; SCHIZOPHRENIA; ANIMAL; BRAIN; DRUG ANTAGONISM; METABOLISM;

ANIMALS; ANTIPSYCHOTIC AGENTS; BRAIN; DOPAMINE ANTAGONISTS; HUMANS; LIGANDS; RECEPTORS, DOPAMINE D2; RECEPTORS, DOPAMINE D4; SCHIZOPHRENIA;

EID: 0031595105     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(98)00312-4     Document Type: Review

References (123)

1. Amalric, M., Koob, G.F., 1993. Functionally selective neurochemical afferents and efferents of the mesocorticolimbic and nigrostriatal dopamine system. Prog. Brain Res. 99, 209-226.
2. Ariano, M.A., Wang, J., Noblett, K.L., Larson, E.R., Sibley, D.R., 1997. Cellular distribution of the rat D4 dopamine receptor protein in the CNS using anti-receptor antisera. Brain Res. 752, 26-34.
3. Arnt, J., Skarsfeldt, T., 1998. Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence. Neuropsychopharmacology 18, 63-101.
4. 4 receptor repeat: analysis of different native and mutant forms of the human and rat genes. Mol. Pharmacol. 46, 364-373.
5. 2 receptors. Nature 377, 424-428.
6. 2 receptors in vivo in rat brain. Implications for pet studies. J. Recept. Signal Transduction Res. 17, 419-431.
7. Brenner, H.D., Dencker, S.J., Goldstein, M.J., Hubbard, J.W., Keegan, D.L., Kruger, G., Kulhanek, F., Liberman, R.P., Malm, U., Midha, K.K., 1990. Defining treatment refractoriness in schizophrenia. Schizophr. Bull. 16, 551-561.
8. Bristow, L.J., Collinson, N., Cook, G.P., Curtis, N., Freedman, S.B., Kulagowski, J.J., Leeson, P.D., Patel, S., Ragan, C.I., Ridgill, M., Saywell, K.L., Tricklebank, M.D., 1997. L-745,870, a subtype selective dopamine D4 receptor antagonist, does not exhibit a neuroleptic-like profile in rodent behavioral tests. J. Pharmacol. Exp. Ther. 283, 1256-1263.
9. 2 dopamine receptor cDNA. Nature 336, 783-787.
10. Bymaster, F.P., Calligaro, D.O., Falcone, J.F., Marsh, R.D., Moore, N.A., Tye, N.C., Seeman, P., Wong, D.T., 1996. Radioreceptor binding profile of the atypical antipsychotic olanzapine. Neuropsychopharmacology 14, 87-96.
11. Cardno, A.G., Farmer, A.E., 1995. The case for or against heterogeneity in the etiology of schizophrenia. The genetic evidence. Schizophr. Res. 17, 153-159.
12. Casey, D.E., 1995. Motor and mental aspects of extrapyramidal syndromes. Int. Clin. Psychopharmacol. 10 (Suppl.), 105-114.
13. Corbin, A.E., Heffner, T.G., 1997. Effects of dopamine (DA) D4 antagonists on prepulse inhibition of acoustic startle and amphetamine-stimulated locomotion in rats. Soc. Neurosci. Abstr. 939.13.
14. Corbin, A.E., Pugsley, T.A., Akunne, H.C., Whetzel, S.Z., Zoski, K.T., Georgie, L.M., Nelson, C.B., Wright, J.L., Wise, L.D., Heffner, T.G., 1998. Pharmacological characterization of PD 152255, a novel dimeric benzimidazole dopamine D3 antagonist. Pharmacol. Biochem. Behav. 59, 487-493.
15. Creese, I., Burt, D.R., Snyder, S.H., 1976. Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science 192, 481-483.
16. Csernansky, J.G., Murphy, G.M., Faustman, W.O., 1991. Limbic/mesolimbic connections and the pathogenesis of schizophrenia. Biol. Psychiatry 30, 383-400.
17. 2 receptor: two molecular forms generated by alternative splicing. Embo J. 8, 4025-4034.
18. Davis, K.L., Kahn, R.S., Ko, G., Davidson, M., 1991. Dopamine in schizophrenia: a review and reconceptualization. Am. J. Psychiatry 148, 1474-1486.
19. Dearry, A., Gingrich, J.A., Falardeau, P., Fremeau, R.T. Jr., Bates, M.D., Caron, M.G., 1990. Molecular cloning and expression of the gene for a human D1 dopamine receptor. Nature 347, 72-76.
20. 3H](+)-pentazocine to sigma recognition sites in guinea pig brain. Eur. J. Pharmacol. 227, 371-378.
21. Deutch, A.Y., Moghaddam, B., Innis, R.B., Krystal, J.H., Aghajanian, G.K., Bunney, B.S., Charney, D.S., 1991. Mechanisms of action of atypical antipsychotic drugs. Implications for novel therapeutic strategies for schizophrenia. Schizophr. Res. 4, 121-156.
22. 11C]raclopride in man. Synapse 20, 200-208.
23. Farde, L., Nordstrom, A.L., 1993. PET examination of central D2 dopamine receptor occupancy in relation to extrapyramidal syndromes in patients being treated with neuroleptic drugs. Psychopharmacol. Ser. 10, 94-100.
24. Farde, L., Nordstrom, A.L., Nyberg, S., Halldin, C., Sedvall, G., 1994. D1-, D2-, and 5-HT2-receptor occupancy in clozapine-treated patients. J. Clin. Psychiatry 55 (B), 67-69.
25. Farde, L., Nordstrom, A.L., Wiesel, F.A., Pauli, S., Halldin, C., Sedvall, G., 1992. Positron emission tomographic analysis of central D1 and D2 dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine. Relation to extrapyramidal side effects. Arch. Gen. Psychiatry 49, 538-544.
26. 11C]raclopride. Arch. Gen. Psychiatry 47, 213-219.
27. Feinberg, A.P., Snyder, S.H., 1975. Phenothiazine drugs: structure-activity relationships explained by a conformation that mimics dopamine. Proc. Natl. Acad. Sci. USA 72, 1899-1903.
28. Feldpausch, D.L., Needham, L.M., Meng, Z.-H., Stone, M.P., Svensson, K.A., Merchant, K.M., 1996. Dopamine D4-selective antagonist, U-101387G, blocks amphetamine-sensitization in rats: behavioral and biochemical changes. Soc. Neurosci. Abstr. 697.14.
29. Garimella, B., Wu, H., Fitch, C.S., Essani, K., Merchant, K.M., 1997. Does the dopamine D4 receptor selective antagonis, PNU-101387G, block amphetamine sensitization by enhancing dynorphin neurotransmission? Soc. Neurosci. Abstr. 874.3.
30. Giros, B., Sokoloff, P., Martres, M.P., Riou, J.F., Emorine, L.J., Schwartz, J.C., 1989. Alternative splicing directs the expression of two D2 dopamine receptor isoforms. Nature 342, 923-926.
31. Grandy, D.K., Marchionni, M.A., Makam, H., Stofko, R.E., Alfano, M., Frothingham, L., Fischer, J.B., Burke-Howie, K.J., Bunzow, J.R., Server, A.C. et al., 1989. Cloning of the cDNA and gene for a human D2 dopamine receptor. Proc. Natl. Acad. Sci. U.S.A. 86, 9762-9766.
32. Grandy, D.K., Zhang, Y.A., Bouvier, C., Zhou, Q.Y., Johnson, R.A., Allen, L., Buck, K., Bunzow, J.R., Salon, J., Civelli, O., 1991. Multiple human D5 dopamine receptor genes: a functional receptor and two pseudogenes. Proc. Natl. Acad. Sci. U.S.A. 88, 9175-9179.
33. Gudelsky, G.A., Koenig, J.I., Simonovic, M., Koyama, T., Ohmori, T., Meltzer, H.Y., 1987. Differential effects of haloperidol, clozapine, and fluperlapine on tuberoinfundibular dopamine neurons and pro lactin secretion in the rat. J. Neural Transm. 68, 227-240.
34. Gurevich, E.V., Bordelon, Y., Shapiro, R.M., Arnold, S.E., Gur, R.E., Joyce, J.N., 1997. Mesolimbic dopamine D3 receptors and use of antipsychotics in patients with schizophrenia. A postmortem study. Arch. Gen. Psychiatry 54, 225-232.
35. Hartman, D.S., Smeyne, R., Zenner, M.-T., Goepfert, C., Schlaeger, E.-J., Jenck, F., Civelli, O., Godel, T., Riemer, C., 1996. RO 61-6270, a new highly selective dopamine D4 receptor antagonist, induces c-fos expression in mouse cortex. Soc. Neurosci. Abstr. 202.1.
36. 3H]-nemonapride binding sites in calf brain. Naunyn-Schmiedeberg's Arch. Pharmacol. 356, 17-21.
37. Hietala, J., Syvalahti, E., Vuorio, K., Nagren, K., Lehikoinen, P., Ruotsalainen, U., Rakkolainen, V., Lehtinen, V., Wegelius, U., 1994. Striatal D2 dopamine receptor characteristics in neuroleptic-naive schizophrenic patients studied with positron emission tomography. Arch. Gen. Psychiatry 51, 116-123.
38. Holland, J.P., Costello, D.G., de Wet, J.R., Rollema, H., Sanner, M.A., Zorn, S.G., Seeger, T.F., 1996. CP-293,029: a D4-selective dopamine antagonist produces clozapine-like effects on c-fos mRNA and dopamine levels in rat brain. Soc. Neurosci. Abstr. 697.2.
39. Joyce, J.N., Meador-Woodruff, J.H., 1997. Linking the family of D2 receptors to neuronal circuits in human brain: insights into schizophrenia. Neuropsychopharmacology 16, 375-384.
40. Kalkman, H.O., Neumann, V., Tricklebank, M.D., 1997. Clozapine inhibits catalepsy induced by olanzapine and loxapine, but prolongs catalepsy induced by SCH 23390 in rats. Naunyn-Schmiedeberg's Arch. Pharmacol. 355, 361-364.
41. Kane, J., Honigfeld, G., Singer, J., Meltzer, H., 1988a. Clozapine for the treatment-resistant schizophrenic. A double-blind comparison with chlorpromazine. Arch. Gen. Psychiatry 45, 789-796.
42. Kane, J.M., Freeman, H.L., 1994. Towards more effective antipsychotic treatment. Br. J. Psychiatry 25 (Suppl.), 22-31.
43. Kane, J.M., Honigfeld, G., Singer, J., Meltzer, H., 1988b. Clozapine in treatment-resistant schizophrenics. Psychopharmacol. Bull. 24, 62-67.
44. Kane, J.M., Lieberman, J.A., 1987. Maintenance pharmacotherapy in schizophrenia. In: Meltzer, H.Y. (Ed.), Psychopharmacology: The Third Generation of Progress. Raven Press, New York, pp. 1103-1109.
45. 18F]methylspiperone demonstrates D2 dopamine receptor binding differences of clozapine and haloperidol. J. Neural Transm. Gen. Sect. 86, 163-173.
46. Kelly, M.A., Rubinstein, M., Asa, S.L., Zhang, G., Saez, C., Bunzow, J.R., Allen, R.G., Hnasko, R., Ben-Jonathan, N., Grandy, D.K., Low, M.J., 1997. Pituitary lactotroph hyperplasia and chronic hyperprolactinemia in dopamine D2 receptor-deficient mice. Neuron 19, 103-113.
47. Kramer, M.S., Last, B., Getson, A., Reines, S.A., 1997. The effects of a selective D4 dopamine receptor antagonist (L-745,870) in acutely psychotic inpatients with schizophrenia: D4 Dopamine Antagonist Group. Arch. Gen. Psychiatry 54, 567-572.
48. Lahti, R.A., Roberts, R.C., Conley, R.R., Cochrane, E.V., Mutin, A., Tamminga, C.A., 1996. D2-type dopamine receptors in postmortem human brain sections from normal and schizophrenic subjects. Neuroreport 7, 1945-1948.
49. Levant, B., Vansell, N.R., 1997. In vivo occupancy of D2 dopamine receptors by nafadotride. Neuropsychopharmacology 17, 67-71.
50. Lieberman, J.A., Kane, J.M., Alvir, J., 1987. Provocative tests with psychostimulant drugs in schizophrenia. Psychopharmacology (Berlin) 91, 415-433.
51. Majchrzak, M.J., Zorn, S.H., Sanner, M.A., Seymour, P.A., 1997. Blockade of the locomotor activity response to apomorphine: a proposed in vivo behavioral assay to detect dopamine D4 receptor antagonists. Soc. Neurosci. Abstr. 165.8.
52. Mansbach, R.S., Brooks, E.W., Sanner, M.A., Zorn, S.H., 1998. Selective dopamine D4 receptor antagonists reverse apomorphine-induced blockade of prepulse inhibition. Psychopharmacology (Berlin) 135 2, 194-200.
53. Mansour, A., Meador-Woodruff, J.H., Bunzow, J.R., Civelli, O., Akil, H., Watson, S.J., 1990. Localization of dopamine D2 receptor mRNA and D1 and D2 receptor binding in the rat brain and pituitary: an in situ hybridization- receptor autoradiographic analysis. J. Neurosci. 10, 2587-2600.
54. Markstein, R., Gull, P., Rudeberg, C., Urwyler, S., Jalon, A.L., Kalkman, H.O., Dixon, A.K., Hoyer, D., 1996. SDZ GLC 756, a novel octahydrobenzo[g]quinoline derivative exerts opposing effects on dopamine Dl and D2 receptors. J. Neural Transm. 103, 17-30.
55. 3H]raclopride is increased in schizophrenia. Biol. Psychiatry 42, 648-654.
56. Meador-Woodruff, J.H., Mansour, A., Bunzow, J.R., Van Tol, H.H.M., Watson, S.J. Jr., Civelli, O., 1989. Distribution of D2 dopamine receptor mRNA in rat brain. Proc. Natl. Acad. Sci. U.S.A. 86, 7625-7628.
57. Meador-Woodruff, J.H., Haroutunian, V., Powchik, P., Davidson, M., Davis, K.L., Watson, S.J., 1997. Dopamine receptor transcript expression in striatum and prefrontal and occipital cortex. Focal abnormalities in orbitofrontal cortex in schizophrenia. Arch. Gen. Psychiatry 54, 1089-1095.
58. Meltzer, H.Y., Gudelsky, G.A., 1992. Dopaminergic and serotonergic effects of clozapine. Implications for a unique clinical profile. Arzneimittelforschung 42, 268-272.
59. Meltzer, H.Y., Koenig, J.I., Nash, J.F., Gudelsky, G.A., 1989. Melperone and clozapine: neuroendocrine effects of atypical neuroleptic drugs. Acta Psychiatr. Scand. 352, 24-29.
60. Mengod, G., Martinez-Mir, M.I., Vilaro, M.T., Palacios, J.M., 1989. Localization of the mRNA for the dopamine D2 receptor in the rat brain by in situ hybridization histochemistry. Proc. Natl. Acad. Sci. USA 86, 8560-8564.
61. Merchant, K.M., Gill, G.S., Harris, D.W., Huff, R.M., Eaton, M.J., Lookingland, K., Lutzke, B.S., McCall, R.B., Piercey, M.F., Schreur, P.J., Sethy, V.H., Smith, M.W., Svensson, K.A., Tang, A.H., Vonvoigtlander, P.F., Tenbrink, R.E., 1996. Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist. J. Pharmacol. Exp. Ther. 279, 1392-1403.
62. Millan, M.J., Gressier, H., Brocco, M., 1997. The dopamine D3 receptor antagonist, (+)-S 14297, blocks the cataleptic properties of haloperidol in rats. Eur. J. Pharmacol. 321, R7-9.
63. Mogenson, G.J., Yang, C.R., Yim, C.Y., 1988. Influence of dopamine on limbic inputs to the nucleus accumbens. Ann. New York Acad Sci. 537, 86-100.
64. Monsma, Jr., F.J., Mahan, L.C., McVittie, L.D., Gerfen, C.R., Sibley, D.R., 1990. Molecular cloning and expression of a D1 dopamine receptor linked to adenylyl cyclase activation. Proc. Natl. Acad. Sci. USA 87, 6723-6727.
65. Monsma, Jr., F.J., McVittie, L.D., Gerfen, C.R., Mahan, L.C., Sibley, D.R., 1989. Multiple D2 dopamine receptors produced by alternative RNA splicing. Nature 342, 926-929.
66. Mrzljak, L., Bergson, C., Pappy, M., Huff, R., Levenson, R., Goldman-Rakic, P.S., 1996. Localization of dopamine D4 receptors in GABAergic neurons of the primate brain. Nature 381, 245-248.
67. Murray, A.M., Hyde, T.M., Knable, M.B., Herman, M.M., Bigelow, L.B., Carter, J.M., Weinberger, D.R., Kleinman, J.E., 1995. Distribution of putative D4 dopamine receptors in postmortem striatum from patients with schizophrenia. J. Neurosci. 15, 2186-2191.
68. Najlerahim, A., Barton, A.J., Harrison, P.J., Heffernan, J., Pearson, R.C. 9.Me, 1989. Messenger RNA encoding the D2 dopaminergic receptor detected by in situ hybridization histochemistry in rat brain. FEBS Lett. 255, 335-339.
69. Nordin, C., Aime, B., Bondesson, U., 1995. CSF and serum concentrations of clozapine and its demethyl metabolite: a pilot study. Psychopharmacology (Berlin) 122, 104-107.
70. 11C]N- methylspiperone. Psychiatry Res. 61, 67-83.
71. 2A receptor and alpha-1 adrenoceptor antagonist (R)-(+)-2-amino-4-(4-fluorophenyl)-5-[1-[4-(4-fluorophenyl)-4-oxopyrrolidin-3- yl]thiazole(NRA0045). J. Pharmacol. Exp. Ther. 282, 56-63.
72. Okuyama, S., Chaki, S., Kawashima, N., Suzuki, Y., Ogawa, S., Kumagai, T., Nakazato, A., Nagamine, M., Yamaguchi, K., Tomisawa, K., 1997b. The atypical antipsychotic profile of NRA0045, a novel dopamine D4 and 5-hydroxytryptamine2A receptor antagonist, in rats. Br. J. Pharmacol. 121, 515-525.
73. Patel, S., Freedman, S., Chapman, K.L., Emms, F., Fletcher, A.E., Knowles, M., Marwood, R., McAllister, G., Myers, J., Curtis, N., Kulagowski, J.J., Leeson, P.D., Ridgill, M., Graham, M., Matheson, S., Rathbone, D., Watt, A.P., Bristow, L.J., Rupniak, N.M., Baskin, E., Lynch, J.J., Ragan, C.I., 1997. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J. Pharmacol. Exp. Ther. 283, 636-647.
74. Pearlson, G.D., Wong, D.F., Tune, L.E., Ross, C.A., Chase, G.A., Links, J.M., Dannals, R.F., Wilson, A.A., Ravert, H.T., Wagner, H.N. Jr. et al., 1995. In vivo D2 dopamine receptor density in psychotic and nonpsychotic patients with bipolar disorder. Arch. Gen. Psychiatry 52, 471-477.
75. Pilowsky, L.S., Costa, D.C., Ell, P.J., Murray, R.M., Verhoeff, N.P., Kerwin, R.W., 1992. Clozapine, single photon emission tomography, and the D2 dopamine receptor blockade hypothesis of schizophrenia. Lancet 340, 199-202.
76. 3H]NGD 94-1. J. Pharmacol. Exp. Ther. 282, 1020-1027.
77. Raleigh, F., 1996. Use of novel antipsychotic drugs. Pharmacotherapy 16, 160S-165S, discussion 166S-168S.
78. Randrup, A., Munkvad, I., 1965. Special antagonism of amphetamine-induced abnormal behaviour: inhibition of stereotyped activity with increase of some normal activities. Psychopharmacologia 7, 416-422.
79. Rao, P.A., Pickar, D., Gejman, P.V., Ram, A., Gershon, E.S., Gelernter, J., 1994. Allelic variation in the D4 dopamine receptor (DRD4) gene does not predict response to clozapine. Arch. Gen. Psychiatry 51, 912-917.
80. Robertson, G.S., Fibiger, H.C., 1992. Neuroleptics increase c-fos expression in the forebrain: contrasting effects of haloperidol and clozapine. Neuroscience 46, 315-328.
81. Roth, B.L., Craigo, S.C., Choudhary, M.S., Uluer, A., Monsma, F.J. Jr., Shen, Y., Meltzer, H.Y., Sibley, D.R., 1994. Binding of typical and atypical antipsychotic agents to 5- hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J. Pharmacol. Exp. Ther. 268, 1403-1410.
82. Rubinstein, M., Phillips, T.J., Bunzow, J.R., Falzone, T.L., Dziewczapolski, G., Zhang, G., Fang, Y., Larson, J.L., McDougall, J.A., Chester, J.A. Chest, Saez, C., Pugsley, T.A., Gershanik, O., Low, M.J., Grandy, D.K., 1997. Mice lacking dopamine D4 receptors are supersensitive to ethanol, cocaine, and methamphetamine. Cell 90, 991-1001.
83. Sautel, F., Griffon, N., Sokoloff, P., Schwartz, J.C., Launay, C., Simon, P., Costentin, J., Schoenfelder, A., Garrido, F., Mann, A. etal et al., 1995. Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents. J. Pharmacol. Exp. Ther. 275, 1239-1246.
84. Schoots, O., Seeman, P., Guan, H.C., Paterson, A.D., Van Tol, H.H.M., 1995. Long-term haloperidol elevates dopamine D4 receptors by 2-fold in rats. Eur. J. Pharmacol. 289, 67-72.
85. Seeman, P., 1987. Dopamine receptors and the dopamine hypothesis of schizophrenia. Synapse 1, 133-152.
86. Seeman, P., 1992. Dopamine receptor sequences. Therapeutic levels of neuroleptics occupy D2 receptors, clozapine occupies D4. Neuropsychopharmacology 7, 261-284.
87. Seeman, P., 1995. Therapeutic receptor-blocking concentrations of neuroleptics. Int. Clin. Psychopharmacol. 10 (Suppl.), 5-13.
88. Seeman, P., Bzowej, N.H., Guan, H.C., Bergeron, C., Reynolds, G.P., Bird, E.D., Riederer, P., Jellinger, K., Tourtellotte, W.W., 1987. Human brain D1 and D2 dopamine receptors in schizophrenia: Alzheimer's, Parkinson's, and Huntington's diseases. Neuropsychopharmacology 1, 5-15.
89. Seeman, P., Corbett, R., Nam, D., Van Tol, H.H.M., 1996. Dopamine and serotonin receptors: amino acid sequences, and clinical role in neuroleptic parkinsonism. Jpn. J. Pharmacol. 71, 187-204.
90. Seeman, P., Corbett, R., Van Tol, H.H.M., 1997a. Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors. Neuropsychopharmacology 16, 93-110, discussion 111-135.
91. 3H]benzquinoline. Synapse 25, 137-146.
92. Seeman, P., Guan, H.C., Van Tol, H.H.M., 1993. Dopamine D4 receptors elevated in schizophrenia. Nature 365, 441-445.
93. Seeman, P., Lee, T., 1975. Antipsychotic drugs: direct correlation between clinical potency and presynaptic action on dopamine neurons. Science 188, 1217-1219.
94. Seeman, P., Lee, T., Chau-Wong, M., Wong, K., 1976. Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature 261, 717-719.
95. Seeman, P., Tallerico, T., 1998. Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors. Mol. Psychiatry in press.
96. Seeman, P., Tallerico, T., Corbett, R., Van Tol, H.H.M., Kamboj, R.K., 1997c. Role of dopamine D2, D4 and serotonin(2A) receptors in antipsychotic and anticataleptic action. J. Psychopharmacol. 11, 15-17.
97. Seeman, P., Van Tol, H.H.M., 1995. Deriving the therapeutic concentrations for clozapine and haloperidol: the apparent dissociation constant of a neuroleptic at the dopamine D2 or D4 receptor varies with the affinity of the competing radioligand. Eur. J. Pharmacol. 291, 59-66.
98. Shaikh, S., Collier, D., Kerwin, R.W., Pilowsky, L.S., Gill, M., Xu, W.M., Thornton, A., 1993. Dopamine D4 receptor subtypes and response to clozapine. Lancet 341, 116.
99. Snyder, S.H., 1973. Amphetamine psychosis: a model schizophrenia mediated by catecholamines. Am. J. Psychiatry 130, 61-67.
100. Sokoloff, P., Giros, B., Martres, M.P., Bouthenet, M.L., Schwartz, J.C., 1990. Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature 347, 146-151.
101. Stefanis, N.C., Bresnick, J.N., Kerwin, R.W., Schofield, W.N., McAllister, G., 1998. Elevation of D4 dopamine receptor mRNA in postmortem schizophrenic brain. Brain Res. Mol. Brain Res. 53, 112-119.
102. Stone, M.P., Waters, N., Green, J.B., Myers, J.E., Lewis, R.A., Cimini, M.G., Svensson, K.A., 1996. Effects of the selective dopamine D4 antagonist U-101387G on locomotor activity and brain monoamine neurochemistry in the rat. Soci. Neurosci. Abstr. 697.17.
103. 3H]raclopride binding in postmortem caudate nucleus of subjects with schizophrenia or major depression. Brain Res. 681, 109-116.
104. Sunahara, R.K., Guan, H.C., BF, O.D., Seeman, P., Laurier, L.G., Ng, G., George, S.R., Torchia, J., Van Tol, H.H.M., Niznik, H.B., 1991. Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than Dl. Nature 350, 614-619.
105. Sunahara, R.K., Niznik, H.B., Weiner, D.M., Stormann, T.M., Brann, M.R., Kennedy, J.L., Gelernter, J.E., Rozmahel, R., Yang, Y.L., Israel, Y. et al., 1990. Human dopamine D1 receptor encoded by an intronless gene on chromosome 5. Nature 347, 80-83.
106. Tallman, J.F., Primus, R.J., Brodbeck, R., Cornfield, L., Meade, R., Woodruff, K., Ross, P., Thurkauf, A., Gallager, D.W., 1997. INGD 94-1: Identification of a novel, high affinity antagonist at the human dopamine D4 receptor. J. Pharmacol. Exp. Ther. 282, 1011-1019.
107. 3H]haloperidol binding in guinea pig brain membranes. Proc. Natl. Acad. Sci. USA 81, 5618-5621.
108. Tamminga, C.A., Gerlach, J., 1987, New Neuroleptics and experimental antipsychotics in schizophrenia. In: Meltzer, H.Y. (Ed.), Psychopharmacology: The Third Generation of Progress. Raven Press, New York.
109. Tarazi, F.I., Kula, N.S., Baldessarini, R.J., 1997a. Regional distribution of dopamine D4 receptors in rat forebrain. Neuroreport 8, 3423-3426.
110. Tarazi, F.I., Yeghiayan, S.K., Baldessarini, R.J., Kula, N.S., Neumeyer, J.L., 1997b. Long-term effects of S(+)N-n-propylnorapomorphine compared with typical and atypical antipsychotics: differential increases of cerebrocortical D2-like and striatolimbic D4-like dopamine receptors. Neuropsychopharmacology 17, 186-196.
111. Tiberi, M., Jarvie, K.R., Silvia, C., Falardeau, P., Gingrich, J.A., Godinot, N., Bertrand, L., Yang-Feng, T.L., Fremeau, R.T. Jr., Caron, M.G., 1991. Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor. Proc. Natl. Acad. Sci. USA 88, 7491-7495.
112. Tsuang, M.T., Farrone, S.V., 1995. The case for heterogeneity in the etiology of schizophrenia. Schizophr. Res. 17, 161-175.
113. Tune, L., Barta, P., Wong, D., Powers, R.E., Pearlson, G., Tien, A.Y., Wagner, H.N., 1996. Striatal dopamine D2 receptor quantification and superior temporal gyrus: volume determination in 14 chronic schizophrenic subjects. Psychiatry Res. 67, 155-158.
114. 11CN-methylspiperone. Psychiatry Res. 49, 219-237.
115. Van Tol, H.H.M., Bunzow, J.R., Guan, H.C., Sunahara, R.K., Seeman, P., Niznik, H.B., Civelli, O., 1991. Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. Nature 350, 610-614.
116. Von Bahr, C., Wiesel, F.A., Movin, G., Eneroth, P., Jansson, P., Nilsson, L., Ogenstad, S., 1991. Neuroendocrine responses to single oral doses of remoxipride and sulpiride in healthy female and male volunteers. Psychopharmacology (Berlin) 103, 443-448.
117. Weiner, D.M., Brann, M.R., 1989. The distribution of a dopamine D2 receptor mRNA in rat brain. FEBS Lett. 253, 207-213.
118. Wong, D.F., Wagner, H.N. Jr., Tune, L.E., Dannals, R.F., Pearlson, G.D., Links, J.M., Tamminga, C.A., Broussolle, E.P., Ravert, H.T., Wilson, A.A. et al., 1986. Positron emission tomography reveals elevated D2 dopamine receptors in drug-naive schizophrenics. Science 234, 1558-1563.
119. Wong, W.F., Pearlson, G.D. D.T, Tune, L.E., Young, L.T., Meltzer, C.C., Dannals, R.F., Ravert, H.T., Reith, J., Kuhar, M.J., Gjedde, A., 1997. Quantification of neuroreceptors in the living human brain: IV. Effect of aging and elevations of D2-like receptors in schizophrenia and bipolar illness. J. Cereb. Blood Flow Metab. 17, 331-342.
120. Wright, J.L., Gregory, T.F., Heffner, T.G., MacKenzie, R.G., Pugsley, T.A., Bander Meulen, S.J., Wise, L.D., 1996. A Novel series of 1-aryloxy-3(4-aryloxypiperidinyl)-2-propanols and potent, selective dopamine D4 receptor antagonists. Soc. Neurosci. Abstr. 189.14.
121. Youngren, K.D., Jentsch, J.D., Tran, A., Roth, R.H., 1997. Dopamine D4 receptors regulate dopamine synthesis without affecting utilization of release. Soc. Neurosci. Abstr. 271.7.
122. Zhou, Q.Y., Grandy, D.K., Thambi, L., Kushner, J.A., Van Tol, H.H.M., Cone, R., Pribnow, D., Salon, J., Bunzow, J.R., Civelli, O., 1990. Cloning and expression of human and rat D1 dopamine receptors. Nature 347, 76-80.
123. Zorn, S.H., Johnson, C.G., Jackson, E.R., Seymour, P., Majchrzak, M., Mansbach, R., Winson, E., de Wet, J.R., Dunaiskis, A., Chappie, T.A., Sanner, M.A., 1996. CP-293,029: A D4 dopamine antagonist with an in vitro and in vivo profile suggestive of an atypical antipsychotic. Soc. Neurosci. Abstr. 697.1.