D4/5-HT(2A) receptor antagonists: LU-111995 and other potential new antipsychotics in development

Drugs of the Future

Volumn 23, Issue 2, 1998, Pages 191-204

  Steiner, Gerd ^a   Bach, Alfred ^a   Bialojan, Siegfried ^a   Greger, Gerd ^a   Hege, Hans Günter ^a   Höger, Thomas ^a   Jochims, Karin ^a   Munschauer, Rainer ^a   Neumann, Barbara ^a   Teschendorf, Hans Jürgen ^a   Traut, Martin ^a   Unger, Liliane ^a   Gross, Gerhard ^a  

^a NONE

Author keywords

[No Author keywords available]

Indexed keywords

BELAPERIDONE; DOPAMINE 4 RECEPTOR; DOPAMINE RECEPTOR BLOCKING AGENT; NEUROLEPTIC AGENT; SEROTONIN 2A ANTAGONIST; UNCLASSIFIED DRUG;

DRUG METABOLISM; DRUG RECEPTOR BINDING; NONHUMAN; REVIEW; SCHIZOPHRENIA; STRUCTURE ACTIVITY RELATION;

EID: 0031896751     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.1998.023.02.485880     Document Type: Review

References (107)

1. Reynolds, G.P. Developments in the drug treatment of schizophrenia. Trends Pharmacol Sci 1992, 13: 116-21.
2. Davis, K.L., Kahn, R.S., Ko, G., Davidson, M. Dopamine in schizophrenia: A review and reconceptualization. Am J Psychiatry 1991, 148: 1474-86.
3. Seeman, P. Dopamine receptors and the dopamine hypothesis of schizophrenia. Synapse 1987, 1: 133-52.
4. Creese, I., Burt, D.R., Snyder, S.H. Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science 1976, 192: 481-3.
5. Kane, J., Honigfeld, G., Singer, J., Meltzer, H.Y. Clozapine for the treatment-resistant schizophrenic: A double-blind comparison with chlorpromazine. Arch Gen Psychiatry 1988, 45: 789-96.
6. Meltzer, H.Y. The importance of serotonin-dopamine interactions in the action of clozapine. Br J Psychiatry 1992, 160 (Suppl. 17): 22-9.
7. Meltzer, H.Y. Clinical studies on the mechanism of action of clozapine: The dopamine-serotonin hypothesis of schizophrenia. Psychopharmacology 1989, 99: 18-27.
8. Baldessarini, R.J., Huston-Lyons, D., Cambell, A., Marsh, E., Cohen, B.M. Do central antiadrenergic actions contribute to the atypical properties of clozapine? Br J Psychiatry 1992, 160: 12-6.
9. Monsma, F.J., Shen, Y., Ward, R.P. et al. Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol 1993, 43: 320-7.
10. Roth, B.L., Craigo, S.C., Choudhary, M.S. et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther 1994, 268: 1403-10.
11. 3) as a target for neuroleptics. Nature 1990, 347: 146-51.
12. Wustrow, D.J., Wise, L.D. Progress in developing dopamine D3 ligands as potential antipsychotic agents. Curr Pharm Design 1997, 3: 391-404.
13. 4 receptor with high affinity for the antipsychotic clozapine. Nature 19991, 350: 610-4.
14. 4 receptors in schizophrenia and antipsychotic action. J Psychiat Res 1997, 31: 219-32.
15. 4 receptors. Potential therapeutic implications in the treatment of schizophrenia. CNS Drugs 1997, 8: 1-11.
16. 4 receptor antagonists. Curr Pharm Design 1997, 3: 355-66.
17. 4. Neuropsychopharmacology 1992, 7: 261-84.
18. Goldman-Rakic, P.S., Bergson, C., Mrzljak, L., Williams, G.V. Dopamine receptors and cognitive function in nonhuman primates. In: The Dopamine Receptors. Neve, K.A., Neve, R.L. (Eds.). Humana Press: Totowa, NJ 1977, 499-522.
19. 4 receptor. Mol Brain Res 1995, 29: 157-62.
20. Tamminga, C.A., Thaker, G.K., Buchanan, R. et al. Limbic systems abnormalities identified in schizophrenia using positron emission tomography with fluorodeoxyglucose and neocortical alteration with deficit syndrome. Arch Gen Psychiatry 1992, 49: 522-30.
21. 3H]NGD94-1. J Pharmacol Exp Ther 1997, 282: 1020-7.
22. 4 receptors elevated in schizophrenia. Nature 1993, 365: 441-5.
23. 125l]-epidepride. Eur J Pharmacol 1995, 286: R3-5.
24. 4 receptors increased in schizophrenia? J Neurochem 1994, 63: 1576-7.
25. 4 sites in schizophrenic brains. Eur J Pharmacol 1996, 314: R3-5.
26. 4 dopamine receptors in postmortem striatum from patients with schizophrenia. J Neurosci 1995, 15: 2186-91.
27. 3H]nemonapride. J Neurochem 1995, 64: 1413-5.
28. i values. J Pharmacol Exp Ther 1989, 251: 238-46.
29. Stockmeier, C.A., DiCarlo, J.J., Zhang, Y., Thompson, P., Meltzer, H.Y. Characterization of typical and atypical antipsychotic drugs based on in vivo occupancy of serotonin-2 and dopamine-2 receptors. J Pharmacol Exp Ther 1993, 266: 1374-84.
30. 4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs. Psychopharmacology 1995, 120: 365-8.
31. Schotte, A., Janssen, P.F.M, Gomeren, W. et al. Risperidone compared with new and reference antipsychotic drugs: In vitro and in vivo receptor binding. Psychopharmacology 1996, 124: 57-73.
32. 2 receptor subtypes. J Psychiatry Neurosci 1996, 21: 29-35.
33. Bymaster, P.P., Calligaro, D.O., Falcone, J.F. et al. Radioreceptor binding profile of the atypical antipsychotic olanzapine. Neuropsychopharmacology 1996, 14: 87-96.
34. Seeger, T.F., Seymour, P.A., Schmidt, A.W. et al. Ziprasidone (CP-88059): A new antipsychotic with combined dopamine and serotonin receptor antagonist activity. J Pharmacol Exp Ther 1995. 275: 101-13.
35. 4 receptors. Neuropsychopharmacology 1997, 16: 93-110.
36. 2-dopamine receptor occupancy during treatment with conventional atypical neuroleptics. Psychopharmacology 1989, 99: 28-31.
37. Friedman, J.H., Lannon, M.C. Clozapine in the treatment of psychosis in Parkinson's desease. Neurology 1989, 39: 1219-21.
38. Kulagowski, J.J., Broughton, H.B., Curtis, N.R. et al. 3-[[4-(4-Chlorophenyl)piperazin-1 -yl]methyl]-1H-pyrrolo[2,3-b]pyridine: An antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem 1996, 39: 1941-2.
39. 4 receptor antagonist. Trends Pharmacol Sci 1997, 18: 186-8.
40. 4 dopamine receptor antagonist (L-745870) in acutely psychotic patients with schizophrenia. Arch Gen Psychiatry 1997, 54:567-72.
41. 4 receptors. J Med Chem 1996, 39: 1943-5.
42. 4 receptor. J Med Chem 1997, 40: 2374-85.
43. 4 antagonists. 213th ACS Nat Meeting (April 13-17, San Francisco) 1997, MEDI 162.
44. 4 receptor. Bioorg & Med Chem Lett 1997, 7: 2211-2216.
45. 4 receptors. J Med Chem 1997, 40: 1-3.
46. R&D Focus, Drug Updates, 26 May 1997, IMS World Publications.
47. 4 ligands: 3-([4-Arylpiperazin-1-yl]alkylamino)-2H-1,4-benzoxazines. Bioorg & Med Chem Lett 1997, 7: 2399-402.
48. 4 antagonist. J Med Chem 1996, 39: 2435-7.
49. 4 receptor. 213th ACS Natl Meet (April 13-17, San Francisco) 1997, MEDI 163.
50. 4 receptor. Eur J Pharmacol 1997, 322: 283-6.
51. 4 receptor antagonist CP-293,019. 213th ACS Natl Meet (April 13-17, San Francisco) 1997, MEDI 161.
52. 4 receptor. 213th ACS Natl Meet (April 13-17, San Francisco) 1997, MEDI 160.
53. Wright, J.L., Gregory, T.F., Heffner, T.G. et ai. Discovery of selective dopamine D4 receptor antagonists: 1-Aryloxy-3-(4-aryloxypiperidinyl)-2-propanols. Bioorg & Med Chem Lett 1997, 7: 1377-80.
54. 4 receptor antagonists as potential antipsychotic agents. J Med Chem 1997, 40: 2688-93.
55. 4 antagonists. J Med Chem 1996, 39: 1946-8.
56. 4 receptors. Bioorg & Med Chem Lett 1996, 6: 1227-32.
57. 4 antagonists: Synthesis and structure-activity relationships of (R)-5-chloro-4-cyclopropylcarbonylamino-2-methoxy-N-[1-(3-methoxy-benzyl)-3- pyrrolidinyl]benzamide (YM-50001) and related compounds. AIMECS 97 (July 27-Aug 1, Seoul) 1997, Abst PA-21.
58. Prous Science Trilogy Database.
59. 4 receptor. Bioorg & Med Chem Lett 1997, 7: 1327-30.
60. Schmidt, C.J., Sorensen, S.M., Kehne, J.H. et al. The role of 5-HT2A receptors in antipsychotic activity. Life Sci 1995, 56: 2209-22.
61. 2 antagonists: A concept for the treatment of schizophrenia. Curr Pharm Design 1997, 3: 367-90.
62. 2 receptor blocking agent. Curr Ther Res 1986, 40: 492-9.
63. 1C receptors. J Pharmacol Exp Ther 1992, 260: 1361-5.
64. 2 antagonist. Mol Pharmacol 1985, 27: 600-11.
65. 2 receptor blocker. Drug Dev Res 1986, 8: 205-11.
66. Borison, R.L. Clinical efficacy of serotonin-dopamine antagonists relative to classical neuroleptics, J Clin Psychopharmacol 1995, 15 (Suppl. 1): 24-9S.
67. 2C serotonin receptors. Nature J 1995, 374: 542.
68. 2 receptors in GABAergic neurons of the primate brain. Nature 1996, 381: 245-8.
69. Kato, T., Hirose, A., Ohno, Y. et al. Binding profile of SM-9018, a novel antipsychotic candidate. Jpn J Pharmacol 1990, 54: 478-81.
70. 2 antagonistic actions. Jpn J Pharmacol 1990, 53: 321-9.
71. 4 receptors in CHO cells. Jpn J Pharmacol 1997, 73 (Suppl. 1): P-234.
72. Kongsamut, S., Roehr, J.E., Cai, J. et al. Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol 1996, 317: 417-23.
73. Sainati, S.M., Hubbard, J.W., Chi, E. et al. Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol 1995, 35:713-20.
74. Jones-Humble, S.A., Durcan, M.J., Lyerly, D. etal. Preclinical neurochemical and electrophysiological profile of 1192U90, a potential antipsychotic. Neuropsychopharmacology 1996, 15: 217-30.
75. Rigdon, G.G., Norman, M.H., Cooper, B.R. et al. 1192U90 in animal tests that predict antipsychotic efficacy, anxiolysis, and extrapyramidal side effects. Neuropsychoparmacology 1996, 15: 231-42.
76. 4 receptor? Life Sci 1995, 57: 275-83.
77. Liégeois, J.-F., Rogister, F.A.; Bruhwyler, J. et al. Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: Synthesis and neurochemical study. J Med Chem 1994, 37: 519-25.
78. Liégeois, J.-F., Eyrolles, L., Dupont, L. et al. A new synthetic approach of JL13, a pyridobenzoxazepine with a potential atypical antipsychotic profile. J Pharm Belg 1997, 52 (Suppl.): 35.
79. Prous Science Trilogy Database.
80. 2 receptors, and an "atypical" antipsychotic profile in the rat. Br J Pharmacol 1995, 114 (Suppl.): Abst 156P.
81. 4 sites. Eur Neuropsychopharmacol 1995, 5: Abst P-4-13.
82. Peglion, J.-L., Audinot, V., Brocco, M. et al. S17828 and S14956. novel benzisoxazoles displaying antipsychotic properties and a low side-effect profile in animal models: A comparison to risperidone. Soc Neurosci Abstr 1994, 20: 1773.
83. Volonté, M., Cerutti, M., Giraldo, E. et al. Effect of BIMG80, a novel potential atypical antipsychotic, on dopamine levels measured by microdialysis. Eur Neuropsychopharmacol 1995, 5: Abst P-4-9.
84. Brambilla, A., Cesana, R., Gil, M. et al. Pharmacological profile of BIMG80, a novel potential atypical antipsychotic. Eur Neuropsychopharmacol 1995, 5: Abst P-4-10.
85. Volonté, M., Monferini, E., Cerutti, M. et al. BIMG80, a novel potential antipsychotic drug: Evidence for multireceptor actions and preferential release of dopamine in prefrontal cortex. J Neurochem 1997, 69: 182-90.
86. Ohno, Y., Ishida, K., Ishibashi, T. et al. Pharmacological profile of SM-13496, a novel antipsychotic agent with minimal extrapyramidal and CNS depressive side effects. Soc Neurosci Abstr 1994, 20: Abst 726. 12.
87. Ishibashi, T., Ohno, Y., Ishida, K. et al. Behavioural and biochemical studies on SM-13496, a novel atypical antipsychotic agent. Soc Neurosci Abstr 1995, 21: Abst 191.16.
88. Ishibashi, T., Ohno, Y., Ishida, K. et al. Biochemical profile of SM-13496, a novel antipsychotic candidate with minimal extrapyramidal side effects. Jpn J Pharmacol 1995, 67 (Suppl. 1): Abst P1-239.
89. Ohno, Y., Ishida, K., Ishibashi, T. et al. Pharmacological characteristics of SM-13496, a novel atypical antipsychotic candidate with minimal CNS depressive side effects. Int Acad Biomed Drug Res 1994, 158.
90. Malleron, J.-L., Comte, M.-T., Gueremy, C. et al. Naphtosultam derivatives: A new class of potent and selective 5-HT2 antagonists. J Med Chem 1991, 34: 2477-83.
91. 2 receptor antagonist. Br J Pharmacol 1992, 105: 27-36.
92. Pharmaprojects, PJB Publications Ltd., fananserin, 13/10/94.
93. 4 receptor. Eur J Pharmacol 1996, 314: 229-33.
94. Scrip 1996, 2168:20.
95. Pharmaprojects, PJB Publications Ltd. fananserin, 9/6/97.
96. 2A receptor antagonist, in rats. Br J Pharmacol 1997, 121: 515-25.
97. 4 receptor antagonist (R)-(+)-2-amino-4-(4-fluorophenyl)-5-(1-(4-(4-fluorophenyl)-4-oxobutyl) pyrrolidin-3-yl)thiazole (NRA0045). Jpn J Pharmacol 1997, 73 (Suppl. 1): 242P.
98. 4 receptor antagonist (R)-(+)-2-amino-4-(4-fluorophenyl)-5-(1-(4-(4-fluorophenyl)-4-oxobutyl) pyrrolidin-3-yl)thiazole (NRA0045). Jpn J Pharmacol 1997, 73 (Suppl. 1): 242 P.
99. 4 receptor, serotonin 5-HT2A receptor and alpha-1 adrenoceptor antagonist (R)-(+)-2-amino-4-(4-fluorophenyl)-5-(1-(4-(4-fluorophenyl)-4-oxobutyl) pyrrolidin-3-yl)thiazole (RNA0045). J Pharmacol Exp Ther 1997, 282: 56-63.
100. 4 receptor antagonists (3): Benzylydenepiperidinoethylthiazole derivatives. 214th ACS Natl Meet (Sept 7-11, Las Vegas) 1997, MEDI 17.
101. Tang, A.M., Franklin, S.R. Himes, C.S., et al. PNU-96415E, a potential antipsychotic agent with clozapine-like pharmacological properties. J Pharmacol Exp Ther 1997, 281: 440-7.
102. 4 receptor 213th ACS Natl Meet (April 13-17, San Francisco) 1997, MEDI 160.
103. Steiner, G., Hofmann, H.P., Kreiskott, H. et al. EP 35711.
104. Phillips, S.T., de Paulis, T., Baron, B.M. et al. Binding of 5-H-dibenzo[b,e][1,4]diazepine and chiral 5-H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. J Med Chem 1994, 37: 2686-96.
105. Steiner, G. Unger, L., Behl, B. et al. WO 94/00458: EP 647231.
106. Steiner, G., Bach, A., Bialojan, S. et al. LU 111995: A novel D/5-HT, receptor antagonist and potential new antipsychotic. 213th ACS Natl Meet (April 13-17, San Francisco) 1997, MEDI 186.
107. Steiner G., Munschauer, R., Klebe, G. et al. Diastereoselective synthesis of exo-6-aryl-3-azabicyclo[3.2.0]-heptane derivatives by intramolecular [2+2]photocycloadditions of diallylic amines. Heterocycles 1995, 40: 319-30.