Selective agents for serotonin2c (5-HT2c) receptor

Current Topics in Medicinal Chemistry

Volumn 6, Issue 18, 2006, Pages 1927-1970

  Lacivita, Enza ^a   Leopoldo, Marcello ^a  

^a UNIVERSITY OF BARI   (Italy)

Author keywords

Anxiolytic; CYP1A2; mCPP; Phenylpiperazine; RO600175; WAY 629

Indexed keywords

(2,3 DIHYDROBENZOFURAN 2 YL)METHYLAMINE DERIVATIVE; 1 (3 PYRIDYLCARBAMOYL)INDOLINE DERIVATIVE; 1,2,3,5 TETRAHYDRO 5 METHYL 1 (3 PYRIDYLCARBAMOYL)PYRROLO[2,3 F]INDOLE; 2 (6 CHLORO 5 FLUORO 1 INDOLYL) 1 METHYLETHYLAMINE; 2 CHLOROBENZYLPIPERAZINE DERIVATIVE; 2 TRIFLUOROMETHYLBENZYLPIPERAZINE DERIVATIVE; 2,3,4,4A TETRAHYDRO 1H PYRAZINO[1,2 A]QUINOXALIN 5(6H) ONE; 3 TRIFLUOROMETHYLBENZYLPIPERAZINE DERIVATIVE; 5 METHYL 1 [[2 [(2 METHYL 3 PYRIDYL)OXY] 5 PYRIDYL]CARBAMOYL] 6 TRIFLUOROMETHYLINDOLINE; 5 METHYLTHIO 1 (3 PYRIDYLCARBAMOYL) 6 (TRIFLUOROMETHYL)INDOLINE; 6 CHLORO 5 METHYL 1 [[2 [(2 METHYL 3 PYRIDYL)OXY] 5 PYRIDYL]CARBAMOYL]INDOLINE; 6,8 DICHLOROBENZAZEPINE; BENZAZEPINE DERIVATIVE; DIHYDROBENZOFURAN DERIVATIVE; INDAZOLE DERIVATIVE; INDOLE DERIVATIVE; INDOLINYL CINNAMIDE DERIVATIVE; PIPERAZINE DERIVATIVE; PYRROLOQUINOLINE DERIVATIVE; QUINOLINE DERIVATIVE; R 95292; SB 247853; SEROTONIN 2C AGONIST; SEROTONIN 2C ANTAGONIST; SEROTONIN 2C RECEPTOR; SEROTONIN RECEPTOR AFFECTING AGENT; TRIAZAFLUORNE DERIVATIVE; TRYPTAMINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; WAY 629; SEROTONIN AGONIST; SEROTONIN ANTAGONIST;

ANXIETY DISORDER; APPETITE; CHEMICAL MODIFICATION; DEPRESSION; DOSE RESPONSE; DRUG ABSORPTION; DRUG IDENTIFICATION; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; NONHUMAN; OBSESSIVE COMPULSIVE DISORDER; PANIC; PATENT; RECEPTOR AFFINITY; RECEPTOR INTRINSIC ACTIVITY; REGULATORY MECHANISM; REVIEW; STRUCTURE ACTIVITY RELATION; SUBSTANCE ABUSE; TRANQUILIZING ACTIVITY; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; DRUG ANTAGONISM; DRUG POTENTIATION;

ANIMALS; HUMANS; MOLECULAR STRUCTURE; RECEPTOR, SEROTONIN, 5-HT2C; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS;

EID: 33749515078     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/156802606778522168     Document Type: Review

References (57)

1. Hoyer, D.; Hannon, J. P.; Martin, G. R. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol. Biochem. Behav. 2002, 71, 533-554.
2. 2C receptor as a potential therapeutic target for the design of antiobesity and antiepileptic drugs. Drugs Fut. 2001, 26, 383-393.
3. 1C receptors mediate 1-(3-chlorophenyl)piperazine-induced hypophagia. Br. J. Pharmacol. 1991, 103, 2016-2020.
4. 2C serotonin receptors. Nature 1995, 374, 542-546.
5. 2C receptor antagonist. Neuropharmacology 1997, 36, 609-620.
6. 2B receptor antagonists: neurochemical and behavioural studies. Neuropharmacology 2000, 39, 2318-2328.
7. 2B receptors in regulating generalised seizure threshold in rodents. Eur. J. Pharmacol. 1998, 359, 33-40.
8. 2C receptor antagonist Br. J. Pharmacol. 1999, 126, 572-574.
9. Reynolds, G. P. Receptor mechanisms in the treatment of schizophrenia. J. Psychopharmacol. 2004, 18, 340-345.
10. 2 ligands on three mouse models of anxiety. Behav. Brain Res. 2003, 140, 203-214.
11. 2C receptor antagonist, SB-242084, in tests of anxiety. Pharmacol. Biochem. Behav. 2002, 71, 615-625.
12. 2C receptors potentiates consequences of serotonin reuptake blockade. Neuropsychopharmacology 2004, 29, 1782-1789.
13. 2C receptors on cocaine- and food-maintained behavior. J. Pharmacol. Exp. Ther. 2000, 295, 1183-1191.
14. 2C receptors. Eur. J. Pharmacol. 2003, 480, 151-162.
15. 2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists. Eur. J. Pharmacol. 1997, 325, 9-12.
16. Bancila, M.; Verge, D.; Rampin, O.; Backstrom, J. R.; Sanders-Bush, E.; McKenna, K. E.; Marson, L.; Calas, A.; Giuliano, F. 5-Hydroxytryptamine2C receptors on spinal neurons controlling penile erection in the rat. Neuroscience 1999, 92, 1523-1537.
17. 2C receptor antagonist. J. Med Chem. 1997, 40, 3494-3496.
18. 2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines. J. Med. Chem. 1998, 41, 1598-1612.
19. B receptor antagonists. Bioorg. Med. Chem. 1999, 7, 2767-2773.
20. 2C receptor inverse agonists: identification of 5-methyl-1- 2-[(2-methyl-3-pyridyl) oxy]-5-pyridyl]carbamoyl]-6-trifluoromethylin-doline (SB-243213) as a potential antidepressant/ anxiolytic agent. J. Med. Chem. 2000, 43, 1123-1134.
21. 2C receptor inverse agonists with potential as antidepressant/ anxiolytic agents. Bioorg. Med. Chem. Lett. 2000, 10, 1863-1866.
22. 2C receptor inverse agonists. Bioorg. Med. Chem. Lett. 2000, 10, 1867-1870.
23. Bromidge, S. M.; Lovell, P. J.; Moss, S. F.; Serafinowska, H. T. Indoline derivatives as 5-HT2C antagonists, useful as anxiolytics and antidepressants. PCT Int. Appl. WO 2002014273, 2002. Chem. Abstr. 136:183704.
24. C receptor antagonists. Bioorg. Med. Chem. Lett. 2005, 15, 4989-4993.
25. 2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder. J. Med. Chem. 1997, 40, 2762-2769.
26. 2C receptor agonists. Bioorg. Med. Chem. Lett. 2004, 14, 2367-2370.
27. 2C agonists. PCT Int. Appl. WO 2000012481, 2000. Chem. Abstr. 132:194372.
28. Adams, D. R.; Bentley, J. M.; Roffey, J. R. A.; Bodkin, C. D.; Mansell, H. L.; George, A. R.; Cliffe, I. A. Preparation of pyrroloquinolines for treatment of obesity. PCT Int. Appl. WO 2000012502, 2000. Chem. Abstr. 132:194301.
29. 2C receptor. PCT Int. Appl. WO 2001012603, 2001. Chem. Abstr. 134:193339.
30. 2C receptor. Eur. J. Med. Chem. 1997, 32, 253-261.
31. Adams, D. R.; Bentley, J. M.; Davidson, J.; Duncton, M.; Porter, R. H. P. Preparation of Pyrazino(aza)indole derivatives. PCT Int. Appl. WO 200044753, 2000. Chem. Abstr. 133:150579.
32. 2 receptor ligands for the treatment of obesity and other disorders. PCT Int. Appl. WO 2002072584, 2002. Chem. Abstr. 137:232679.
33. 2 receptor ligands. PCT Int. Appl. WO 2003064423, 2003. Chem. Abstr. 139:164811.
34. Bentley, J. M.; Hebeisen, P.; Muller, M.; Richter, H.; Roever, S.; Mattei, P.; Taylor, S. Preparation of 1,2,3,4,10,10a-hexahydro-1H-pyrazino[1,2-a]indoles and analogs and 5-HT receptor agonists for treatment of CNS diseases, cardiovascular disorders, gastrointestinal disorders, and obesity. PCT Int. Appl. WO 2002010169, 2002. Chem. Abstr. 136:167392.
35. 2C receptor agonists. Bioorg. Med. Chem. Lett. 2005, 15, 3604-3608.
36. 2C agonists. Bioorg. Med. Chem. Lett. 2003, 13, 2369-2372.
37. 2C receptor. Bioorg. Med. Chem. Lett. 2004, 14, 2603-2607.
38. 2C receptor agonists. PCT Int. Appl. WO 2002042304, 2002. Chem. Abstr. 137:6202.
39. 2A receptor: potential therapeutic applications for epilepsy and obesity. Bioorg, Med. Chem. Lett. 2000, 10, 919-921.
40. 2C agonist. Bioorg. Med. Chem. Lett. 2005, 15, 4555-4559.
41. Welmaker, G. S.; Nelson, J. A.; Sabalski, J. E.; Sabb, A. L.; Potoski, J. R.; Graziano, D.; Kagan, M.; Coupet, J.; Dunlop, J.; Mazandarani, H.; Rosenzweig-Lipson, S., Sukoff,. S.; Zhang, Y. Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino [1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines. Bioorg. Med. Chem. Lett. 2000, 10, 1991-1994.
42. 2C agonists. U.S. US 6372745, 2002. Chem. Abstr 136:294853.
43. 2C receptor binding affinities of novel pyrimidine derivatives. Bioorg. Med. Chem. Lett. 2002, 12, 3097-3099.
44. 2 receptor. PCT Int. Appl. WO 2002040457, 2002. Chem. Abstr. 136:401780.
45. 2C receptor agonists. U.S. US 6465467, 2002. Chem. Abstr. 137:294982.
46. Briner, K.; Burkholder, T. P.; Heiman, M. L.; Nelson, D. L. G. Preparation of 1-(4-trifluoromethylbenzofur-7-yl)piperazines useful as serotonin agonists. PCT Int. Appl. WO 2001009123, 2001. Chem. Abstr. 134:163062.
47. 2 receptor. PCT Int. Appl. WO 2002048124, 2002. Chem. Abstr. 137:47226.
48. 2C receptor antagonists. Part 1. Bioorg. Med. Chem. Lett. 2002, 12, 243-248.
49. 2C receptor antagonists. Part 2. Bioorg. Med. Chem. Lett. 2002, 12, 249-253.
50. 2C antagonist with potential anxiolytic properties. Bioorg. Med. Chem. Lett. 2002, 12, 3573-3577.
51. 2C receptor antagonists. Bioorg. Med. Chem. Lett. 2004, 14, 2765-2771.
52. Smith, J.; Smith, B. Preparation of benzazepines as 5HT2C receptor modulators. PCT Int. Appl. WO 2003086306, 2003. Chem. Abstr. 139:337897.
53. 2C receptor agonists for the treatment of obesity. Bioorg. Med. Chem. Lett. 2005, 15, 1467-1470.
54. 2C receptor-associated diseases. PCT Int. Appl. WO 2005042490, 2005. Chem. Abstr. 142:463621.
55. 2C agonists and partial agonists for treating central nervous system disorders like schizophrenia PCT Int. Appl. WO 2005044812, 2005. Chem. Abstr. 142:481936.
56. 2C receptor homodimers on the plasma membrane of living cells. Biochemistry 2004, 43, 13963-13971.
57. Herrick-Davis, K.; Grinde, E.; Harrigan, T. J.; Mazurkiewicz, J. E. Inhibition of serotonin 5-hydroxytryptamine2c receptor function through heterodimerization: receptor dimers bind two molecules of ligand and one G-protein. J. Biol. Chem. 2005, 280, 40144-40151.