ACP-103: 5-HT2A receptor inverse agonist treatment of psychosis treatment of sleep disorders

Drugs of the Future

Volumn 31, Issue 11, 2006, Pages 939-943

  Wang, Y ^a   Bolos J ^b   Serradell, N ^b  

^a Prous Science ^*  (United States)

^b PROUS SCIENCE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

ACP 103; AMPHETAMINE; DIZOCILPINE; HALOPERIDOL; N (4 FLUOROBENZYL) N' (4 ISOBUTOXYBENZYL) N (1 METHYLPIPERIDIN 4 YL)UREA HEMIFUMARATE; NEUROLEPTIC AGENT; PLACEBO; RISPERIDONE; SEROTONIN 2A ANTAGONIST; SEROTONIN 2A RECEPTOR; UNCLASSIFIED DRUG;

AKATHISIA; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG DOSE COMPARISON; DRUG DOSE ESCALATION; DRUG EFFECT; DRUG EFFICACY; DRUG METABOLISM; DRUG POTENCY; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; HUMAN; INSOMNIA; MAXIMUM TOLERATED DOSE; NONHUMAN; PARKINSON DISEASE; PLASMA HALF LIFE; PROLACTIN RELEASE; PSYCHOSIS; RANDOMIZED CONTROLLED TRIAL; REPEATED DRUG DOSE; REVIEW; SCHIZOPHRENIA; SIDE EFFECT; SINGLE DRUG DOSE; SLEEP DISORDER; SLOW WAVE SLEEP; UNSPECIFIED SIDE EFFECT;

EID: 33846497853     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.2006.031.11.1047693     Document Type: Review

References (22)

1. Thygesen, M., Schlienger, N., Tolf, B.-R., Blatter, F., Berghausen, J. (Acadia Pharmaceuticals, Inc.). Salts of N-(4-fluorobenzyl)-N-(1- methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation. WO 2006036874.
2. Freedman, R. Schizophrenia. New Engl J Med 2003, 349(18): 1738-49.
3. Seeman, R Atypical antipsychotics: Mechanism of action. Can J Psychiatry 2002, 47(1): 27-38.
4. Snyder, S. The dopamine hypothesis of schizophrenia: Focus on the dopamine receptor. Am J Psychiatry 1976, 133(2): 197-202.
5. Sawa, A., Snyder, S.H. Schizophrenia: Diverse approaches to a complex disease. Science 2002, 296(5568): 692-5.
6. Thaker, G.K., Carpenter, W.T. Jr. Advances in schizophrenia. Nat Med 2001, 7(6): 667-71.
7. Weiner, D.M., Burstein, E.S., Nash, N. et al. 5-Hydroxytryptamine2A receptor inverse agonists as antipsychotics. J Pharmacol Exp Ther 2001, 299(1): 268-76.
8. Vanover, K.E., Harvey, S.C., Son, T. et al. Pharmacological characterization of AC-90179: A selective 5-HT2A receptor inverse agonist. J Pharmacol Exp Ther 2004, 310(3): 943-51.
9. Vanover, K.E., Weiner, D.M., Makhay, M. et al. Pharmacological and behavioral profile of N-(4-fluorophenyl-methyl)-N-(1-methylpiperidin-4-yl)- N′-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxy- butanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine2A receptor inverse agonist. J Pharmacol Exp Ther 2006, 317(2): 910-8.
10. Vanover, K.E., Lameh, J., Gardell, L.R. et al. ACP-103, a potent 5-HT-2A receptor inverse agonist, as an adjunctive therapy in schizophrenia. Acta Pharmacol Sin [15th World Congr Pharmacol (July 2-7, Beijing) 2006] 2006, 27(Suppl. 1): Abst P040047.
11. 2A receptor inverse agonist, improves the efficacy and side effect profile of haloperidol in experimental models. Schizophr Res [13th Bienn Winter Workshop Schizophr Res (Feb 4-10, Davos) 2006] 2006, 81(Suppl. 1): Abst 33.
12. 2A receptor inverse agonist, in the human brain. Schizophr Res [13th Bienn Winter Workshop Schizophr Res (Feb 4-10, Davos) 2006] 2006, 81(Suppl, 1): Abst 179.
13. 2A receptor inverse agonist. Safety, tolerability, and pharmacokinetics in healthy volunteers. Int J Neuropsychopharmacol [24th CINP Congr (June 20-24, Paris) 2004] 2004, 7(Suppl. 2): Abst P01.461.
14. 2A receptor inverse agonist in Parkinson's disease patients. Mov Disord [9th Int Congr Parkinson's Dis Mov Disord (March 5-8, New Orleans) 2005] 2005, 20(Suppl. 10): Abst P241.
15. Grannen, A.E., Vanover, K.E., Weiner, D.M. et al. Reduction of haloperidol-induced side effects by ACP-103 in healthy volunteers. Clin Pharmacol Ther [Annu Meet Am Soc Clin Pharmacol Ther (ASCPT) (March 2-6, Orlando) 2005] 2005, 77(2): Abst LB-4.
16. Vanover, K.E., Taylor, E.M., Weiner, D., Davis, R.E., van Kammen, D., Meltzer, H.Y. ACP-103 reduces psychosis without impairing motor function in Parkinson's disease. Int J Neuropsychopharmacol [25th CINP Congr (July 9-13, Chicago) 2006] 2006, 9(Suppl. 1): Abst P01.229.
17. ACP-103 reduces haloperidol-induced akathisia in patients with schizophrenia. DailyDrugNews.com December 7, 2005.
18. ACP-103 increases slow wave sleep in clinical study. DailyDrugNews.com April 24, 2006.
19. Anipsychotic and motor effects of ACP-103 when administered in combination with haloperidol and risperidone (NCT00361166). ClinicalTrials.gov Web site 2006.
20. 2A/2C inverse agonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. Psychopharmacology 2006, 183(2): 144-53.
21. 2A/2C inverse agonist ACP103 on dopamine (DA) efflux in rat brain. 35th Annu Meet Soc Neurosci (Nov 12-16, Washington, D.C.) 2005, Abst 914.8.
22. 2A receptor occupancy and pharmacodynamic measures at plasma steady state with ACP-103. Int J Neuropsychopharmacol [25th CINP Congr (July 9-13, Chicago) 2006] 2006, 9(Suppl. 1): Abst P03.088.