A 5-HT2A receptor inverse agonist, ACP-103, reduces tremor in a rat model and levodopa-induced dyskinesias in a monkey model.
作者： K VANOVER , A BETZ , S WEBER , F BIBBIANI , A KIELAITE
DOI: 10.1016/J.PBB.2008.04.010
关键词:
摘要: A potent 5-hydroxytryptamine (5-HT)2A receptor inverse agonist and antagonist, ACP-103 [N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1, active:salt)], was evaluated for its ability to reduce the primary motor symptom of tremor using tacrine-induced tremulous jaw movements in rats, which is an animal model parkinsonian tremor. Furthermore, levodopa-induced dyskinesias monkeys rendered with MPTP [1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine]. reduced rats. In addition, administered combination levodopa caused a dose-related reduction monkeys. These data suggest that may have potential Parkinson's disease.
elsevier.com
sci-hub.se 参考文章(57)
Elliott Richelson, Terry Souder, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sciences. ,vol. 68, pp. 29- 39 ,(2000) , 10.1016/S0024-3205(00)00911-5
T N Chase, J D Oh, Striatal mechanisms and pathogenesis of parkinsonian signs and motor complications. Annals of Neurology. ,vol. 47, ,(2000)
C. W. Olanow, W. C. Koller, An algorithm (decision tree) for the management of Parkinson's disease: treatment guidelines. American Academy of Neurology. Neurology. ,vol. 50, ,(1998) , 10.1212/WNL.50.3_SUPPL_3.S1
Brian B. Carlson, Ania Wisniecki, J. Salamone, Local injections of the 5-hydroxytryptamine antagonist mianserin into substantia nigra pars reticulata block tremulous jaw movements in rats: studies with a putative model of Parkinsonian tremor. Psychopharmacology. ,vol. 165, pp. 229- 237 ,(2003) , 10.1007/S00213-002-1247-3
Kazuya Kannari, Hiroshi Yamato, Huo Shen, Masahiko Tomiyama, Toshihiro Suda, Muneo Matsunaga, Activation of 5-HT(1A) but not 5-HT(1B) receptors attenuates an increase in extracellular dopamine derived from exogenously administered L-DOPA in the striatum with nigrostriatal denervation. Journal of Neurochemistry. ,vol. 76, pp. 1346- 1353 ,(2001) , 10.1046/J.1471-4159.2001.00184.X
K. Krebs-Thomson, S. C. Harvey, N. Nash, K. E. Vanover, M. R. Brann, D. M. Weiner, M. A. Geyer, G. E. Croston, S. B. Powell, D. F. C. Gibson, E. Donohue, C. M. Andersson, U. Hacksell, H. C. Hansen, E. A. Currier, T. A. Spalding, E. S. Burstein, 5-Hydroxytryptamine2A Receptor Inverse Agonists as Antipsychotics Journal of Pharmacology and Experimental Therapeutics. ,vol. 299, pp. 268- 276 ,(2001)
F Durif, B Debilly, M Galitzky, D Morand, F Viallet, M Borg, S Thobois, E Broussolle, O Rascol, None, Clozapine improves dyskinesias in Parkinson disease A double-blind, placebo-controlled study Neurology. ,vol. 62, pp. 381- 388 ,(2004) , 10.1212/01.WNL.0000110317.52453.6C
Jennifer T. Trevitt, Maureen Lyons, Juliet Aberman, Debra Carriero, Marianne Finn, J. D. Salamone, Effects of clozapine, thioridazine, risperidone and haloperidol on behavioral tests related to extrapyramidal motor function Psychopharmacology. ,vol. 132, pp. 74- 81 ,(1997) , 10.1007/S002130050322
Gonzalo J. Gomez Arevalo, Oscar S. Gershanik, Modulatory effect of clozapine on levodopa response in parkinson's disease: A preliminary study Movement Disorders. ,vol. 8, pp. 349- 354 ,(1993) , 10.1002/MDS.870080317
Elissa J Chesler, John D Salamone, Effects of acute and repeated clozapine injections on cholinomimetic-induced vacuous jaw movements. Pharmacology, Biochemistry and Behavior. ,vol. 54, pp. 619- 624 ,(1996) , 10.1016/0091-3057(95)02280-5