Evaluation of the behavioral and pharmacokinetic profile of SYA013, a homopiperazine analog of haloperidol in rats

Pharmacology Biochemistry and Behavior

Volumn 102, Issue 2, 2012, Pages 294-301

  Bricker, Barbara ^a   Jackson, Tanise ^a   Boateng, Bernard ^a   Zhu, Xue Y ^a   Ablordeppey, Seth Y ^a  

^a FLORIDA A AND M UNIVERSITY   (United States)

Author keywords

5HT1A receptor; Antipsychotic profile; Catalepsy test chamber instrument; Conditioned avoidance response; Locomotor activity; SYA013

Indexed keywords

DEXAMPHETAMINE; HALOPERIDOL; HEXAHYDRO 1,4 DIAZEPINE DERIVATIVE; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; PIPERAZINE DERIVATIVE; SEROTONIN 1A ANTAGONIST; SYA 013; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; AVOIDANCE BEHAVIOR; BLOOD PLACENTA BARRIER; CATALEPSY; CONTROLLED STUDY; DOSE RESPONSE; DRUG BINDING; DRUG INHIBITION; DRUG RECEPTOR BINDING; ESCAPE BEHAVIOR; HYPOTHESIS; LOCOMOTION; MALE; MENTAL DISEASE; NONHUMAN; PHARMACOKINETICS; PRIORITY JOURNAL; PROTEIN BLOOD LEVEL; RAT; RECEPTOR BINDING; TREATMENT INDICATION;

ANIMALS; ANTIPSYCHOTIC AGENTS; AVOIDANCE LEARNING; AZEPINES; BEHAVIOR, ANIMAL; BRAIN; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DOSE-RESPONSE RELATIONSHIP, DRUG; HALOPERIDOL; MALE; PIPERAZINES; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY;

ANIMALIA; MUS; RATTUS;

EID: 84861536099     PISSN: 00913057     EISSN: 18735177     Source Type: Journal    
DOI: 10.1016/j.pbb.2012.05.003     Document Type: Article

References (50)

1. Ablordeppey SY, Altundas R, Bricker B, Zhu XY, Kumar EVKS, Jackson T, et al. Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chloro-phenyl)-1,4-diazepan-1yl]-1-(4-fluorophenyl) butan-1-one. Bioorg Med Chem 2008;16:7291-301.
2. Ahlenius S, Hillegaart V. Involvement of extrapyramidal motor mechanisms in the suppression of locomotor activity by antipsychotic drugs: a comparison between the effects produced by pre- and postsynaptic inhibition of dopaminergic neurotransmission. Pharmacol Biochem Behav 1986;24:1409-15.
3. Arnt J. Pharmacological specificity of conditioned avoidance response inhibition in rats. Inhibition by neuroleptics and correlation to dopamine receptor blockade. Acta Pharmacol Toxicol 1982;51:321-9.
4. Arterburn D, Rukstalis M, Wood C, Westbrook E, Theis K, Daar Z, et al. C-a3-02: identification of extreme weight gain among users of atypical antipsychotic medications. Clin Med Res 2011;9(3-4):160.
5. 1A receptor antagonists on hippocampal 5-hydroxytryptamine levels: (S)-WAY100135, but not WAY100635, has partial agonist properties. Eur J Pharmacol 1996;304:15-21.
6. 1A partial agonists with potential as atypical antipsychotic agents. J Med Chem 1999;42:3341-55.
7. Bourdon KH, Rae DS, Locke BZ, Narrow WE, Regier DA. Estimating the prevalence of mental disorders in U.S. adults from the epidemiologic catchment area survey. Public Health Rep 1992;107:663-8.
8. Bundgaard C, Larsen F, Kreilgaard M, Brennum LT, Olsen CK. Pharmacokinetics of sertindole and its metabolite dehydrosertindole in rats and characterization of their comparative pharmacodynamics based on in vivo D2 receptor occupancy and behavioural conditioned avoidance response. Biopharm Drug Dispos 2009;30:209-20.
9. Campbell A, Baldessarini RJ, Cremens MC. Dose-catalepsy response to haloperidol in rat: effects of strain and sex. Neuropharmacology 1988;27:1197-9.
10. Coccurello R, Moles A. Potential mechanisms of atypical antipsychotic-induced metabolic derangement: clues for understanding obesity and novel drug design. Pharmacol Ther 2010;127:210-51.
11. Depoortere R, Bardin L, Auclair AL, Kleven MS, Prinssen E, Colpaert F, et al. F15063, a compound with D2/D3 antagonist, 5-HT1A agonist and D4 partial agonist properties: (II) activity in models of positive symptoms of schizophrenia. Br J Pharmacol 2007;151:253-65.
12. Ellenbroek BA. Treatment of schizophrenia: a clinical and preclinical evaluation of neuroleptic drugs. Pharmacol Ther 1993;57:1-78.
13. Ellenbroek BA. Psychopharmacological treatment of schizophrenia: What do we have, and what could we get? Neuropharmacology. 2012;62:1371-80.
14. Ellenbroek BA, Cools AR. The paw test: an animal model for neuroleptic drugs which fulfils the criteria for pharmacological isomorphism. Life Sci 1988;42:1205-13.
15. FDA Reference ID: 3031346. Label information, p. 4. http://www. accessdata.fda.gov/drugsatfda-docs/label/2011/019758s063lbl.pdf
16. Geffen Y, Nudelman A, Gil-Ad I, Rephaeli A, Huang M, Savitsky K, et al. BL-1020: a novel antipsychotic drug with GABAergic activity and low catalepsy, is efficacious in a rat model of schizophrenia. Eur Neuropsychopharmacol 2009;19:1-13.
17. Geyer M, Ellenbroek B. Animal behavior models of the mechanisms underlying antipsychotic atypicality. Prog Neuropsychopharmacol Biol Psychiatry 2003;27:1071-9.
18. Guitart X, Codony X, Ballarin M, Dordal A, Farre AJ. E-5842: a new potent and preferential sigma ligand. Preclinical pharmacological profile. CNS Drug Rev 1998;4: 201-24.
19. Hoffman DC, Donovan H. Catalepsy as a rodent model for detecting antipsychotic drugs with extrapyramidal side effect liability. Psychopharmacology 1995;120:128-33.
20. Jones CA, McCreary AC. Serotonergic approaches in the development of novel antipsychotics. Neuropharmacology 2008;55:1056-65.
21. 2 receptors. Prog Neuropsychopharmacol Biol Psychiatry 2003;27:1081-90.
22. 1Areceptor agonist/dopamine D2 receptor antagonists to inhibit methylphenidate-induced behaviors in rats. Eur J Pharmacol 1996;313:25-34.
23. Kleven MS, Barret-Grevoz C, Slot LB, Newman-Tancredi A. Novel antipsychotic agents with 5-HT1A agonist properties: role of 5-HT1A receptor activation in attenuation of catalepsy induction in rats. Neuropharmacology 2005;49:135-43.
24. 1A receptor agonist potential antipsychotic drug. Neuropsychopharmacology 2007;32:78-94.
25. McElroy JF. Inhibition of haloperidol- and chlorpromazine-induced catalepsy by XJ448, a sigma-selective receptor antagonist. Schizophr Res 1993;9:224.
26. Meltzer HY. Atypical antipsychotic drugs. In: Bloom FE, Kupfer D, editors. Psychopharmacology: fourth generation of progress. New York: Raven Press; 1995. p. 1277-86.
27. Meltzer HY. The role of serotonin in antipsychotic drug action. Neuropsychopharmacology 1999;21:106-15.
28. Meltzer HY, Massey BW. The role of serotonin receptors in the action of atypical antipsychotic drugs. Curr Opin Pharmacol 2011;11:59-67.
29. 2 pKi values. J Pharmacol Exp Ther 1989;251:238-46.
30. Natesan S, Reckless GE, Barlow KBL, Nobrega JN, Kapur S. Amisulpride the 'atypical'atypical antipsychotic-comparison to haloperidol, risperidone and clozapine. Schizophr Res 2008;105:224-35.
31. Needham PL, Atkinson J, Skill MJ, Heal DJ. Zotepine: preclinical tests predict antipsychotic efficacy and an atypical profile. Psychopharmacol Bull 1996;32:123-8.
32. 1A receptors. Neuropharmacology 1996;35:119-21.
33. Olsen CK, Brennum LT, Kreilgaard M. Using pharmacokinetic-pharmacodynamic modelling as a tool for prediction of therapeutic effective plasma levels of antipsychotics. Eur J Pharmacol 2008;584:318-27.
34. Palenicek T, Balikova M, Rohanova M, Novak T, Horacek J, Fujakova M, et al. Behavioral, hyperthermic and pharmacokinetic profile of para- methoxymethamphetamine (PMMA) in rats. Pharmacol Biochem Behav 2011;98:130-9.
35. Prinssen EPM, Kleven MS, Koek W. The cataleptogenic effects of the neuroleptic nemonapride are attenuated by its 5-HT1A receptor agonist properties. Eur J Pharmacol 1998;356:189-92.
36. Reeve B, Dingwall B, Darlington CL, Scott SJ, Sansom AJ, Smith PF. Simple device for quantifying drug effects on the righting reflex. Pharmacol Biochem Behav 1992;42:183-5.
37. Sanberg PR, Bunsey MD, Giordano M, Norman AB. The catalepsy test: its ups and downs. Behav Neurosci 1988;102:748-59.
38. Schlumberger C, Pietraszek M, Gravius A, Danysz W. Effects of a positive allosteric modulator of mGluR5 ADX47273 on conditioned avoidance response and PCP-induced hyperlocomotion in the rat as models for schizophrenia. Pharmacol Biochem Behav 2010;95:23-30.
39. Seeger TF, Seymour PA, Schmidt AW, Zorn SH, Schulz DW, Lebel LA, et al. Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity. Pharmacol Exp Ther 1995;275:101-13.
40. Shimokawa Y, Akiyama H, Kashiyama E, Koga T, Miyamoto E. High performance liquid chromatographic methods for the determination of aripiprazole with ultraviolet detection in rat plasma and brain: application to the pharmacokinetic study. J Chromatogr B 2005;821:8-14.
41. Sikazwe DMN, Li S, Mardenborough L, Cody V, Roth BL, Ablordeppey SY. Haloperidol: towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors. Bioorg Med Chem Lett 2004;14:5739-42.
42. Siuciak JA, Chapin DS, McCarthy SA, Guanowsky V, Brown JC, Phoebe Marala R, et al. CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity. Neuropharmacology 2007;52:279-90.
43. Starrenburg FCJ, Bogers JPAM. How can antipsychotics cause diabetes mellitus? Insights based on receptor-binding profiles, humoral factors and transporter proteins. Eur Psychiatry 2009;24:164-70.
44. Struyker-Boudier HA, Cools AR. (3,4-Dihydroxyphenylimino)-2-imidazoline (DPI): a stimulant of alpha-adrenoceptors and dopamine receptors. J Pharm Pharmacol 1984;36:859-60.
45. Sun L, Lau CE. Intravenous and oral clozapine pharmacokinetics, pharmacodynamics, and concentration-effect relations: acute tolerance. Eur J Pharmacol 2000;398: 225-38.
46. Sun T, Zhao C, Hu G, Li M. Iptakalim: a potential antipsychotic drug with novel mechanisms? Eur J Pharmacol 2010;634:68-76.
47. Vilar S, Chakrabarti M, Costanzi S. Prediction of passive blood-brain partitioning: straightforward and effective classification models based on in silico derived physicochemical descriptors. J Mol Graph Model 2010;28:899-903.
48. 2 receptor occupancy is a common mechanism underlying animal models of antipsychotics and their clinical effects. Neuropsychopharmacology 2001;25:633-41.
49. Wadenberg MLG. Conditioned avoidance response in the development of new antipsychotics. Curr Pharm Des 2010;16:358-70.
50. Wadenberg MLG, Hicks PB. The conditioned avoidance response test re-evaluated: is it a sensitive test for the detection of potentially atypical antipsychotics? Neurosci Biobehav Rev 1999;23:851-62.