Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: II. Behavioural characterisation of RG-15

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 378, Issue 5, 2008, Pages 529-539

  Gyertyán, István ^a   Sághy, Katalin ^a   Laszy, Judit ^a   Elekes, Ottilia ^a   Kedves, Rita ^a   Gémesi, Larisza I ^a   Pásztor, Gabriella ^a   Zájer Balázs, Mária ^a   Kapás, Margit ^a   Ágai Csongor, Éva ^a   Domány, György ^a   Kiss, Béla ^a   Szombathelyi, Zsolt ^a  

^a GEDEON RICHTER LTD   (Hungary)

Author keywords

Antipsychotic; Cognitive improvement; Dopamine D3 receptor antagonist; Lack of catalepsy; RG 15; Schizophrenia

Indexed keywords

AMISULPRIDE; AMPHETAMINE; CLOZAPINE; DIAZEPAM; DOPAMINE 2 RECEPTOR; DOPAMINE 3 RECEPTOR; DOPAMINE RECEPTOR BLOCKING AGENT; HALOPERIDOL; N [4 [2 [4 (3 CYANO 5 TRIFLUOROMETHYLPHENYL)PIPERAZIN 1 YL]ETHYL]CYCLOHEXYL] 3 PYRIDINESULFONIC AMIDE; NEUROLEPTIC AGENT; OLANZAPINE; RG 15; SCOPOLAMINE BROMIDE; UNCLASSIFIED DRUG; BENZODIAZEPINE DERIVATIVE; DRUG DERIVATIVE; N (4 (2 (4 (3 CYANO 5 TRIFLUOROMETHYLPHENYL)PIPERAZIN 1 YL)ETHYL)CYCLOHEXYL) 3 PYRIDINESULFONIC AMIDE; N-(4-(2-(4-(3-CYANO-5-TRIFLUOROMETHYLPHENYL)PIPERAZIN-1-YL)ETHYL)CYCLOHEXYL)-3-PYRIDINESULFONIC AMIDE; PYRIDINE DERIVATIVE; SULFONAMIDE; SULPIRIDE; SULTOPRIDE;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; AVOIDANCE BEHAVIOR; CATALEPSY; COGNITION; CONDITIONING; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BRAIN LEVEL; DRUG EFFICACY; EXTRAPYRAMIDAL SYMPTOM; HYPERACTIVITY; LEARNING DISORDER; MALE; MAXIMUM PLASMA CONCENTRATION; MOTOR ACTIVITY; NEGATIVE SYNDROME; NONHUMAN; POSITIVE SYNDROME; RAT; RECEPTOR AFFINITY; TIME TO MAXIMUM PLASMA CONCENTRATION; ANIMAL; BIOAVAILABILITY; CHEMICALLY INDUCED DISORDER; COMPARATIVE STUDY; DOSE RESPONSE; DRUG ANTAGONISM; DRUG EFFECT; TISSUE DISTRIBUTION; WISTAR RAT;

ANIMALS; ANTIPSYCHOTIC AGENTS; AVOIDANCE LEARNING; BENZODIAZEPINES; BIOLOGICAL AVAILABILITY; CATALEPSY; CLOZAPINE; DOPAMINE ANTAGONISTS; DOSE-RESPONSE RELATIONSHIP, DRUG; MALE; MOTOR ACTIVITY; PYRIDINES; RATS; RATS, WISTAR; RECEPTORS, DOPAMINE D2; RECEPTORS, DOPAMINE D3; SULFONAMIDES; SULPIRIDE; TISSUE DISTRIBUTION;

EID: 54249166152     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00210-008-0311-x     Document Type: Article

References (41)

1. D Accili CS Fishburn J Drago H Steiner JE Lachowicz BH Park EB Gauda EJ Lee MH Cool DR Sibley CR Gerfen H Westphal S Fuchs 1996 A targeted mutation of the D3 dopamine receptor gene is associated with hyperactivity in mice Proc Natl Acad Sci USA 93 1945 1949
2. S Ahlenius 1999 Clozapine: dopamine D1 receptor agonism in the prefrontal cortex as the code to decipher a Rosetta stone of antipsychotic drugs Pharmacol Toxicol 84 193 196
3. DM Coward 1992 General pharmacology of clozapine Brit J Psychiatry Suppl 17 5 11
4. EV Gurevich JN Joyce 1999 Distribution of dopamine D3 receptor expressing neurons in the human forebrain: comparison with D2 receptor expressing neurons Neuropsychopharmacology 20 60 80
5. I Gyertyán K Sághy 2004 Effects of dopamine D3 receptor antagonists on spontaneous and agonist-reduced motor activity in NMRI mice and Wistar rats: comparative study with nafadotride, U 99194A and SB 277011 Behav Pharmacol 15 253 262
6. I Gyertyán K Sághy 2007 The selective dopamine D3 receptor antagonists, SB 277011-A and S33084 block haloperidol-induced catalepsy in rats Eur J Pharmacol 572 171 174
7. J Ichikawa J Dai IA O'Laughlin WL Fowler HY Meltzer 2002 Atypical, but not typical, antipsychotic drugs increase cortical acetylcholine release without an effect in the nucleus accumbens or striatum Neuropsychopharmacology 26 325 339
8. JN Joyce 2001 Dopamine D3 receptor as a therapeutic target for antipsychotic and antiparkinsonian drugs Pharmacol Ther 90 231 259
9. HO Kalkman E Loetscher 2003 a2C-Adrenoceptor blockade by clozapine and other antipsychotic drugs Eur J Pharmacol 462 33 40
10. Kiss B, Laszlovszky I, Horváth A, Némethy Z, Schmidt É, Bugovics G, Gyertyán I, Ágai-Csongor É, Domány G, Szombathelyi Z (2008) Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic activity. I. Neurochemical characterisation of RG-15. Naunyn-Schmiederbergs Arch Pharmacol DOI 10.1007/s00210-008-0308-5
11. LP Lacroix ME Hows AJ Shah JJ Hagan CA Heidbreder 2003 Selective antagonism at dopamine D3 receptors enhances monoaminergic and cholinergic neurotransmission in the rat anterior cingulate cortex Neuropsychopharmacology 28 839 849
12. J Laszy I Laszlovszky I Gyertyán 2005 Dopamine D3 receptor antagonists improve the learning performance in memory-impaired rats Psychopharmacology 179 567 575
13. Lecrubier Y (2003) Amisulpride as a model: clinical effects of a pure dopaminergic agent. In: Kapur S, Lecrubier Y (eds) Dopamine in the pathophysiology and treatment of schizophrenia. New findings. Martin Dunitz, London and New York, pp 69-91
14. G Marchese F Bartholini S Ruiu P Casti P Saba G Gessa L Pani 2002 Effect of the amisulpride isomers on rat catalepsy Eur J Pharmacol 444 69 74
15. HY Meltzer 1994 An overview of the mechanism of action of clozapine J Clin Psychiatry 55 Suppl B 47 52
16. HY Meltzer Z Li Y Kaneda J Ichikawa 2003 Serotonin receptors: their key role in drugs to treat schizophrenia Prog Neuro-Psychopharmacol Biol Psychiatry 27 1159 1172
17. MJ Millan H Gressier M Brocco 1997 The dopamine D3 receptor antagonist, (+)-S 14297, blocks the cataleptic properties of haloperidol in rats Eur J Pharmacol 321 R7 R9
18. 3 receptors: II. Functional and behavioral profile compared with GR218,231 and L741,626 J Pharmacol Exp Ther 293 1063 1073
19. MJ Millan L Seguin A Gobert D Cussac M Brocco 2004 The role of dopamine D3 compared with D2 receptors in the control of locomotor activity: a combined behavioural and neurochemical analysis with novel, selective antagonists in rats Psychopharmacology (Berl) 174 341 357
20. MJ Millan B Di Cara A Dekeyne F Panayi L De Groote D Sicard L Cistarelli R Billiras A Gobert 2007 Selective blockade of dopamine D(3) versus D(2) receptors enhances frontocortical cholinergic transmission and social memory in rats: a parallel neurochemical and behavioural analysis J Neurochem 100 1047 1061
21. NA Moore NC Tye MS Axton FC Risius 1992 The behavioral pharmacology of olanzapine, a novel "atypical" antipsychotic agent J Pharmacol Exp Ther 262 545 551
22. T Morimoto K Hashimoto H Yasumatsu H Tanaka M Fujimura M Kuriyama K Kimura S Takehara K Yamagami 2002 Neuropharmacological profile of a novel potential atypical antipsychotic drugY-931 (8-fluoro-12-(4-methylpiperazin-1-yl) - 6H-[1]benzothieno[2,3-b][1,5] benzodiazepine maleate) Neuropsychopharmacology 26 456 467
23. S Nyberg Y Nakashima A-L Nordström C Halldin L Farde 1996 Positron emission tomography of in vivo binding characteristics of atypical antipsychotic drugs. Review of D2 and 5-HT2 receptor occupancy studies and clinical response Br J Psychiatry 168 40 44
24. GH Perrault R Depoortere E Morel DJ Sanger B Scatton 1997 Psychopharmacological profile of amisulpride: an antipsychotic drug with presynaptic D2/D3 dopamine receptor antagonist activity and limbic selectivity J Pharmacol Exp Ther 280 73 82
25. LM Pritchard AH Newman RK McNamara AD Logue B Taylor JA Welge M Xu J Zhang NM Richtand 2007 The dopamine D3 receptor antagonist NGB 2904 increases spontaneous and amphetamine-stimulated locomotion Pharmacol Biochem Behav 86 718 726
26. P Protais C Hermier J Costentin 1985 The discriminant dopamine antagonist property of benzamides is observed at various times after their systemic or intracerebroventricular administration Neuropharmacology 24 861 867
27. C Reavill SG Taylor MD Wood T Ashmeade NE Austin KY Avenell I Boyfield CL Branch J Cilia MC Coldwell MS Hadley AJ Hunter P Jeffrey F Jewitt CN Johnson DN Jones AD Medhurst DN Middlemiss DJ Nash GJ Riley C Routledge G Stemp KM Thewlis B Trail AK Vong JJ Hagan 2000 Pharmacological actions of a novel, high-affinity, and selective human dopamine D3 receptor antagonist, SB-277011-A J Pharmacol Exp Ther 294 1154 1165
28. NM Richtand SC Woods SP Berger SM Strakowski 2001 D3 dopamine receptor, behavioral sensitization, and psychosis Neurosci Biobehav Rev 25 427 443
29. F Sautel N Griffon P Sokoloff J-C Schwartz C Launay P Simon J Costetin A Schienfelder F Garrido A Mann 1995 Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents J Pharmacol Exp Ther 275 1239 1246
30. B Scatton Y Claustre A Cudennec A Oblin G Perrault DJ Sanger H Schoemaker 1997 Amisulpride: from animal pharmacology to therapeutic action Int Clin Psychopharmacol 12 Suppl 2 S29 S36
31. Schoemaker H, Claustre Y, Fage D, Rouquier L, Chergui K, Curet O, Oblin A, Gonon F, Carter C, Benavides J, Scatton B (1997) Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. J Pharmacol Exp Ther 280:83-97
32. JC Schwartz J Diaz C Pilon P Sokoloff 2000 Possible implications of the dopamine D3 receptor in schizophrenia and in antipsychotic drug actions Brain Res Rev 31 77 287
33. P Seeman 2001 Antipsychotic drugs, dopamine receptors and schizophrenia Clin Neurosci Res 1 53 60
34. S Sigala C Missale P Spano 1997 Opposite effects of dopamine D2 and D3 receptors in learning and memory in the rat Eur J Pharmacol 336 107 112
35. Stahl SM (2002) Essential psychopharmacology. Neuroscientific basis and practical applications. 2nd edn. Cambridge University Press, Cambridge
36. 3 receptors on dopaminergic and nondopaminergic cell bodies and terminals J Pharmacol Exp Ther 295 1223 1231
37. G Stille H Lauener G Eichenberger 1971 The pharmacology of 8-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]-diazepine (Clozapine) Il Farmaco 26 603 625
38. M Vasse P Protais J Costentin JC Schwartz 1985 Unexpected potentiation by discriminant benzamide derivatives of stereotyped behaviours elicited by dopamine agonists in mice Naunyn Schmiedebergs Arch Pharmacol 329 108 116
39. M-L Wadenberg A Soliman SC VanderSpek S Kapur 2001 Dopamine D2 receptor occupancy is a common mechanism underlying animal models of antipsychotics and their clinical effects Neuropsychopharmacology 25 633 641
40. N Waters K Svensson SR Haadsma-Svensson MW Smith A Carlsson 1993 The dopamine D3 receptor: a postsynaptic receptor inhibitory on rat locomotor activity J Neural Transm Gen Sect 94 11 19
41. DM Weiner HY Meltzer I Veinbergs EM Donohue TA Spalding TT Smith N Mohell SC Harvey J Lameh N Nash KE Vanover R Olsson K Jayathilake M Lee AI Levey U Hacksell ES Burstein RE Davis MR Brann 2004 The role of M1 muscarinic receptor agonism of N-desmethylclozapine in the unique clinical effects of clozapine Psychopharmacology (Berl) 177 207 216