S 16924 ((r)-2-{1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-yloxy)-ethyl]-fyrrolidin-3yl}-1-(4-Fluoro-Phenyl)-Ethanone), a Novel, Potential Antipsychotic with Marked Serotonin (5-HT)1A Agonist Properties: II. Functional Profile in Comparison to Clozapine and Haloperidol

Journal of Pharmacology and Experimental Therapeutics

Volumn 286, Issue 3, 1998, Pages 1356-1373

  Millan, Mark J ^a   Schreiber, Rudy ^a   Dekeyne, Anne ^a   Rivet, Jean Michel ^a   Bervoets, Karin ^a   Mavridis, Michaelis ^a   Sebban, Claude ^a   Maurel Remy, Sophie ^a   Newman Tancredi, Adrian ^a   Spedding, Michael ^a   Muller, Oliver ^a   Lavielle, Gilbert ^a   Brocco, Mauricette ^a  

^a INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

Author keywords

[No Author keywords available]

Indexed keywords

2 [1 [2 [2,3 DIHYDROBENZO[1,4]DIOXIN 5 YLOXY]ETHYL]PYRROLIDIN 3 YL] 1 (4 FLUOROPHENYL)ETHANONE; 2,3,4,5 TETRAHYDRO 7,8 DIHYDROXY 1 PHENYL 1H 3 BENZAZEPINE; 4 IODO 2,5 DIMETHOXYAMPHETAMINE; ALPHA [1 [2 (1,4 BENZODIOXAN 5 YLOXY)ETHYL] 3 PYRROLIDINYL] 4 FLUOROACETOPHENONE; AMPHETAMINE; APOMORPHINE; CLOZAPINE; COCAINE; DIZOCILPINE; DOPAMINE; DOPAMINE 1 RECEPTOR STIMULATING AGENT; DOPAMINE 2 RECEPTOR STIMULATING AGENT; DOPAMINE RECEPTOR; ECOPIPAM; HALOPERIDOL; HISTAMINE RECEPTOR; METHYLPHENIDATE; MUSCARINIC RECEPTOR; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; PHENCYCLIDINE; PROLACTIN; PYRROLIDINE DERIVATIVE; QUINPIROLE; SEROTONIN; SEROTONIN 1A ANTAGONIST; SEROTONIN 1A RECEPTOR; UNCLASSIFIED DRUG; 4-IODO-2,5-DIMETHOXYPHENYLISOPROPYLAMINE; AMPHETAMINE DERIVATIVE; NEUROLEPTIC AGENT; SEROTONIN 1 RECEPTOR; SEROTONIN AGONIST; SEROTONIN RECEPTOR;

ANIMAL MODEL; ARTICLE; AVOIDANCE BEHAVIOR; CATALEPSY; COGNITION; DOPAMINERGIC TRANSMISSION; DOSE RESPONSE; DRUG DISCRIMINATION; DRUG RECEPTOR BINDING; ELECTROENCEPHALOGRAM; EXTRAPYRAMIDAL SYMPTOM; GNAWING; HEAD TWITCH; LATENT INHIBITION; LOCOMOTION; MALE; NONHUMAN; PALLIATIVE THERAPY; PRIORITY JOURNAL; PROLACTIN BLOOD LEVEL; RAT; SCHIZOPHRENIA; SEROTONINERGIC TRANSMISSION; ANIMAL; ATTENTION; BLOOD; COMPARATIVE STUDY; DISCRIMINATION LEARNING; DRUG EFFECT; ELECTROENCEPHALOGRAPHY; HUMAN; INSTITUTE FOR CANCER RESEARCH MOUSE; METABOLISM; MOTOR ACTIVITY; MOUSE; WISTAR RAT;

AMPHETAMINES; ANIMALS; ANTIPSYCHOTIC AGENTS; ATTENTION; CLOZAPINE; COGNITION; DISCRIMINATION LEARNING; ELECTROENCEPHALOGRAPHY; HALOPERIDOL; HUMANS; MALE; MICE; MICE, INBRED ICR; MOTOR ACTIVITY; PROLACTIN; PYRROLIDINES; RATS; RATS, WISTAR; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN AGONISTS;

EID: 0032466835     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (80)

1. Andersen HL and Kilpatrick 1C (1996) Prevention by (±)-8-hydroxy-2-(di-npropylamino) tetralin of both catalepsy and the rises in rat striatal dopamme metabolism caused by haloperidol. Br J Pharmacol 118:421-427.
2. Andreasen NC, Rezai K, Alliger R, Swayze VW, Flaum M, Kirchner P, Cohen G and O'Leary D (1992) Hypofrontality in neuroleptic-naive patients and in patients with chronic schizophrenia. Arch Gen Psychiatry 49:943-958.
3. Bakshi VP and Geyer MA (1997) Phencyclidine-induced deficits in prepulse inhibition of startle are blocked by prazosin, an alpha-1 noradrenergic antagonist. J Pharmacol Exp Ther 283:665-674.
4. Bartha R, Williamson PC, Drost DJ, Malla A, Carr TJ, Cortese L, Canaran G, Rylutt RJ and Neufeld WJ (1997) Measurement of glutamate and glutamine in the medial prefrontal cortex of never-treated schizophrenic patients and healthy controls by proton magnetic resonance spectroscopy. Arch Gen Psychiatry 54:959-965.
5. 1A Receptors are not involved in clozapine's lack of cataleptogenic potential. Neuropharmacology 35:1645-1646.
6. Blanc G, Trovero F, Vezina P, Hervé D, Godeheu AM, Glowinski J and Tassin JP (1994) Blockade of prefronto-cortical aradrenergic receptors prevents locomotor hyperactvity induced by subcortical D-amphetamine injection. Eur J Neuroscl 6:293-298.
7. Broersen LM, Heinsbroek RPW, De Bruin JPC and Berend O (1996) Effects of local application of dopaminergic drugs into the medial prefrontal cortex of rats on latent inhibition. Biol Psychiatry 40:1093-1090.
8. Brunello N, Masotto C, Steardo L, Markstein R and Racagni G (1995) New insights into the biology of schizophrenia through the mechanism of action of clozapine. Neuropsychopharmacology 13:177-213.
9. 2A receptor mRNAs and binding site densities are differentially altered in schizophrenia. Neuropsychopharmacology 15:442-455.
10. Carey J and Bergman J (1997) Discriminative-stimulus effects of clozapine in squirrel monkeys: Comparison with conventional and novel antipsychotic drugs. Psychopharmacology 132:261-269.
11. Cunningham-Owens DC (1996) Adverse effects of antipsychotic agents. Do newer agents offer advantages? Drugs 51:895-930.
12. Dekeyne A, Brocco M, Schreiber R, Gressier H, De Ladonchamps B and Millan MJ (1997) Anxiolytic profile of S 16924, a novel antipsychotic possessing marked serotonin (5-HT)1A receptor agonist properties. Behav Pharmacol 8:645.
13. Delfs JM, Schreiber L and Kelley AE (1990) Microinjection of cocaine into the nucleus accumbens elicits locomotor activation in the rat. J Neurosci 10:303-310.
14. Evenden JL (1992) Effects of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) after repeated administration on a conditioned avoidance response (CAR) in the rat. Psychopharmacology 109:134-144.
15. Evins AE, Amico ET, Shih V and Goff DC (1997) Clozapine treatment increases serum glutamate and aspartate compared to conventional neuroleptics. J Neural Transm 104:761-766.
16. Geaney D (1995) Clozapine can cause hallucinations by inducing complex partial seizures of temporal lobe origin (temporal lobe epilepsy). A potentially serious complication in the management of schizophrenia with clozapine. J Neural Transm 9:64-66.
17. Goldberg TE and Gold JM (1995) Neurocognitive functioning in patients with schizophrenia, in Psychopharmacology: The Fourth Generation of Progress (Bloom FE and Kupfer DJ eds) pp 1245-1257, Raven Press Ltd., New York.
18. Gorelick DA and Balster RL (1995) Phencyclidine (PCP, in Psychopharmacology: The Fourth Generation of Progress (Bloom FE and Kupfer DJ eds) pp 1767-1776 Raven Press Ltd., New York.
19. Gray NS, Jeffrey A, Joseph MH, Hemsley DR, Young AMJ, Warburton EC, Boulenguez P, Grigoryan GA, Peters SL, Rawlins JNP, Taib CT, Yee BK, Cassaday H, Weiner I, Gal G, Gusak O, Joel D, Shadach E, Shalev U, Tarrasch R and Feldon J (1995) The role of mesolimbic dopaminergic and retrohippocampal afférents to the
20. nucleus accumbens in latent inhibition: implications for schizophrenia. Behai Brain Res 71:19-31.
21. Gurevich EV and Joyce JN ( 1997) Alterations in the cortical serotonergic system in schizophrenia: a postmortem study. Biol Psychiatry 54:225-232.
22. 2 dopamine receptors. Br J Pharmacol 121:731-736.
23. 2 agonist DOI: Effects of MDL 100,907, clozapine risperidone and haloperidol. Behav Brain Res 88:43-49.
24. 2 receptors. J Pharmacol Exp Ther 263:276-284.
25. Hoffinan DC and Donovan H (1995) Catalepsy as a rodent model for detecting antipsychotk drugs with extrapyramidal side effect liability. Psychopharmacology 120:128-133.
26. Invernizzi RW, Cervo L and Samanin R (1988) 8-Hydroxy-2-(di-rc-propylamino) tetralin a selective serotonin1A receptor agonist, blocks haloperidol-induced catalepsy by an action of raphe nuclei medianus and dorsalis. Neuropharmacology 27:515-518.
27. Jackson DM, Johansson C, Lindgren LM and Bengtsson A ( 1994) Dopamine receptoi antagonists block amphetamine and phencyclidine-induced motor stimulation ir rats. Pharmacol Biochem Behav 48:465-471.
28. Jones-Humble SA, Durcan MJ, Lyerly D, Norton RM, Tang FLM, Russell AV Watson MJ, Gengo PJ, Morgan PF, Wang CM, Cooper BR and Cox RF (1996; Preclinical neurochemical and electrophysiological profile of 1192U90, a potential antipsychotic. Neuropsychopharrnacology 15:217-230.
29. Josselin SA, Miller R and Beninger RJ (1997) Behavioural effects of clozapine and dopamine receptor subtypes. Neurosci Biobehav Rev 21:531-558.
30. Kahn RS and Davis KL (1995) New developments in dopamine and schizophrenia, in Psychopharmacology: The Fourth Generation of Progress (Bloom FE and Kupfei DJ eds) pp 1215-1228, Raven Press, Ltd., New York.
31. Kalkman KO, Neumann V and Tricklebank MD ( 1997) Clozapine inhibits catalepsy induced by olanzapine and loxapine, but prolongs catalepsy induced by SCH 2339C in rats. Naunyn-Schmiedeberg Arch Pharmacoi 355:361-364.
32. Kane JM and Freeman HL (1994) Towards more effective antipsychotic treatment Br J Pharmacol 165:22-31.
33. Kato T, Hirose A, Ohno Y, Shimizu H, Tanaka H and Nakamura M (1990) Binding profile of SM-9018, a novel antipsychotic candidate. Jpn J Pharmacol 54:478-489
34. 2A antagonist with a favorable CNS safety profile. J Pharmacol Exp Ther 277:968-981.
35. Keks NA (1996) Minimizing the non-extrapyramidal side-effects of antipsychotics Acta Psychiatry Scand 94:18-24
36. 2 receptor antagonists to inhibit methylphenidate-induced behaviors in rats. Eur J Pharmacol 313:25-34.
37. Knable MB and Weinberger DR (1997) Dopamine, the prefrontal cortex and schizophrenia. J Psychopharmacol 11:123-131.
38. Lieberman JA, Saltz BL, Johns CA, Pollack S, Borenstein M and Kane J (1991) The effects of clozapine on tardive dyskinesia. Br J Pharmacol 158:503-510.
39. Liu ZC and Uetrecht JP (1995) Clozapine is oxidized by activated human neutrophik to a reactive nitrenium ion that irreversibly binds to the cells. J Pharmacol Exp Ther 275:1476-1483.
40. 2A/Cantagonist, reverse haloperidol-induced catalepsy in rats independently of striatal dopamine release Psychopharmacology 131:57-63.
41. Malhotra AK, Adler CM, Kennison SD, Elman I, Pickar D and Breier A (1997 Clozapine blunts N-methyl-D-aspartate antagonist-induced psychosis: a study with ketamine. Biol Psychiatry 42:664-668.
42. Martin P, Svensson A, Carlsson A and Carlsson ML (1994) On the roles of dopamine D-l vs D-2 receptors for the hyperactivity response elicited by MK-801. J Neurai Transm 95:113-121.
43. Martin P, Waters N, Waters S, Carlsson A and Carlsson ML (1997) MK-801-induced hyperlocomotion: differential effects of MDL 100,907, SDZ PSD 958 and raclo pride. Eur J Pharmacol 335:107-116.
44. Mathe JM, Nomikos GG, Hildebrand BE, Hertel P and Svensson TH (1996) Prazosir inhibits MK-801-induced hyperlocomotion and dopamine release in the nucleus accumbens. Eur J Pharmacol 309:1-11.
45. 2A receptors Br J Pharmacol 114:]54P.
46. Maurel-Remy S, Bervoets K and Millan MJ (1995b) Blockade of phencyclidine induced hyperlocomotion by clozapine and MDL 100,907 in rats reflects antago nism of 5-HT2A receptors. Eur J Pharmacol 280:R9-R11.
47. McCormick DA and Pape HC (1990) Noredrenergic and serotonergic modulation of £ hyperpolarization-activated cation current in thalamic relay neurones. J Physiol ogy 431:319-342.
48. Meltzer HY (1995) Atypical antipsychotic drugs, \nPsychopharmacology: The Fourth Generation of Progress (Bloom FE and Kupfer DJ eds) pp 1277-1286, Raven Press Ltd., New York.
49. 1C/2 antagonists as therapeutic agents. Drug Newi Perspect 5:397-406.
50. 3 receptor activation in the rat in vivo ant their modulation by the selective antagonist, ( + )-S 14297:1. Activation of postsyn
51. 2 receptors elicits prolactin secretion and catalepsy. J Pharmacol Exp Ther 275:885-898.
52. 1A receptors in vivo. J Pharmacol Exp Ther 273:1418-1427.
53. 1A receptor agonists in the spontaneous tail-flick paradigm. J Pharmacol Exp Ther 269:121-131.
54. Moore S and Kenyon P (1994) Atypical antipsychotics, clozapine and sulpiride, do not antagonise amphetamine-induced stereotyped locomotion. Psychopharmacology 114:123-130.
55. Moran PM, Fischer TR, Hitchcock JM and Moser PC (1996) Effects of clozapine on latent inhibition in the rat. Behav Pharmacol 7:42-48.
56. 3 antagonist, facilitates latent inhibition in the rat. Pharmacol Biochem Behav 42:519-522.
57. Moser PC and Moran PM (1994) Effect of the 5-HT2 antagonist MDL 100,907 on latent inhibition in the rat. Behav Pharmacol 5:120-121.
58. Narayanan S, Willins D, Dalia A, Wallace L and Uretsky N (1996) Role of dopaminergic mechanisms in the stimulatory effects of MK-801 injected into the ventral tegmental area and the nucleus accumbens. Pharmacol Biochem Behav 54:565-573.
59. Nielsen EB (1988) Cholinergic mediation of the discriminative stimulus properties of clozapine. Psychopharmacology 94:115-118.
60. 2 receptor is antagonized by R(-)-n-propylnorapomorphine, raclopride and phenoxybenzamine. Neuropsychopharmacology 15:54-61.
61. Olianas MC, Maullu C and Onali P (1997) Effects of clozapine on rat striatal muscarinic receptors coupled to inhibition of adenylyl cyclase activity and on the human cloned m4 receptor. Br J Pharmacol 122:401-408.
62. Pickar D (1995) Prospects for pharmacotherapy of schizophrenia. Lancet 1:557-558.
63. 3H]NGD 94-1. J Pharmacol Exp Ther 282:1020-1027.
64. Prinssen EPM, Eilenbrock BA and Cools AR (1994) Combined antagonism of adrenoceptors and dopamine and 5-HT receptors underlies the atypical profile of clozapine. Eur J Pharmacol 262:167-170.
65. Ruob C, Eisner J, Weiner I and Feldon J (1997) Amphetamine-induced disruption and haloperidol-induced potentation of latent inhibition depend on the nature of the stimulus. Behav Brain Res 88:35-41.
66. Roth BL and Meltzer HY (1995) The role of serotonin in schizophrenia, in Psychopharmacology: The Fourth Generation of Progress (Bloom FE and Kupfer DJ eds) pp 1215-1228, Raven Press, Ltd., New York.
67. 1A receptor ligands in animal models of anxiety, impulsivity and depression: multiple mechanisms of actions? Prog. NeuroPsychopharmacol Biol Psychiat 17:87-104.
68. 2A/2C antagonists, Dj antagonists and 5-HT,A agonists. J Pharmacol Exp Ther 273:101-112.
69. Schreiber R, Brocco M and Millan MJ (1994) Blockade of the discriminative stimulus effects of DOT by MDL 100,907 and the 'atypical' antipsychotics, clozapine and risperidone. Eur J Pharmacol 264:99-102.
70. Seeger TF, Seymour PA, Schmidt AW, Zorn SH, Schulz DW, Lebel LA, McLean S, Guanowsky V, Howard HR, Löwe JA and Heym J (1995) Ziprasidone (CP-88,059): A new antipsychotic with combined dopamine and serotonin receptor antagonist activity. J Pharmacol Exp Ther 275:101-113.
71. Shvaloff A, Tesolin B and Sebban C (1988) Effects of apomorphine in quantified electroencephalography in the frontal cortex: changes with dose and time. Neu.ropharmacology 27:1313-1317.
72. Steinpreis RE (1996) The behavioral and neurochemical effects of phencyclidine in humans and animals: some implications for modeling psychosis. Behav Brain Res 74:45-55.
73. 2 receptor and aradrenoceptor antagonism. J Clin Psychopharmacol 15:11S-18S.
74. Tricklebank MD (1985) The behavioural response to 5-HT receptor agonists and subtypes of the central 5-HT receptor. Trends Pharmacol Sei 5:403-407, 1985.
75. Wadenberg ML (1996) Serotonergic mechanisms in neuroleptic-induced catalepsy in the rat. Neurosci Biobehav Rev 20:325-339.
76. Weiner I and Feldon J (1997) The switching model of latent inhibition: an update of neural substrates. Behav Brain Res 88:11-25.
77. Willins DL and Meltzer HY (1997) Direct injection of 5-HT2A receptor agonists into the medial prefrontal cortex produces a head-twitch response in rats. J Pharmacol Exp Ther 282:699-706.
78. Wirsching WC, Marder SR, Van Putten T and Ames D (1995) Acute treatment of schizophrenia, in Psychopharmacology: The Fourth Generation of Progress (Bloom FE and Kupfer DJ eds) pp 1259-1266, Raven Press, Ltd., New York.
79. 4 receptor agonist. Eur J Pharmacol 269:R1-R2.
80. Send reprint requests to: Dr Mark J. Millan, Institut de Recherches Servier, Centre de Recherches de Croissy, Psychopharmacology Department, 125 Chemin de Ronde, 78290 - Croissy-sur-Seine, Paris, France.