SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4- [5-(4-fluoro-phenyl)- pyridin-3-ylmethyl]-piperazine monohydrochloride): A novel dopamine D 2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug

Neuropsychopharmacology

Volumn 32, Issue 1, 2007, Pages 78-94

  McCreary, Andrew C ^a   Glennon, Jeffrey C ^a   Ashby Jr , Charles R ^b   Meltzer, Herbert Y ^c   Li, Zhu ^c   Reinders, Jan Hendrik ^a   Hesselink, Mayke B ^a   Long, Stephen K ^a   Herremans, Arnoud H ^a   Van Stuivenberg, Herman ^a   Feenstra, Rolf W ^a   Kruse, Chris G ^a  

^a Solvay Pharmaceuticals Inc   (Netherlands)

^b ST JOHN'S UNIVERSITY   (United States)

^c VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

5 HT1A; Atypical antipsychotic; D2; Medial prefrontal cortex; Neuroleptic; SLV313

Indexed keywords

1 (2,3 DIHYDRO BENZO[1,4]DIOXIN 5 YL) 4 [5 (4 FLUOROPHENYL)PYRIDIN 3 YLMETHYL]PIPERAZINE; 5 [4 [5 (4 FLUOROPHENYL) 3 PYRIDINYLMETHYL] 1 PIPERAZINYL] 1,4 BENZODIOXAN; ACETYLCHOLINE; ALPHA 1 ADRENERGIC RECEPTOR; ALPHA 2 ADRENERGIC RECEPTOR; APOMORPHINE; CLOZAPINE; DOPAMINE; DOPAMINE 2 RECEPTOR; DOPAMINE 2 RECEPTOR BLOCKING AGENT; DOPAMINE 3 RECEPTOR; DOPAMINE 3 RECEPTOR BLOCKING AGENT; DOPAMINE 4 RECEPTOR; FLESINOXAN; HISTAMINE H1 RECEPTOR; MUSCARINIC M1 RECEPTOR; MUSCARINIC M4 RECEPTOR; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; SEROTONIN; SEROTONIN 1A AGONIST; SEROTONIN 1A ANTAGONIST; SEROTONIN 1A RECEPTOR; SEROTONIN 2A RECEPTOR; SEROTONIN 2B RECEPTOR; SEROTONIN 3 RECEPTOR; SEROTONIN 4 RECEPTOR; SEROTONIN 6 RECEPTOR; SEROTONIN 7 RECEPTOR; SEROTONIN TRANSPORTER;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; ATTENTION DEFICIT DISORDER; CATALEPSY; CHRONIC DRUG ADMINISTRATION; CLIMBING; COGNITIVE DEFECT; DOPAMINE BLOOD LEVEL; DOPAMINERGIC NERVE CELL; DRUG ACTIVITY; DRUG ANTAGONISM; DRUG DISCRIMINATION; DRUG EFFICACY; DRUG POTENTIATION; GUINEA PIG; HIPPOCAMPUS; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MALE; NONHUMAN; NUCLEUS ACCUMBENS; PREFRONTAL CORTEX; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; SCHIZOPHRENIA; SUBSTANTIA NIGRA; VENTRAL TEGMENTUM;

ANALYSIS OF VARIANCE; ANIMALS; ANTIPSYCHOTIC AGENTS; BEHAVIOR, ANIMAL; BINDING, COMPETITIVE; BRAIN CHEMISTRY; CATALEPSY; CHO CELLS; COLUMBIDAE; CRICETINAE; CRICETULUS; DISCRIMINATION (PSYCHOLOGY); DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; HUMANS; MALE; PIPERAZINES; RATS; RATS, WISTAR; RECEPTOR, SEROTONIN, 5-HT1A; RECEPTORS, DOPAMINE D2; SEROTONIN AGONISTS; TRANSFECTION;

EID: 33845707537     PISSN: 0893133X     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.npp.1301098     Document Type: Article

References (91)

1. 1A receptor activation to neurochemical profile of novel antipsychotics: frontocortical dopamine and hippocampal serotonin release in rat brain. J Pharmacol Exp Ther 315: 265-272.
2. 1A receptor in schizophrenia: a promising target for novel atypical neuroleptics? J Psychopharmacol 15: 37-46.
3. 1A receptors induces lower lip retraction in the rat. Pharmacol Biochem Behav 33: 821-827.
4. Bill DJ, Knight M, Forster EA, Fletcher A (1991). Direct evidence for an important species difference in the mechanism of 8-OH-DPAT-induced hypothermia. Br J Pharmacol 103: 1857-1864.
5. 2C receptors. Br J Pharmacol 115: 622-628.
6. 4 receptor antagonist, does not exhibit a neuroleptic-like profile in rodent behavioral tests. J Pharmacol Exp Ther 283: 1256-1263.
7. 4 receptor antagonist. TIPS 18: 186-188.
8. 2 dopamine receptor cDNA. Nature 336: 783-787.
9. 2A receptor mRNAs and binding site densities are differentially altered in schizophrenia. Neuropsychopharmacology 15: 442-555.
10. Casey DE (1996). Extrapyramidal syndromes and new antipsychotic drugs: findings in patients and non-human primate models. Br J Psychiatr 29: 32-39.
11. Chiodo LA (1988). Dopamine-containing neurons in the mammalian central nervous system: electrophysiology and pharmacology. Neurosci Biobehav 12: 49-91.
12. Chiodo LA, Bunney BS (1983). Typical and atypical neuroleptics: Differential effects of chronic administration on the activity of A9 and A10 dopamine neurons. J Neurosci 7: 1607-1619.
13. Christoffersen CL, Meltzer LT (1998). Reversal of haloperidol-induced extrapyramidal side effects in cebus monkeys by 8-hydroxy-2-(di-n-propylamino) tetralin and its enantiomers. Neuropsychopharmacology 18: 399-402.
14. (1A) receptor agonism. Brain Res 1023: 54-63.
15. (1A) receptor agonist. I: Neurochemical and electrophysiological profile. Neuropsychopharmacology 28: 2064-2076.
16. 1A receptor agonist. II: Behavioral profile predictive of an atypical antipsychotic activity. Neuropsychopharmacology 28: 1889-1902.
17. Dini S, Caselli GF, Ferrari MP, Giani R, Clavenna G (1991). Heterogeneity of [3H]-mepyramine binding sites in guinea pig cerebellum and lung. Agents Actions 33: 181-184.
18. Dorje F, Wess J, Lambrecht G, Tackle R, Mutschler E, Brann MR (1991). Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J Pharmacol Exp Ther 256: 727-733.
19. Eichenbaum H, Dudchenko P, Wood E, Shapiro M, Tanila H (1999). The hippocampus, memory, and place cells: is it spatial memory or a memory space? Neuron 23: 209-226.
20. 1A receptor. J Biol Chem 64: 14848-14852.
21. Fernandez G, Klaver P, Fell J, Grunwald T, Elger CE (2002). Human declarative memory formation: segregating rhinal and hippocampal contributions. Hippocampus 12: 514-519.
22. Freeman AS, Bunney BS (1987). Chronic neuroleptic effects on DA neuron activity: a model for predicting therapeutic efficacy and side effects? Psychopharmacol Ser 3: 225-235.
23. Goff DC, Midha KK, Brotman AW, McCormick S, Waites M, Amico ET (1991). An open trial of buspirone added to neuroleptics in schizophrenic patients. J Clin Psychopharmacol 11: 193-197.
24. Goldman-Rakic PS (1998). The cortical dopamine system: role in memory and cognition. Adv Pharmacol 42: 707-711.
25. Grandy DK, Marchionni MA, Makam H, Stofko RE, Alfano M, Frothingham L et al (1989). Cloning of the cDNA and gene for a human D2 DA receptor. Proc Natl Acad Sci USA 86: 9762-9766.
26. 3H-prazosin to rat brain alpha-adrenergic receptors. Eur J Pharmacol 55: 323-326.
27. Gurevich EV, Joyce JN (1997). Alterations in the cortical serotonergic system in schizophrenia: a postmortem study. Biol Psychiatr 42: 529-545.
28. Hartfield AW, Moore NA, Clifton PG (2003). Serotonergic and histaminergic mechanisms involved in intralipid drinking? Pharmacol Biochem Behav 76: 251-258.
29. Harvey PD, Keefe RS (2001). Studies of cognitive change in patients with schizophrenia following novel antipsychotic treatment. Am J Psychiatr 158: 176-184.
30. 2 receptor antagonists. Pharmacol Biochem Behav 64: 389-395.
31. Hertel P, Nomikos GG, Iurlo M, Svensson TH (1996). Risperidone: regional effects in vivo on release and metabolism of dopamine and serotonin in the rat brain. Psychopharmacology (Berlin) 124: 74-86.
32. 3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells. Br J Pharmacol 118: 1237-1245.
33. 2A) receptors minimally contribute to clozapine-induced acetylcholine release in rat medial prefrontal cortex. Brain Res 939: 34-42.
34. Ichikawa J, Dai J, O'Laughlin IA, Fowler WL, Meltzer HY (2002b). Atypical, but not typical, antipsychotic drugs increase cortical acetylcholine release without an effect in the nucleus accumbens or striatum. Neuropsychopharmacology 26: 325-339.
35. (1A) receptor activation: a possible mechanism of atypical antipsychotic-induced cortical dopamine release. J Neurochem 76: 1521-1531.
36. (1A) receptor agonist, potentiated S(-)-sulpiride-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens but not striatum. J Pharmacol Exp Ther 291: 1227-1232.
37. Jones-Humble SA, Durcan MJ, Lyerly D, Norton MS, Tang FLM, Russell AV et al (1996). Preclinical neurochemical and electrophysiological profile of 1192U90, a potential antipsychotic. Neuropsychopharmacology 15: 217-229.
38. 1A receptor. Eur J Pharmacol 441: 137-140.
39. 3 receptor antagonists as therapeutic agents. Drug Discovery Today 10: 917-925.
40. 1A agonist properties: evidence for lowered EPS liability. Soc Neurosci Abstr 33: 956.2.
41. Kuroki T, Meltzer HY, Ichikawa J (1999). Effects of antipsychotic drugs on extracellular dopamine levels in rat medial prefrontal cortex and nucleus accumbens. J Pharmacol Exp Ther 288: 774-781.
42. 1A receptors. Eur J Pharmacol 260: 79-83.
43. Li Z, Ichikawa J, Dai J, Meltzer HY (2004). Aripiprazole, a novel antipsychotic drug, preferentially increases dopamine release in the prefrontal cortex and hippocampus in rat brain. Eur J Pharmacol 493: 75-83.
44. Mackenzie RG, Vanleeuven D, Pugsley TA, Shih Y-H, Demattos S, Tang L et al (1994). Characterization of the human dopamine D3 receptor expressed in transfected cell lines. Eur J Pharmacol 266: 79-85.
45. McCreary AC, Glennon JC, Tuinstra T, Herremans AHJ, Van der Heyden J, Long SK et al (2002). SLV313: a novel antipsychotic with additional antidepressant and anxiolytic-like acitons. Eur Neuropsychopharmacol 12: S274.
46. Meltzer HY (1999). The role of serotonin in antipsychotic drug action. Neuropsychopharmacology 2: 106-115.
47. Meltzer HY, Li Z, Kaneda Y, Ichikawa J (2003). Serotonin receptors: their key role in drugs to treat schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry 27: 1159-1172.
48. Meltzer HY, McGurk SR (1999). The effect of clozapine, risperidone and olanzapine on cognitive function in schizophrenia. Schizophrenia Bull 25: 233-255.
49. (4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells. Br J Pharmacol 131: 827-835.
50. 1A receptors. J Pharmacol Exp Ther 295: 853-861.
51. Moghaddam B, Bunney BS (1990). Acute effects of typical and atypical antipsychotic drugs on the release of dopamine from prefrontal cortex, nucleus accumbens, and striatum of the rat: an in vivo microdialysis study. J Neurochem 54: 1755-1760.
52. Monsma FJ, Shen Y, Ward RP, Hamblin MW, Sibley DR (1993). Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol 43: 320-327.
53. 1A agonist flesinoxan in pigeons. Eur J Pharmacol 325: 145-153.
54. 1A receptor expressed in insect cells activates endogenous G(o)-like G protein(s). J Biol Chem 269: 12954-12962.
55. Nakamura K, Suzuki K, McCreary AC, Ashby Jr CR (2006). The acute and chronic administration of (±)-8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) significantly alters the activity of spontaneously active midbrain dopamine neurons in rats: an in vivo electrophysiological study. Synapse 59: 359-367.
56. Newman-Tancredi A, Assie M-B, Leduc N, Ormiere A-M, Danty N, Cosi C (2004). Novel antipsychotics activate recombinant human and native rat serotinin 5-HT1A receptors: affinity, efficacy and potential implications for the treatment of scizophrenia. Int J Neuropsychopharmacol 8: 1-16.
57. 4.4 receptors: actions of antiparkinsonian and antipsychotic agents. J Pharmacol Exp Ther 282: 181-191.
58. 1A receptors. Neuropharmacology 35: 119-121.
59. 35S]thio)-triphosphate binding and antibody study. Mol Pharmacol 55: 564-574.
60. 3H]WAY100, 635 binding affinity ratios: relationship to efficacy for G-protein activation. Eur J Pharmacol 428: 177-184.
61. Nomikos GG, Iurlo M, Andersson JL, Kimura K, Svensson TH (1994). Systemic administration of amperozide, a new atypical antipsychotic drug, preferentially increases dopamine release in the rat medial prefrontal cortex. Psychopharmacol (Berlin) 115: 147-156.
62. Paxinos G, Watson C (1998). The Rat Brain In Stereotaxic Coordinates. Academic Press: New York.
63. Pehek EA, Meltzer HY, Yamamoto BK (1993). The atypical antipsychotic drug amperozide enhances rat cortical and striatal dopamine efflux. Eur J Pharmacol 240: 107-109.
64. Prinssen EP, Kleven MS, Koek W (1996). Effects of dopamine antagonists in a two-way active avoidance procedure in rats: interactions with 8-OH-DPAT, ritanserin, and prazosin. Psychopharmacology 128: 191-197.
65. (1A) ligands in preclinical behavioral models for antipsychotic and extrapyramidal effects. Psychopharmacology 144: 20-29.
66. 1A behavioural syndrome, but not to its ability to attenuate haloperidol-induced catalepsy. Behav Pharmacol 11: 299-305.
67. 2C receptor gene polymorphism. Lancet 359: 2086-2087.
68. (1A) receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex. Biol Psychiatr 48: 229-237.
69. 1A receptor activation. Eur J Pharmacol 338: R3-R5.
70. Salomon Y, Londos C, Rodbell M (1974). A highly selective adenylate cyclase assay. Analyt Biochem 58: 541-548.
71. Seeman P, Lee T, Chau-Wong M, Wong K (1976). Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature 261: 717-719.
72. Seidman LG, Kremen WS, Koren D, Faraone SV, Goldstein JM, Tsuang MT (2002). A comparative profile analysis of neuropsychological functioning in patients with schizophrenia and bipolar psychoses. Schizophren Res 53: 31-44.
73. 7 serotonin receptor subtype. J Biol Chem268: 18200-18204.
74. Shirazi-Southall S, Rodriguez DE, Nomikos GG (2002). Effects of typical and atypical antipsychotics and receptor selective compounds on acetylcholine efflux in the hippocampus of the rat. Neuropsychopharmacology 26: 583-594.
75. 1A receptor activation. Neuropsychopharmacology 21: 622-631.
76. Sumiyoshi T, Matsui M, Nohara S, Yamashita I, Kurachi M, Sumiyoshi C et al (2001a). Enhancement of cognitive performance in schizophrenia by addition of tandospirone to neuroleptic treatment. Am J Psychiatr 158: 1722-1725.
77. (1A) agonist, on memory function in schizophrenia. Biol Psychiatr 15: 861-868.
78. Tatsumi M, Groshan K, Blakeley RD, Richelson E (1997). Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol 340: 249-258.
79. 1 receptor and of catecholaminergic systems in the behavioral response to 8-hydroxy-2-(di-n-propylamino)-tetralin in the rat. Eur J Pharmacol 106: 271-282.
80. 3H-RX821002 ligand binding. Pharmacol Toxicol 69: 341-350.
81. 4 receptor variants in the human population. Nature 358: 149-152.
82. Wadenberg ML (1996). Serotonergic mechanisms in neuroleptic-induced catalepsy in the rat. Neurosci Biobehav Rev 20: 325-339.
83. Wadenberg ML, Ahlenius S (1991). Antipsychotic-like profile of combined treatment with raclopride and 8-OH-DPAT in the rat: enhancement of antipsychotic-like effects without catalepsy. J Neural Transm 83: 43-53.
84. Wadenberg ML, Young KA, Richter JT, Hicks PB (1999). Effects of local application of 5-hydroxytryptamine into the dorsal or median raphe nuclei on haloperidol-induced catalepsy in the rat. Neuropharmacology 38: 151-156.
85. Weinberger DR, Lipska BK (1995). Cortical maldevelopment, antipsychotic drugs, and schizophrenia: a search for common ground. Schizophren Res 16: 87-110.
86. Weiss S, Sebben M, Bockaert JJ (1985). Corticotropin-peptide regulation of intracellular cyclic AMP production in cortical neurons in primary culture. J Neurochem 45: 869-874.
87. White FJ, Wang RY (1983). Differential effects of classical and atypical antipsychotic drugs on A9 and A10 dopamine neurons. Science 221: 1054-1057.
88. Winstanley CA, Chudasama Y, Dalley JW, Theobald DE, Glennon JC, Robbins TW (2003). Intra-prefrontal 8-OH-DPAT and M100907 improve visuospatial attention and decrease impulsivity on the five-choice serial reaction time task in rats. Psychopharmacology (Berlin) 167: 304-314.
89. 2 receptor activity Schizophren. Research 60(S 1): 119.
90. 1A receptor binding in amygdala of schizophrenia. Biol Psychiatr 55: 439-444.
91. Yoshida K, Sugita T, Higuchi H, Hishikawa Y (1998). Effects of tandospirone on tardive dyskinesia and parkinsonian symptoms. Eur Psychol 13: 421-422.