Biochemical profile of YM992, a novel selective serotonin reuptake inhibitor with 5-HT(2A) receptor antagonistic activity

Neuropharmacology

Volumn 35, Issue 11, 1996, Pages 1621-1626

  Hatanaka, K ^a   Nomura, T ^a   Hidaka, K ^a   Takeuchi, H ^a   Yatsugi, S ^a   Fujii, M ^a   Yamaguchi, T ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

5 HT(2A) receptor antagonist; Antidepressant; Selective serotonin reuptake inhibitor (SSRI); Serotonin (5 HT); YM992

Indexed keywords

1 METHYL 3 INDOLECARBOXYLIC ACID [1 [2 (METHYLSULFONYLAMINO)ETHYL] 4 PIPERIDINYLMETHYL] ESTER; 2 (2 METHOXY 1,4 BENZODIOXAN 2 YL) 2 IMIDAZOLINE; 2 [[(7 FLUORO 4 INDANYL)OXY]METHYL]MORPHOLINE; 2 DIPROPYLAMINO 8 HYDROXYTETRALIN; 3 (5 METHYL 1H IMIDAZOL 4 YL) 1 (1 METHYL 1H INDOL 3 YL) 1 PROPANONE; ADENOSINE DIPHOSPHATE; AMITRIPTYLINE; ANTIDEPRESSANT AGENT; CITALOPRAM; DIHYDROALPRENOLOL; DOPAMINE; FLUOXETINE; FLUPENTIXOL; GR 13808; KETANSERIN; MEPYRAMINE; MESULERGINE; METERGOLINE; NORADRENALIN; PIRENZEPINE; PRAZOSIN; QUINUCLIDINYL BENZILATE; RADIOLIGAND; RESLIN; RITANSERIN; SEROTONIN; SEROTONIN 1C RECEPTOR; SEROTONIN 2A ANTAGONIST; SEROTONIN 2A RECEPTOR; SEROTONIN UPTAKE INHIBITOR; TRAZODONE; TROPISETRON; UNCLASSIFIED DRUG; UNINDEXED DRUG;

AMINO ACID TRANSPORT; ANIMAL TISSUE; ARTICLE; BRAIN CORTEX; CATECHOLAMINE UPTAKE; CONTROLLED STUDY; CORPUS STRIATUM; DEPRESSION; DOPAMINE UPTAKE; DRUG ANTAGONISM; HUMAN; HUMAN CELL; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; RECEPTOR BINDING; SEROTONIN UPTAKE; SEROTONINERGIC TRANSMISSION; THROMBOCYTE AGGREGATION;

ANIMALS; ANTIDEPRESSIVE AGENTS; BIOGENIC MONOAMINES; HUMANS; MALE; MORPHOLINES; PLATELET AGGREGATION; PLATELET AGGREGATION INHIBITORS; RATS; RATS, WISTAR; RECEPTORS, NEUROTRANSMITTER; RECEPTORS, SEROTONIN; SEROTONIN ANTAGONISTS; SEROTONIN UPTAKE INHIBITORS; SYNAPTOSOMES;

EID: 0030445797     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(96)00079-2     Document Type: Article

References (31)

1. Åsberg M., Thoren P., Traskman L., Bertilisson L. and Ringberger V. (1976) "Serotonin depression" - a biochemical subgroup within the affective disorders? Science 191: 478-480.
2. 2A receptors in the rat medial prefrontal cortex: an iontophoretic study. Synapse 17: 173-181.
3. 1A receptors. Br. J Pharmacol. 100: 793-799.
4. Blier P. and De Montigny C. (1994) Current advances and trends in the treatment of depression. Trends Pharmac. Sci. 15: 220-226.
5. 2 receptor function: hypothesis for a faster antidepressant action. Pharmacol. Res. 30: 1-11.
6. Cheng Y. C. and Prussoff W. H. (1973) Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50% inhibition of an enzymatic reaction. Biochem. Pharmacol 22: 3099-3108.
7. 3H]imipramine. J Pharmacol. Exp. Ther. 242: 364-371.
8. 1-receptor density in brain. Eur. J. Pharmacol. 87: 497-498.
9. 2-receptor antagonist. Agents Act. 12: 388-397.
10. 2 receptor sites on human blood platelets. Biochem. Pharmacol. 33: 2807-2811.
11. Edwards J. G. (1995) Drug choice in depression. Selective serotonin reuptake inhibitors or tricyclic antidepressants?. CNS Drugs 4: 141-159.
12. Ehlert F. J. (1988) Gallamine allosterically antagonizes muscarinic receptor-mediated inhibition of adenylate cyclase activity in the rat myocardium. J. Pharmacol. Exp. Ther. 247: 596-602.
13. Fuller R. W. (1994) Uptake inhibitors increase extracellular serotonin concentration measured by brain microdialysis. Life Sci. 55: 163-167.
14. 4 receptors in guinea-pig and rat brain. Br. J. Pharmacol. 109: 618-624.
15. Harada M. and Maeno H. (1979) Biochemical characteristics of a potential antidepressant, 2-(7-indenyloxymethyl)morpholine hydrochloride (YM-08054-1). Biochem. Pharmacol. 28: 2645-2651.
16. 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes. J. Neurosci. 7: 894-903.
17. 3 receptor antagonist, in rabbit nodose ganglion and N1E-115 neuroblastoma cells. J. Pharmacol. Exp. Ther. 263: 1127-1132.
18. Leonard B. E. (1995) Mechanisms of action of antidepressants. CNS Drugs 4: 1-12.
19. 2 receptor binding sites. Molec. Pharmacol. 21: 301-314.
20. Marek G. J., McDougle C. J., Price L. H. and Seiden L. S. (1992) A comparison of trazodone and fluoxetine: implications for a serotonergic mechanism of antidepressant action. Psycopharmacology 109: 2-11.
21. 2 receptor antagonists-LY53857, sergolexole, and LY237733. Life Sci. 47: 2089-2095.
22. 2-adrenergic drugs also bind with high affinity to a noradrenergic site. Molec. Pharmacol. 35: 324-330.
23. Pazos A., Hoyer D. and Palacios J. M. (1985) The binding of serotonergic ligands to the porcine choroid plexus: characterization of a new type of serotonin recognition site. Eur. J. Pharmacol. 106: 539-546.
24. 1C binding sites in rat frontal cortex. J. Neurochem. 47: 529-540.
25. Potter L. T., Ferrendelli C. A. and Hanchett H. E. (1988) Two affinity states of M1 muscarine receptors. Cell. Molec. Neurobiol. 8: 181-191.
26. Sugrue M. F. (1983) Chronic antidepressant therapy and associated changes in central monoaminergic receptor functioning. Pharmacol. Ther. 21: 1-33.
27. Terai M., Usuda M., Kuroiwa I., Noshiro O. and Maeno H. (1983) Selective binding of YM-09151-2, a new potent neuroleptic, to D2-dopaminergic receptors. Jap. J. Pharmacol. 33: 749.
28. 3H]raclopride for dopamine D-2 receptor binding to rat striatum. Eur. J. Pharmacol. 173: 177-182.
29. Yamaguchi T., Yatsugi S., Takeuchi H. and Fujii M. (1994) Biochemical studies of YM-35992-A novel antidepressant. Soc. Neurosci. Abstr. 20: 1776.
30. Yamaguchi T., Hatanaka K., Nomura T., Takeuchi H., Fujii M. and Yatsugi S. (1995) Biochemical studies of YM992: a novel selective serotonin re-uptake inhibitor. Soc. Neurosci. Abstr. 21: 1737.
31. 2 antagonistic activity. Soc. Neurosci. Abstr. 20: 1776.