Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors

Journal of Medicinal Chemistry

Volumn 46, Issue 18, 2003, Pages 3930-3937

  Khorana, Nantaka ^a   Smith, Carol ^b   Herrick Davis, Kathy ^b   Purohit, Anil ^b   Teitler, Milt ^b   Grella, Brian ^a   Dukat, Małgorzata ^a   Glennon, Richard A ^a  

^a VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

^b ALBANY MEDICAL COLLEGE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,2,3,4 TETRAHYDRO GAMMA CARBOLINE; 5 METHYL 5H 1,2,3,4 TETRAHYDROPYRIDO[4,3 B]INDOLE (5 METHYL 1,2,3,4 TETRAHYDRO GAMMA CARBOLINE); CARBOLINE DERIVATIVE; SEROTONIN 5A RECEPTOR; TETRAHYDROCARBOLINE; TRYPTOLINE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ANIMALS; BINDING, COMPETITIVE; CARBOLINES; CELL LINE; HUMANS; MICE; RADIOLIGAND ASSAY; RATS; RECEPTORS, SEROTONIN; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0042921555     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm030080s     Document Type: Article

References (26)

1. Glennon, R. A.; Dukat, M. Serotonin receptors and drugs affecting serotonergic neurotransmission. In Foye's Principles of Medicinal Chemistry; Williams, D. A., Lemke, T. M., Eds., Lippincott Williams & Wilkins, Philadelphia, 2002; pp 315-337.
2. Hoyer, D.; Hannon, J. P.; Martin, G. R. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol. Biochem. Behav. 2002, 71, 533-554.
3. Humphrey, P. P. A.; Hartig, P. R.; Hoyer, D. A new nomenclature for 5-HT receptors. Trends Pharmacol. Sci. 1993, 14, 233-236.
4. Barnes, N. M.; Sharp, T. A review of central 5-HT receptors and their function. Neuropharmacology 1999, 38, 1083-1152.
5. 1D family. EMBO J. 1992, 11, 4779-4786.
6. 5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization. Mol. Pharmacol. 1993, 43, 313-319.
7. Erlander, M. G.; Lovenberg, T. W.; Baron, B. M.; deLeccea, L.; Danielson, P. E.; Racke, M.; Slone, A. L.; Siegel, B. W.; Foye, P. E.; Cannon, K.; Burns, J. E.; Sutcliffe, J. G. Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 3452-3456.
8. 5B receptor. FEBS Lett. 1993, 333, 25-31.
9. 5A serotonin receptor. FEBS Lett. 1994, 355, 242-246.
10. 5B receptor was lost during mammalian evolution. Eur. J. Pharmacol. 2001, 418, 157-167.
11. 5A receptors stably expressed in C6 glioma cells couple to multiple signal transduction pathways. J. Neurochem. 2003, 84, 222-232.
12. 5A gene in depression, psychosis and antipsychotic response. Neuroreport 2000, 11, 2017-2020.
13. 5A receptor gene in patients with bipolar disorder and major depression. Neurosci. Lett. 2001, 303, 111-114.
14. 5A receptor. Neuron 1999, 22, 581-591.
15. 5A serotonin receptor is expressed predominantly by astrocytes in which it inhibits cAMP accumulation: A mechanism for neuronal suppression of reactive astrocytes. Glia 1996, 17, 317-326.
16. 5A serotonin receptor binding: A preliminary structure-affinity investigation. Med. Chem. Res. 1997, 7, 207-218.
17. 5A serotonin receptors. Bioorg. Med. Chem. 2003, 11, 717-722.
18. 2) and benzodiazepine receptors. Drug Alcohol Depend. 2000, 60, 121-132.
19. 1C-selective antagonist. J. Med. Chem. 1993, 36, 2519-2525.
20. 1 melatonin receptor partial agonists, antagonists, putative inverse agonists. J. Med. Chem. 1998, 41, 3624-3634.
21. Clitheroe, A.; Green, D.; Jansen, A. B. A.; Phillips, P. C.; Rule, A. W. Nitroethylenes and related compounds as trichomonacides and candidacides. J. Pharm. Pharmacol. 1965, 17, 167-172.
22. Herz, W.; Tocker, S. Pyrrolo[3,2-c]pyridines. J. Am. Chem. Soc. 1955, 77, 6353-6355.
23. Marvell, E. N.; Sturmer, D.; Rowell, C. Bicyclo[3.3.1]nonanes. A new synthesis of 2-bicyclo[3.3.1]nonanone. Tetrahedron 1966, 22, 861-866.
24. Vigroux, A.; Bergon, M.; Zedde, C. Cyclization-activated pro-drugs: N-(Substituted 2-hydroxyphenyl and 2-hydroxypropyl)-carbamates based on ring-opened derivatives of active benzoxazolones and oxazolidinones as mutual prodrugs of acetaminophen. J. Med. Chem. 1995, 38, 3983-3994.
25. 2 serotonin receptors. Bioorg. Med. Chem. Lett. 2002, 12, 155-158.
26. i) and the concentration of inhibitor which causes 50% inhibition (IC50) of an enzyme reaction. Biochem. Pharmacol. 1973, 22, 3099-3108.