Radiolabelling of the human 5-HT2A receptor with an agonist, a partial agonist and an antagonist: Effects on apparent agonist affinities

Biochemical Pharmacology

Volumn 51, Issue 1, 1996, Pages 71-76

  Sleight, Andrew J ^a   Stam, Nico J ^b   Mutel, Vincent ^a   Vanderheyden, Patrick M L ^b  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b NV ORGANON   (Netherlands)

Author keywords

5 HT2A; Agonist binding; Receptor; 3H 5 HT; 3H DOB; 3H ketanserin

Indexed keywords

(3 CHLOROPHENYL)PIPERAZINE; 1 (2,5 DIMETHOXY 4 BROMOPHENYL) 2 AMINOPROPANE KETANSERIN; 4 IODO 2,5 DIMETHOXYAMPHETAMINE; GUANOSINE TRIPHOSPHATE DERIVATIVE; GUANYLYLIMIDODIPHOSPHATE; MESULERGINE; METHYSERGIDE; PARTIAL AGONIST; QUIPAZINE; RADIOLIGAND; SEROTONIN; SEROTONIN 2A AGONIST; SEROTONIN 2A ANTAGONIST; SEROTONIN 2A RECEPTOR; SPIPERONE; UNCLASSIFIED DRUG;

AGONIST; ANIMAL CELL; ARTICLE; BINDING COMPETITION; CELL STRAIN 3T3; CONTROLLED STUDY; DRUG ACTIVITY; DRUG RECEPTOR BINDING; GENE EXPRESSION; HUMAN; MOUSE; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY; RECEPTOR INTRINSIC ACTIVITY;

2,5-DIMETHOXY-4-METHYLAMPHETAMINE; 3T3 CELLS; ANIMALS; BINDING, COMPETITIVE; CELL MEMBRANE; HUMANS; KETANSERIN; MICE; RADIOLIGAND ASSAY; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS;

EID: 0029670995     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/0006-2952(95)02122-1     Document Type: Article

References (23)

1. Boess FG and Martin IL, Molecular biology of 5-HT receptors. Neuropharmacol 133: 275-317, 1994.
2. Gaddum JH and Picarelli ZP, Two kinds of tryptamine receptor. Br J Pharmacol Chemother 12: 323-328, 1957.
3. 3H]spiperone. Mol Pharmacol 16: 687-699, 1979.
4. Humphrey PPA, Hartig P and Hoyer D, A proposed new nomenclature for 5-HT receptors. Trends Pharmacol Sci 14: 233-236, 1993.
5. Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR and Humphrey PPA, International union of pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol Rev 46: 157-204, 1994.
6. 2 serotonin receptors. Eur J Pharmacol 117: 145-146, 1985.
7. 2 receptor subtypes. Mol Pharmacol 38: 594-598, 1990.
8. 3H]-ketanserin. J Neurosci 9: 3482-3490, 1989.
9. 1A receptor genes. Eur J Pharmacol Mol Pharmacol Section 227: 153-162, 1992.
10. McPherson GA, KINETIC, EBDA, LIGAND, LOWRY: A Collection of Radioligand Binding Analysis Programmes, p. 23, Biosoft, Cambridge, 1985.
11. Munson PJ and Rodbard D, LIGAND: a versatile computerized approach for characterisation of ligand-binding systems. Anal Biochem 107: 220-239, 1980.
12. 2 receptor-mediated phosphatidylinositol turnover by d-lysergic acid diethylamide. J Pharmacol Exp Ther 247: 918-925, 1988.
13. 2 binding site in rat cerebral cortex but not in subcortical regions. J Pharmacol Exp Ther 234: 195-203, 1985.
14. Conn PJ and Sanders-Bush E, Selective 5HT-2 antagonists inhibit serotonin stimulated phosphatidylinositol metabolism in cerebral cortex. Neuropharmacol 23: 993-996, 1984.
15. Conn PJ and Sanders-Bush E, Regulation of serotonin-stimulated phosphoinositide hydrolysis: relation to the serotonin 5-HT-2 binding site. J Neurosci 6: 3669-3675, 1986.
16. 2 receptor sites. J Biol Chemistry 260: 7603-7608, 1985.
17. 3H]ketanserin. Eur J Pharmacol 118: 13-23, 1985.
18. 2 receptors. Mol Pharmacol 43: 755-761, 1993.
19. Johnson MP, Loncharich RJ, Baez M and Nelson DL, Species variation in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines. Mol Pharmacol 45: 277-286, 1994.
20. 2 receptor is not sensitive to GTP analogs. Mol Pharmacol 43: 915-920, 1993.
21. 1C cell line. Brain Res 584: 191-196, 1992.
22. 2 receptors. Mol Phamacol 42: 328-335, 1992.
23. 2C receptor. Eur J Pharmacol Mol Pharmacol Section 269: 339-348, 1994.