Ligand dependency of 5-hydroxytryptamine 2C receptor internalization

Journal of Pharmacology and Experimental Therapeutics

Volumn 310, Issue 3, 2004, Pages 865-870

  Schlag, Brian D ^a   Lou, Zhuangwei ^a   Fennell, Myles ^a   Dunlop, John ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(3 CHLOROPHENYL)PIPERAZINE; 1,2,3,5 TETRAHYDRO 5 METHYL 1 (3 PYRIDYLCARBAMOYL)PYRROLO[2,3 F]INDOLE; 2 (6 CHLORO 5 FLUORO 1 INDOLYL) 1 METHYLETHYLAMINE; 5 METHOXYGRAMINE; 6 CHLORO 5 METHYL 1 [[2 [(2 METHYL 3 PYRIDYL)OXY] 5 PYRIDYL]CARBAMOYL]INDOLINE; 8,9 DICHLORO 2,3,4,4A TETRAHYDRO 1H PYRAZINO[1,2 A]QUINOXALIN 5(6H) ONE; CALCIUM ION; G PROTEIN COUPLED RECEPTOR; GREEN FLUORESCENT PROTEIN; LIGAND; SEROTONIN 2C AGONIST; SEROTONIN 2C ANTAGONIST; SEROTONIN 2C RECEPTOR; UNCLASSIFIED DRUG;

ARTICLE; CALCIUM CELL LEVEL; CONCENTRATION RESPONSE; CONFOCAL MICROSCOPY; CONTROLLED STUDY; EMBRYO; FLUORESCENCE; FLUOROMETRY; GENE CONSTRUCT; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; INTERNALIZATION; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN TRANSPORT; RECEPTOR DOWN REGULATION;

CALCIUM; CELLS, CULTURED; ENDOCYTOSIS; GREEN FLUORESCENT PROTEINS; HUMANS; LIGANDS; LUMINESCENT PROTEINS; RECEPTOR, SEROTONIN, 5-HT2C; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS;

EID: 4243191447     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.104.067306     Document Type: Article

References (28)

1. Awaji T, Hirasawa A, Kataoka M, Shinoura H, Nakayama Y, Sugawara T, Izumi S, and Tsujimoto G (1998) Real-time optical monitoring of ligand-mediated internalization of alb-adrenoceptor with green fluorescent protein. Mol Endocrinol 12:1099-1111.
2. 2C receptor agonists. Exp Opin Ther Patents 13:1691-1705.
3. Boess FG and Martin IL (1994) Molecular biology of 5-HT receptors. Neuropharmacology 33:275-317.
4. 2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder. J Med Chem 40:2762-2769.
5. 1C sites. Eur J Pharmacol 191:93-96.
6. Conway BR, Minor LK, Xu JZ, D'Andrea MR, Ghosh RN, and Demarest KT (2001) Quantitative analysis of agonist-dependent parathyroid hormone receptor trafficking in whole cells using a functional green fluorescent protein conjugate. J Cell Physiol 189:341-355.
7. Conway BR, Minor LK, Xu JZ, Gunnet JW, DeBiasio R, D'Andrea MR, Rubin R, DeBiasio R, Giuliano K, Zhou L, et al. (1999) Quantification of G-protein coupled receptor internalization using G-protein coupled receptor-green fluorescent protein conjugates with the Arrayscan high-content screening system. J Biomol Screen 4:75-86.
8. 2C receptors. J Pharmacol Exp Ther 295:1120-1126.
9. Ferguson SS (2001) Evolving concepts in G protein-coupled receptor endocytosis: the role in receptor desensitization and signaling. Pharm Rev 53:1-24.
10. 1C receptor activation: a key step in the initiation of migraine? Trends Pharmacol Sci 10:307-309.
11. 2C receptors but not by sympathomimetic effects. Neuropharmacology 33:457-465.
12. 1C antagonists indicate that receptors mediated mCPP-induced hypophagia. Br J Pharmacol 103:2016-2020.
13. 2B receptor antagonist with anxiolytic-like properties. Br J Pharmacol 117:427-434.
14. 2C receptor antagonist. Neuropharmacology 36:609-620.
15. Marion S, Weiner DM, and Caron MG (2004) RNA editing induces variation in desensitization and trafficking of 5-hydroxytrptamine 2C receptor isoforms. J Biol Chem 279:2945-2954.
16. 2- adrenoceptors: comparisons with the unmodified receptors. Br J Pharmacol 130:1825-1832.
17. 2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists. Eur J Pharmacol 325:9-12.
18. Navarro A, Zapata R, Canela EI, Mallol J, Lluis C, and Franco R (1999) Epidermal growth factor (EGF)-induced up-regulation and agonist- and antagonist-induced desensitization and internalization of A1 adenosine receptors in a pituitary-derived cell line. Brain Res 816:47-57.
19. 2C receptor: alterations in suicide and implications for serotonergic pharmacotherapy. Neuropsychopharmacology 24:478-491.
20. Pfeiffer R, Kirsch J, and Fahrenholz F (1998) Agonist and antagonist-dependent internalization of the human vasopressin V2 receptor. Exp Cell Res 244:327-339.
21. 2C receptors in CHO-K1 cells. Br J Pharmacol 128:13-20.
22. 2C receptor. J Pharmacol Exp Ther 299:83-89.
23. Roettger BF, Ghanekar D, Rao R, Toledo C, Yingling J, Pinon D, and Miller LJ (1997) Antagonist-stimulated internalization of the G protein coupled cholecystokinin receptor. Mol Pharm 51:357-362.
24. 1C receptor activation by hallucinogenic drugs. Psychopharmacology 105:340-346.
25. 2A/2C receptor agonist, in two rat models of sustained pain. Anesth Analg 96:1072-1078.
26. Stollak JS and Furchgott RF (1983) Use of selective antagonists for determining the types of receptors mediating the actions of 5-hydroxytryptamine and tryptamine in the isolated rabbit aorta. J Pharmacol Exp Ther 224:215-221.
27. Stowell JN and Craig AM (1999) Axon/Dendrite targeting of metabotropic glutamate receptors by their cytoplasmic carboxy-terminal domains. Neuron 22:525-536.
28. Willins DL, Alsayegh L, Berry SA, Bachstrom JR, Sanders-Bush E, Friedman L, Khan N, and Roth BL (1998) Serotonergic antagonist effects on trafficking of serotonin 5-HT2A receptors in vitro and in vivo. Ann NY Acad Sci 861:121-127.