Activating mutations of the serotonin 5-HT(2C) receptor

Journal of Neurochemistry

Volumn 69, Issue 3, 1997, Pages 1138-1144

  Herrick Davis, Katharine ^a   Egan, Christina ^a   Teitler, Milt ^a  

^a ALBANY MEDICAL COLLEGE   (United States)

Author keywords

Constitutive activity; G protein; Inverse agonist; Mutagenesis; Phosphoinositide hydrolysis; Serotonin 5 HT(2C)

Indexed keywords

MESULERGINE; MIANSERIN; SEROTONIN 1C RECEPTOR;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CARBOXY TERMINAL SEQUENCE; DRUG POTENCY; GENE MUTATION; HORMONAL REGULATION; HYDROLYSIS; NONHUMAN; PHOSPHOINOSITIDE METABOLISM; PRIORITY JOURNAL; PROTEIN DOMAIN; RAT; RECEPTOR UPREGULATION; SECOND MESSENGER; SITE DIRECTED MUTAGENESIS;

ANIMALIA;

EID: 0030757387     PISSN: 00223042     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1471-4159.1997.69031138.x     Document Type: Article

References (34)

1. 2C receptors, respectively. Neuropsychopharmacology 13, 1-8.
2. Barker E. L., Westphal R. S., Schmidt D., and Sanders-Bush E. (1994) Constitutively active 5-hydroxytryptamine receptors reveal novel inverse agonist activity of receptor ligands. J. Biol. Chem. 269, 11687-11690.
3. Berendsen H. H. (1995) Interactions between 5-hydroxytryptamine receptor subtypes. Pharmacol. Ther. 66, 17-37.
4. Berridge M. J., Downes C. P., and Hanley M. R. (1982) Lithium amplifies agonist-dependent phosphatidylinositol responses in brain and salivary glands. Biochem. J. 206, 587-595.
5. Bluml K., Mutschler E., and Wess J. (1994) Functional role in ligand binding and receptor activation of an asparagine residue present in the sixth transmembrane domain of all muscarinic acetylcholine receptors. J. Biol. Chem. 269, 18870-18876.
6. Boyson S. J. and Alexander A. (1990) Net production of cerebrospinal fluid is decreased by SCH-23390. Ann. Neurol. 27, 631-635.
7. Burnstein E. S., Spalding T. A., Hill-Eubanks D., and Brann M. R. (1995) Structure-function of muscarinic receptor coupling to G proteins. J. Biol. Chem. 270, 3141-3146.
8. Canton H., Verriele L., and Millan M. J. (1994) Competitive antagonism of serotonin 5-HT2C and 5-HT2A receptor-mediated phosphoinositide turnover by clozapine in the rat: a comparison to other antipsychotics. Neurosci. Lett. 181, 65-68.
9. 2 binding site in rat cerebral cortex but not in subcortical regions. J. Pharmacol. Exp. Ther. 234, 195-200.
10. Fozard R. J. R. and Gray J. A. (1989) 5-HT1C 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. Julius D., Livelli T. J., Jessell T. M., and Axel R. (1989) Ectopic expression of the serotonin 1c receptor and the triggering of malignant transformation. Science 244, 1057-1060.
13. 1C antagonists indicate that receptors mediate mCPP-induced hypophagia. Br. J. Pharmacol. 103, 2016-2020.
14. 1C receptor subtype. Neurosci. Lett. 105, 174-176.
15. 1b-adrenergic receptor by all amino acid substitutions at a single site. J. Biol. Chem. 267, 1430-1433.
16. Labrecque J., Fargin A., Bouvier A., Chidiac P., and Dennis M. (1995) Serotonergic antagonists differentially inhibit spontaneous activity and decrease ligand binding capacity of the rat 5-hydroxytryptamine type2C receptor in Sf9 cells. Mol. Pharmacol. 46, 937-942.
17. 1C receptors and phosphoinositide systems by ethanol consumption in rat brain and choroid plexus. Eur. J. Pharmacol. 247, 81-88.
18. Parma J., Duprez L., VanSande J., Cochaux P., Gervy C., Mockel J., Dumont J., and Vassart G. (1993) Somatic mutations in the thyrotropin gene cause hyperfunctioning thyroid adenomas. Nature 365, 649-651.
19. Perez D. M., Hwa J., Gaivin R., Mathur M., Brown F., and Graham R. M. (1996) Constitutive activation of a single effector pathway: evidence for multiple activation states of a G protein-coupled receptor. Mol. Pharmacol. 49, 112-122.
20. Rao V. R., Cohen G. B., and Oprian D. D. (1994) Rhodopsin mutation G90D and a molecular mechanism for congenital night blindness. Nature 367, 639-642.
21. 2-adrenergic receptor. J. Biol. Chem. 268, 16483-16487.
22. Robinson P. R., Cohen G. B., Zhukovsky E. A., and Oprian D. D. (1992) Constitutively active mutants of rhodopsin. Neuron 9, 719-725.
23. Roth B. L. (1994) Multiple serotonin receptors: clinical and experimental aspects. Ann. Clin. Psychiatry 6, 67-78.
24. 2-adrenergic receptor. J. Biol. Chem. 268, 4625-4636.
25. 2-adrenergic receptor. Mol. Pharmacol. 45, 390-394.
26. 1C receptor activation by hallucinogenic drugs. Psychopharmacology 105, 340-346.
27. 1B-adrenergic receptor: role of highly conserved polar amino acids in receptor activation. EMBO J. 15, 3566-3578.
28. Schipani E., Kruse K., and Jueppner H. A. (1995) Constitutively active mutant PTH-PTHrP receptor in Jansen-type metaphyseal chondrodysplasia. Science 268, 98-102.
29. Shenker A., Laue L., Kosugi S., Meredino J. J. Jr., Minegishi T., and Cutler G. B. Jr. (1993) A constitutively activating mutation of the luteinizing hormone receptor in familial male precocious puberty. Nature 365, 652-654.
30. Spalding T, A., Burstein E. S., Brauner-Osborne H., Hill-Eubanks D., and Brann M. R. (1995) Pharmacology of a constitutively active muscarinic receptor generated by random mutagenesis. J. Pharmacol. Exp. Ther. 275, 1274-1279.
31. 2C serotonin receptors. Nature 374, 542-546.
32. Tiberi M. and Caron M. G. (1994) High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype. J. Biol. Chem. 269, 27925-27931.
33. Westphal R. S. and Sanders-Bush E. (1994) Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists. Mol. Pharmacol. 46, 937-942.
34. Westphal R. S., Backstrom J. R., and Sanders-Bush E. (1995) Increased basal phosphorylation of the constitutively active serotonin 2C receptor accompanies agonist-mediated desenitization. Mol. Pharmacol. 48, 200-205.