Mutations of transmembrane IV and V serines indicate that all tryptamines do not bind to the rat 5-HT(2A) receptor in the same manner

Molecular Brain Research

Volumn 49, Issue 1-2, 1997, Pages 1-6

  Johnson, Michael P ^a   Wainscott, David B ^a   Lucaites, Virginia L ^a   Baez, Melvyn ^a   Nelson, David L ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

5 HT(2A) receptor; 5 Methoxytryptamine; 125I DOI; 3H ketanserin; Mutation; Tryptamine

Indexed keywords

1 ISOPROPYL 6 METHYLERGOLINE 8 CARBOXYLIC ACID 2 HYDROXY 1 METHYLPROPYL ESTER; 5 METHOXYTRYPTAMINE; ALANINE; INOSITOL TRISPHOSPHATE; KETANSERIN; LY 86057; N 1 ISOPROPYL 5 METHOXYTRYPTAMINE; SERINE; SEROTONIN; SEROTONIN 2A RECEPTOR; SEROTONIN AGONIST; SEROTONIN ANTAGONIST; TRYPTAMINE; TRYPTAMINE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG RECEPTOR BINDING; GENE MUTATION; MUTAGENESIS; PRIORITY JOURNAL; PROTEIN STRUCTURE; RECEPTOR BINDING;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; AMPHETAMINES; ANIMALS; BINDING SITES; BINDING, COMPETITIVE; CELL MEMBRANE; ERGOLINES; KETANSERIN; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; PROTEIN STRUCTURE, SECONDARY; RATS; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; SERINE; SEROTONIN; SEROTONIN ANTAGONISTS; TRYPTAMINES;

EID: 0030665907     PISSN: 0169328X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0169-328X(97)00115-0     Document Type: Article

References (32)

1. 1Dβ receptor. Mol. Pharmacol. 41:1992;1-7.
2. 2 receptor is encoded by a multiple intron-exon gene. Mol. Brain. Res. 14:1992;20-26.
3. Demchyshyn L., Sunahara R.K., Miller K., Teitler M., Hoffman B.J., Kennedy J.L., Seeman P., Van Tol H.H.M. A human serotonin 1D receptor variant (5HT1Dβ) encoded by an intronless gene on chromosome 6. Proc. Natl. Acad. Sci. USA. 89:1992;552-5526.
4. 1D-type. Mol. Pharmacol. 40:1991;143-148.
5. 1B. Biochem. Biophys. Res. Commun. 184:1992;752-759.
6. Hibert M.F., Trumpp-Kallmeyer S., Bruinvels A., Hoflack J. Three-dimensional models of neurotransmitter G-binding protein-coupled receptors. J. Pharmacol. Exp. Ther. 40:1991;8-15.
7. Hoyer D., Middlemiss D.N. Species differences in the pharmacology of terminal 5-HT autoreceptors in mammalian brain. Trends Pharmacol. Sci. 10:1989;130-132.
8. 1B receptor. J. Biol. Chem. 267:1992;5735-5738.
9. 2 receptor in rat and squirrel monkey cortex. Eur. J. Pharmacol. 239:1993;111-118.
10. 2A receptors reveal conserved transmembrane homology to the human rather than rat sequence. Biochim. Biophy. Acta. 1236:1995;201-206.
11. Johnson M.P., Loncharich R.J., Baez M., Nelson D.L. Species variations in transmembrane region V of the 5-HT Type 2A receptor alters the structure-activity relationship of certain ergolines and tryptamines. Mol. Pharmacol. 45:1994;277-286.
12. 2 receptor defines a family of structurally distinct but functionally conserved serotonin receptors. Proc. Natl. Acad. Sci. USA. 87:1990;928-932.
13. 2 receptor from a human to a rat pharmacology. FEBS Lett. 3:1992;324-328.
14. 2F) from rat stomach fundus. Mol. Pharmacol. 42:1992;549-557.
15. Levy F.O., Gudermann T., Perez R.E., Birnbaumer M., Kaumann A.J., Birnbaumer L. Molecular cloning of a human serotonin receptor (S12) with a pharmacological. J. Biol. Chem. 267:1992;7553-7562.
16. 2 serotonin receptor gene Htr-2 is tightly linked to Es-10 on mouse chromosome 14. Genomics. 11:1991;231-234.
17. 1B serotonin receptor: cloning, functional expression, and localization in motor control centers. Proc. Natl. Acad. Sci. USA. 89:1992;3020-3024.
18. 355Asn site directed mutagenesis. Biochem. Pharmacol. 44:1992;1917-1920.
19. 2 receptor: structurally specific differentiation by ergolines and tryptamines. J. Pharmacol. Exp. Ther. 265:1993;1272-1279.
20. 1B receptors. Nature. 360:1992;161-163.
21. 1B receptors. J. Neurochem. 60:1993;380-383.
22. Pazos A., Hoyer D., Palacios J.M. Mesulergine, a selective serotonin-2 ligand in the rat cortex, does not label these receptors in porcine and human cortex: evidence for species differences in brain serotonin-2 receptors. Eur. J. Pharmacol. 106:1985;531-538.
23. 2 receptor. EMBO J. 7:1988;4135-4140.
24. 1C receptor subtypes. Biochem. Biophys. Res. Commun. 181:1991;1469-1478.
25. 1A receptor genes. Eur. J. Pharmacol. 227:1992;153-162.
26. Swillens S. How to estimate the total receptor concentration when the specific radioactivity of the ligand is unknown. Trends Pharmacol. Sci. 13:1992;430-434.
27. Tritch R.J., Rodinson D.L., Sahagan B.G., Horlick R.A. Cloning and nucleotide sequence of human (5-HT) type 2 receptor. Soc. Neurosci. Abstr. 18:1991;163. Abstr. # 168.
28. Trumpp-Kallmeyer S., Bruinvels A., Hoflack J., Hibert M. Recognition site mapping and receptor modeling: application to 5-HT receptors. Neurochem. Int. 19:1991;397-406.
29. 1B receptor. EMBO J. 10:1991;4017-4023.
30. 2F receptor. Mol. Pharmacol. 43:1993;419-426.
31. 1D receptor is encoded by a subfamily of two distinct genes. Proc. Natl. Acad. Sci. USA. 89:1992;3630-3634.
32. 2 receptor. J. Neurosci. Res. 33:1992;196-204.