Site-directed mutagenesis of the 5-HT1B receptor increases the affinity of 5-HT for the agonist low-affinity conformation and reduces the intrinsic activity of 5-HT

European Journal of Pharmacology

Volumn 421, Issue 2, 2001, Pages 69-76

  Grånäs, Charlotta ^a,b   Nordquist, Jenny ^a   Mohell, Nina ^a   Larhammar, Dan ^a  

^a UPPSALA UNIVERSITY   (Sweden)

^b UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

5 HT; 5 HT1B receptor; 5 Hydroxytryptamine; GR125743; Site directed mutagenesis

Indexed keywords

ALANINE; CYCLIC AMP; FORSKOLIN; METHIONINE; N [4 METHOXY 3 (4 METHYL 1 PIPERAZINYL)PHENYL] 3 METHYL 4 (4 PYRIDYL)BENZAMIDE; PHENYLALANINE; SEROTONIN; SEROTONIN 1B RECEPTOR; TRITIUM;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; CELL MEMBRANE; CELL MUTANT; CHO CELL; CONTROLLED STUDY; CORRELATION FUNCTION; HUMAN; NONHUMAN; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN EXPRESSION; RECEPTOR AFFINITY; RECEPTOR INTRINSIC ACTIVITY; SITE DIRECTED MUTAGENESIS;

AMINO ACID SEQUENCE; ANIMALS; BENZAMIDES; BINDING, COMPETITIVE; COS CELLS; CYCLIC AMP; DOSE-RESPONSE RELATIONSHIP, DRUG; FORSKOLIN; GENOTYPE; HUMANS; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; MUTATION; PROTEIN CONFORMATION; PYRIDINES; RADIOLIGAND ASSAY; RECEPTOR, SEROTONIN, 5-HT1B; RECEPTORS, SEROTONIN; SEROTONIN; SEROTONIN AGONISTS; TRITIUM;

EID: 0035817446     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(01)01027-5     Document Type: Article

References (22)

1. Cell-specific coupling of the cloned human 5-HT1F receptor to multiple signal transduction pathways
2. 1B receptor is localized predominantly on axon terminals
3. 1F receptor messenger RNA in rodent and primate brain
4. 1Dbeta-like autoreceptors in the guinea-pig brain cortex
5. Point mutation increases a form of the NK1 receptor with high affinity for neurokinin A and B and septide
6. What intracranial tissues in humans contain sumatriptan-sensitive serotonin 5-HT1-type receptors?
7. 1D/B receptor antagonist
8. 1B binding sites
9. Lipofection: A highly efficient, lipid-mediated DNA-transfection procedure
10. 1A receptor and the role of residue F331 in signal transduction
11. 1B receptor
12. 1Dbeta receptor subtype in human and bovine cerebral arteries
13. 5-HT receptor classification and nomenclature: Towards a harmonization with the human genome
14. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
15. 2 receptor
16. A modification of the Lowry procedure to simplify protein determination in membrane and lipoprotein samples
17. 1D receptor in the action of sumatriptan
18. 1D receptors
19. A mutation changes ligand selectivity and transmembrane signaling preference of the neurokinin-1 receptor
20. Mutations along transmembrane segment II of the NK-1 receptor affect substance P competition with non-peptide antagonists but not substance P binding
21. A mutational-induced activated state of the β2-adrenergic receptor
22. 1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater