Evidence for protean agonism of RX 831003 at α2A-adrenoceptors by co-expression with different Gα protein subunits

Neuropharmacology

Volumn 42, Issue 6, 2002, Pages 855-863

  Pauwels, P J ^a   Rauly, I ^a   Wurch, T ^a   Colpaert, F C ^a  

^a INSTITUT DE RECHERCHE PIERRE FABRE   (France)

Author keywords

2A adrenoceptor; 35S GTP S; Ca2+ response; G protein; Protean agonist

Indexed keywords

2 (2 ETHOXY 1,4 BENZODIOXAN 2 YL) 2 IMIDAZOLINE; 2 (2 PENTYL 2,3 DIHYDROBENZOFURAN 2 YL) 4,5 DIHYDRO 1H IMIDAZOLE; 2 (2,3 DIHYDRO 2 PENTYLBENZOFURAN 2 YL) 2 IMIDAZOLINE; 351 CYSTEINYLISOLEUCINE; 373 THREONYL ALPHA 2A ADRENOCEPTOR; ADRENALIN; ALPHA 15 G PROTEIN; ALPHA 2A ADRENERGIC RECEPTOR; ATIPAMEZOLE; CALCIUM ION; DEXEFAROXAN; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); IMIDAZOLE DERIVATIVE; LIGAND; PROTEIN; PROTEIN SUBUNIT; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CALCIUM CELL LEVEL; CONTROLLED STUDY; DRUG ACTIVITY; DRUG POTENCY; LIGAND BINDING; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN CONTENT; PROTEIN EXPRESSION;

ADRENERGIC ALPHA-ANTAGONISTS; ANIMALS; BENZOPYRANS; CHO CELLS; CRICETINAE; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HETEROTRIMERIC GTP-BINDING PROTEINS; HUMANS; IMIDAZOLES; RECEPTORS, ADRENERGIC, ALPHA-2; SIGNAL TRANSDUCTION;

EID: 0036094811     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(01)00201-5     Document Type: Article

References (32)

1. Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: Evidence for agonist-directed trafficking of receptor stimulus
2. A rapid and sensitive method for the quantification of microgram quantities of protein utilizing the principle of protein-dye binding
3. s
4. 2-adrenergic receptor
5. αo protein
6. Human alpha 2-adrenergic receptor subtype distribution: Widespread and subtype-selective expression of alpha 2C10, alpha 2C4, and alpha 2C2 mRNA in multiple tissues
7. Protean effects of a natural peptide agonist of the G protein-coupled secretin receptor demonstrated by receptor mutagenesis
8. Structural instability of a constitutively active G protein-coupled receptors. Agonist-independent activation due to conformational flexibility
9. sα in which substitutions decrease receptor-mediated activation and increase receptor affinity
10. 2A-adrenoceptors
11. Pharmacological proteus?
12. Agonist-receptor efficacy. II: Agonist trafficking of receptor signals
13. The classification of seven transmembrane receptor in recombinant expression systems
14. Inverse, protean, and ligand-selective agonism: Matters of receptor conformation
15. A three-state model of agonist action
16. Inverse agonism and the regulation of receptor number
17. Inverse agonism: Pharmacological curiosity or potential therapeutic strategy?
18. α15 fusion proteins: Evidence for multiple ligand-activation binding sites
19. 2A-adrenoceptor
20. 1B/D receptor ligands: An answer from GTPγS binding studies with stably transfected C6-glial cell lines
21. αo protein coexpression: Evidence for inverse agonism
22. α15 fusion proteins
23. α-protein
24. α protein density ratio using fusion proteins
25. Effects of the substituted (S)-3-phenylpiperidine (-)-OSU6162 on PET measurements in subhuman primates: Evidence for tone-dependent normalization of striatal dopaminergic activity
26. 2A-adrenergic receptor
27. q class: Expression in murine tissues and in stromal and hematopoietic cell lines
28. A modified overlap extension PCR method to create chimeric genes in the absence of restriction enzymes
29. 2A adrenergic receptors
30. αo protein
31. Influence of G protein type on agonists efficacy
32. α14