Differential effects of the allosteric enhancer (2-amino-4,5-dimethyl-trienyl)[3-(trifluoromethyl) phenyl]methanone (PD81,723) on agonist and antagonist binding and function at the human wild-type and a mutant (T277A) adenosine A1 receptor

Biochemical Pharmacology

Volumn 61, Issue 2, 2001, Pages 137-144

  Kourounakis, Angeliki ^a   Visser, Corine ^a   De Groote, Miriam ^a   IJzerman, Ad P ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

Author keywords

Adenosine A1; Allosteric; G protein coupled receptors; Modulation; Mutant; PD81, 723

Indexed keywords

2 AMINO 4,5 DIMETHYL 3 (3 TRIFLUOROMETHYLBENZOYL)THIOPHENE; 6 N CYCLOPENTYLADENOSINE; 8 CYCLOPENTYL 1,3 DIPROPYLXANTHINE; ADENOSINE A1 RECEPTOR; ADENOSINE A1 RECEPTOR AGONIST; ADENOSINE A1 RECEPTOR ANTAGONIST; CYCLIC AMP; FORSKOLIN; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN;

ALLOSTERISM; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; CELL MEMBRANE; CHINESE HAMSTER; COMPETITIVE INHIBITION; CONTROLLED STUDY; DOSE RESPONSE; DRUG BINDING; DRUG EFFECT; DRUG RECEPTOR BINDING; DRUG STRUCTURE; NONHUMAN; OXYGEN SATURATION; PRIORITY JOURNAL; SITE DIRECTED MUTAGENESIS; STRUCTURE ANALYSIS;

ALANINE; ALLOSTERIC REGULATION; BINDING, COMPETITIVE; CELLS, CULTURED; CYCLIC AMP; HUMANS; MUTATION; RECEPTORS, PURINERGIC P1; THIOPHENES; THREONINE;

EID: 0035863033     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(00)00536-0     Document Type: Article

References (24)

1. Adenosine
2. Allosteric regulation of muscarinic receptors
3. Allosteric interactions at muscarinic cholinoceptors
4. 1 receptor binding and function by 2-amino-3-benzoylthiophenes
5. 1 receptor binding by 2-amino-3-benzoylthiophenes
6. 1, receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding
7. Conformational inductions versus conformational selection: Evidence from allosteric enhancers
8. Allosteric enhancer PD 81,723 acts by novel mechanism to potentiate cardiac actions of adenosine
9. 1 receptor functions by benzoylthiophenes in guinea pig tissues in vitro
10. 1 adenosine receptor, lowers the threshold for ischemic preconditioning in dogs
11. 1 adenosine receptors
12. 1 receptor
13. 1 adenosine receptor mediates specific agonist binding
14. 1 adenosine receptors: Two amino acids are responsible for species differences in ligand recognition
15. 2 adenosine receptors
16. 1 receptors
17. 1 adenosine receptor cDNA
18. Measurement of protein using bicinchoninic acid
19. 50) of an enzymatic reaction
20. 1 adenosine receptor coupling to G proteins
21. 1 adenosine receptors stably expressed in Chinese hamster ovary cells
22. 1 adenosine receptor: Influences of acidic and hydroxy residues in the first four transmembrane domains on ligand binding
23. 1 receptor-dependent and -independent effects of the allosteric enhancer PD 81,723