2-Amino-3-aroyl-4,5-alkylthiophenes: Agonist allosteric enhancers at human a1 adenosine receptors

Journal of Medicinal Chemistry

Volumn 45, Issue 2, 2002, Pages 382-389

  Tranberg, C Elisabet ^a   Zickgraf, Andrea ^b   Giunta, Brian N ^b   Luetjens, Henning ^a   Figler, Heidi ^c   Murphree, Lauren J ^c   Falke, Ruediger ^b   Fleischer, Holger ^d   Linden, Joel ^c   Scammells, Peter J ^a   Olsson, Ray A ^a,b  

^a DEAKIN UNIVERSITY   (Australia)

^b UNIVERSITY OF SOUTH FLORIDA   (United States)

^c UNIVERSITY OF VIRGINIA   (United States)

^d JOHANNES GUTENBERG UNIVERSITY   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINO 3 BENZOYL 4,5 DIMETHYLTHIOPHENE DERIVATIVE; 2 AMINO 4,5 DIMETHYL 3 (3 TRIFLUOROMETHYLBENZOYL)THIOPHENE; ADENOSINE A1 RECEPTOR AGONIST; THIOPHENE DERIVATIVE; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL CELL; ARTICLE; BINDING SITE; DRUG ACTIVITY; DRUG DETERMINATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; ENHANCER REGION; HYDROPHOBICITY; MOLECULAR SIZE; MOLECULAR STABILITY; NONHUMAN; PROTEIN EXPRESSION; RECEPTOR AFFINITY; RECEPTOR UPREGULATION; STRUCTURE ACTIVITY RELATION;

ALLOSTERIC REGULATION; ANIMALS; CHO CELLS; CRICETINAE; HUMANS; HYDROPHOBICITY; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; RECEPTORS, PURINERGIC P1; THIOPHENES;

EID: 0037122790     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010081p     Document Type: Article

References (29)

1. 1 receptor binding and function by 2-amino-3-benzoylthiophenes
2. 1 receptor binding by 2-amino-3-benzoylthiophenes
3. Adenosine: Electrophysiologic effects and therapeutic use for terminating paroxysmal supraventricular tachycardia
4. Diagnostic and therapeutic use of adenosine in patients with supraventricular tachyarrrythmias
5. 1 receptor
6. 1 receptor enhancer of the negative dromotropic action of adenosine in the guinea pig heart
7. Allosteric enhancer PD81,723 acts by novel mechanism to potentiate cardiac actions of adenosine
8. Novel approach for enhancing atrioventricular nodal conduction delay mediated by endogenous adenosine
9. 1 receptor functions by benzoylthiophenes in guinea pig tissues in vitro
10. Modulation of atrioventricular nodal function by metabolic and allosteric regulators of endogenous adenosine in guinea pig heart
11. 1 adenosine receptor, lowers the threshold for ischemic preconditioning in dogs
12. No. Pharmacol. Exp. Ther. vel thieno [2,3-d][1,3]oxazin-4-ones as inhibitors of human leukocyte elastase
13. Heterocyclen aus CH-aciden nitrilen. VIII. 2-Amino-thiophene aus methyleneaktiven nitrilen, carbonylverbindungen und schwefel
14. A simple modification of the Wolff-Kishner reduction
15. Heterocyclen aus CH-aciden nitrilen. XII. 2-Aminothiophene durch decarboxylierung von 2-aminothiophene-3-carbonsäuren
16. A new solid-phase Knoevenagel catalyst
17. LiCl catalyzed Knoevenagel condensations: Comparative study, of conventional method vs microwave irradiation
18. Rare-earth (RE) exchanged NaY zeolite promoted Knoevenagel condensation
19. Selective bromination of substituted acetophenones with dioxan dibromide
20. Selective brominations with copper-(II) bromide
21. Synthesis of bromoacetyl derivatives by use of tetrabutylammonium bromide
22. Potential antiarthritic agents. 2. Benzoylacetonitriles and β-aminocinnamonitriles
23. "Aromatic" substituent constants for structure - Activity correlations
24. 1 receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding
25. 1-adenosine receptor
26. 1 adenosine receptor coupling to G proteins
27. 1 receptor