Inverse agonists and neutral antagonists of recombinant human A1 adenosine receptors stably expressed in Chinese hamster ovary cells
JC Shryock, MJ Ozeck, L Belardinelli - Molecular pharmacology, 1998 - ASPET
Receptor antagonists can be classified as neutral antagonists or antagonists with inverse
agonist activity based on their effectiveness to reduce the spontaneous agonist-independent …
agonist activity based on their effectiveness to reduce the spontaneous agonist-independent …
Agonist-independent effect of an allosteric enhancer of the A1 adenosine receptor in CHO cells stably expressing the recombinant human A1 receptor
CA Kollias-Baker, J Ruble, M Jacobson… - … of Pharmacology and …, 1997 - ASPET
The allosteric enhancer PD 81,723, a 2-amino-3-benzoylthiophene derivative, has been
shown to potentiate agonist binding to A1 adenosine receptors (A1AdoRs) and to enhance …
shown to potentiate agonist binding to A1 adenosine receptors (A1AdoRs) and to enhance …
Serine and alanine mutagenesis of the nine native cysteine residues of the human A1 adenosine receptor
DJ Scholl, JN Wells - Biochemical pharmacology, 2000 - Elsevier
To examine the importance of the nine native cysteine residues in the human A1 adenosine
receptor, each cysteine was individually mutated to both serine and alanine. Saturation …
receptor, each cysteine was individually mutated to both serine and alanine. Saturation …
Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors
B Kull, G Arslan, C Nilsson, C Owman… - Biochemical …, 1999 - Elsevier
To examine possible species differences in pharmacology, rat adenosine A2A receptors
were studied in PC12 (pheochromocytoma) cells, and human receptors in Chinese hamster …
were studied in PC12 (pheochromocytoma) cells, and human receptors in Chinese hamster …
Identification of Domains of the Human A1 Adenosine Receptor That Are Important for Binding Receptor Subtype-selective Ligands Using Chimeric A1/A2a Adenosine …
SA Rivkees, ME Lasbury, H Barbhaiya - Journal of Biological Chemistry, 1995 - ASBMB
To provide new insights into the regions of the human A 1 adenosine receptor (A 1 AR)
involved in ligand binding, a series of chimeric human A 1 and rat A 1 adenosine receptors …
involved in ligand binding, a series of chimeric human A 1 and rat A 1 adenosine receptors …
Constitutive activation of A3 adenosine receptors by site-directed mutagenesis
A Chen, ZG Gao, D Barak, BT Liang… - … and biophysical research …, 2001 - Elsevier
The objective of this study was to create constitutively active mutant human A3 adenosine
receptors (ARs) using single amino acid replacements, based on findings from other G …
receptors (ARs) using single amino acid replacements, based on findings from other G …
[HTML][HTML] Glutamate residues in the second extracellular loop of the human A2a adenosine receptor are required for ligand recognition
J Kim, Q Jiang, M Glashofer, S Yehle… - Molecular …, 1996 - ncbi.nlm.nih.gov
The A 2a adenosine receptor, a member of the G protein-coupled receptor family, is
important in the regulation of dopaminergic pathways of the brain and in platelet and …
important in the regulation of dopaminergic pathways of the brain and in platelet and …
Evidence for co-expression and desensitization of A2a and A2b adenosine receptors in NG108-15 cells
SJ Mundell, E Kelly - Biochemical pharmacology, 1998 - Elsevier
Using receptor-selective agonists and antagonists, the possible presence of both A2a and
A2b adenosine receptor subtypes coupled to activation of adenylyl cyclase was investigated …
A2b adenosine receptor subtypes coupled to activation of adenylyl cyclase was investigated …
Structural Determinants of A3 Adenosine Receptor Activation: Nucleoside Ligands at the Agonist/Antagonist Boundary
ZG Gao, SK Kim, T Biadatti, W Chen… - Journal of medicinal …, 2002 - ACS Publications
Mutagenesis of the human A3 adenosine receptor (AR) suggested that certain amino acid
residues contributed differently to ligand binding and activation processes. Here we …
residues contributed differently to ligand binding and activation processes. Here we …
N6,5'-Disubstituted Adenosine Derivatives as Partial Agonists for the Human Adenosine A3 Receptor
EW van Tilburg… - Journal of medicinal …, 1999 - ACS Publications
5 '-(Alkylthio)-substituted analogues of N 6-benzyl-and N 6-(3-iodobenzyl) adenosine were
synthesized in 37− 61% overall yields. The affinities of these compounds for the adenosine …
synthesized in 37− 61% overall yields. The affinities of these compounds for the adenosine …
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