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1 Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi α-subunits
article 2004    
Author: Klaasse, E. · Ligt, R.A.F.de · Roerink, S.F. · Lorenzen, A. · Milligan, G. · Leurs, R. · IJzerman, A.P.
Keywords: Health · Physiological Sciences · Adenosine A1 receptor · Allosteric modulation · Constitutive activity · Fusion protein · G protein · Inverse agonism · 2 amino 4,5 dimethyl 3 (3 trifluoromethylbenzoyl)thiophene · 6 n cyclopentyladenosine · 8 cyclopentyl 1,3 dipropylxanthine · 8 cyclopentyltheophylline · Adenosine A1 receptor · Amino acid · Arginine · Cysteine · Glycine · Guanine nucleotide binding protein · Guanosine 5' o (3 thiotriphosphate) · Histidine · Hybrid protein · Isoleucine · Phenylalanine · Proline · Radioligand · Serine · Sodium ion · Sulfur 35 · Valine · Allosterism · Alpha chain · Animal cell · Cercopithecidae · Ligand binding · Nonhuman · Priority journal · Protein analysis · Adenosine · Allosteric Site · Animals · Binding, Competitive · Cell Membrane · COS Cells · Cysteine · Dose-Response Relationship, Drug · GTP-Binding Protein alpha Subunits, Gi-Go · Guanosine 5'-O-(3-Thiotriphosphate) · Humans · Mutation · Radioligand Assay · Receptor, Adenosine A1 · Recombinant Fusion Proteins · Sodium Chloride · Sulfur Radioisotopes · Thiophenes · Transfection · Tritium · Xanthines
[Abstract]

2 Synthesis and biological evaluation of disubstituted N6- cyclopentyladenine analogues: The search for a neutral antagonist with high affinity for the adenosine A1 receptor
article 2004    
Author: Ligt, R.A.F. de · Klein, P.A.M. van der · Frijtag Drabbe Künzel, J.K. von · Lorenzen, A. · El Maate, F.A. · Fujikawa, S. · Westhoven, R. van · Hoven, T. van den · Brussee, J. · Ijzerman, A.P.
Keywords: Biology Toxicology · Physiological Sciences · [35S]GTPγS binding · Adenosine A1 receptor · Inverse agonism · N-0840 derivatives · Neutral antagonist · 8 bromo 9 methyladenine · 8 bromo n 6 cyclopentyl 9 methyladenine · 8 bromo n 6 cyclopentyl 9 propyladenine · 9 allyl 8 bromo n 6 cyclopentyladenine · 9 allyl n 6 cyclopentyl 8 methoxyadenine · adenine derivative · adenosine A1 receptor antagonist · luf 5666 · luf 5668 · luf 5669 · luf 5674 · n 0840 · n 6 cyclopentyl 8 (ethylthio) 9 methyladenine · n 6 cyclopentyl 8 (n ethyl n butylamino) 9 methyladenine · n 6 cyclopentyl 8 (n methyl n ethylamino) 9 methyladenine · n 6 cyclopentyl 8 (n methyl n propylamino) 9 methyladenine · n 6 cyclopentyl 8 (n methylamino) 9 methyladenine · n 6 cyclopentyl 8 (n methylisopropylamino) 9 methyladenine · n 6 cyclopentyl 8 (n piperidino) 9 methyladenine · n 6 cyclopentyl 8 (n pyrrolidino) 9 methyladenine · n 6 cyclopentyl 8 (n,n diethylamino) 9 methyladenine · n 6 cyclopentyl 8 ethoxy 9 methyladenine · n 6 cyclopentyl 8 isopropoxy 9 methyladenine · n 6 cyclopentyl 8 methoxy 9 methyladenine · n 6 cyclopentyl 8 methoxy 9 propyladenine · n 6 cyclopentyl 9 methyl 8 oxoadenine · n 6 cyclopentyl 9 methyl 8 propoxyadenine · n 6 cyclopentyl 9 methyladenine · unclassified drug · article · binding affinity · drug determination · drug synthesis · drug tolerability · receptor affinity · substitution reaction · Adenine · Adenosine · Animals · Cell Line · CHO Cells · Cricetinae · Drug Evaluation, Preclinical · Humans · Receptor, Adenosine A1
[Abstract]

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