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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2001-8-27
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pubmed:abstractText |
1. The present work was devoted to the study of A3 adenosine receptors in Jurkat cells, a human leukemia line. 2. The A3 subtype was found by means of RT-PCR experiments and characterized by using the new A3 adenosine receptor antagonist [3H]-MRE 3008F20, the only A3 selective radioligand currently available. Saturation experiments revealed a single high affinity binding site with K(D) of 1.9+/-0.2 nM and B(max) of 1.3+/-0.1 pmol mg(-1) of protein. 3. The pharmacological profile of [3H]-MRE 3008F20 binding on Jurkat cells was established using typical adenosine ligands which displayed a rank order of potency typical of the A3 subtype. 4. Thermodynamic data indicated that [3H]-MRE 3008F20 binding to A3 subtype in Jurkat cells was entropy- and enthalpy-driven, according with that found in cells expressing the recombinant human A3 subtype. 5. In functional assays the high affinity A3 agonists Cl-IB-MECA and IB-MECA were able to inhibit cyclic AMP accumulation and stimulate Ca(2+) release from intracellular Ca(2+) pools followed by Ca(2+) influx. 6. The presence of the other adenosine subtypes was investigated in Jurkat cells. A1 receptors were characterized using [3H]-DPCPX binding with a K(D) of 0.9+/-0.1 nM and B(max) of 42+/-3 fmol mg(-1) of protein. A2A receptors were studied with [3H]-SCH 58261 binding and revealed a K(D) of 2.5+/-0.3 nM and a B(max) of 1.4+/-0.2 pmol mg(-1) of protein. 7. In conclusion, by means of the first antagonist radioligand [3H]-MRE 3008F20 we could demonstrate the existence of functional A3 receptors on Jurkat cells.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-10078988,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-10369472,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-10438932,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-10442481,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-10496952,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-10579811,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-10731034,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-10779381,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-10854059,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-11111830,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-11121831,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-1323836,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-13465304,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-2440339,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-4627078,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-6254391,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-7532939,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-7560091,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-7582525,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-7598508,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-8349579,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-8645277,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-8692279,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-8846829,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-8848003,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-8878055,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-8896425,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-9401772,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-942051,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-9605581,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-9618527,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-9652191,
http://linkedlifedata.com/resource/pubmed/commentcorrection/11522603-9755289
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/1,3-dipropyl-8-cyclopentylxanthine,
http://linkedlifedata.com/resource/pubmed/chemical/5-amino-7-(2-phenylethyl)-2-(2-furyl...,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Guanosine Triphosphate,
http://linkedlifedata.com/resource/pubmed/chemical/MRE 3008-F20,
http://linkedlifedata.com/resource/pubmed/chemical/Phenylurea Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Purinergic P1 Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/RNA, Messenger,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Adenosine A2A,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Adenosine A3,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Purinergic P1,
http://linkedlifedata.com/resource/pubmed/chemical/Triazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium,
http://linkedlifedata.com/resource/pubmed/chemical/Xanthines
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
134
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
116-26
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:11522603-Humans,
pubmed-meshheading:11522603-Animals,
pubmed-meshheading:11522603-Calcium,
pubmed-meshheading:11522603-Pyrimidines,
pubmed-meshheading:11522603-Xanthines,
pubmed-meshheading:11522603-Thermodynamics,
pubmed-meshheading:11522603-Triazoles,
pubmed-meshheading:11522603-Cricetinae,
pubmed-meshheading:11522603-Kinetics,
pubmed-meshheading:11522603-Tritium,
pubmed-meshheading:11522603-Time Factors,
pubmed-meshheading:11522603-RNA, Messenger,
pubmed-meshheading:11522603-CHO Cells,
pubmed-meshheading:11522603-Dose-Response Relationship, Drug,
pubmed-meshheading:11522603-Binding, Competitive,
pubmed-meshheading:11522603-Cyclic AMP,
pubmed-meshheading:11522603-Guanosine Triphosphate,
pubmed-meshheading:11522603-T-Lymphocytes,
pubmed-meshheading:11522603-Phenylurea Compounds,
pubmed-meshheading:11522603-Receptors, Purinergic P1,
pubmed-meshheading:11522603-Receptor, Adenosine A3
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