دورية أكاديمية
Radioligand binding and functional responses of ligands for human recombinant adenosine A(3) receptors.
| العنوان: | Radioligand binding and functional responses of ligands for human recombinant adenosine A(3) receptors. |
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| المؤلفون: | Yates L; Division of Pharmacology, Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff CF10 3XF, UK., Clark JH, Martin TJ, James S, Broadley KJ, Kidd EJ |
| المصدر: | Autonomic & autacoid pharmacology [Auton Autacoid Pharmacol] 2006 Apr; Vol. 26 (2), pp. 191-200. |
| نوع المنشور: | Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Wiley Country of Publication: England NLM ID: 101157306 Publication Model: Print Cited Medium: Print ISSN: 1474-8665 (Print) Linking ISSN: 14748665 NLM ISO Abbreviation: Auton Autacoid Pharmacol Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: 2014-2017 : Oxford, UK : Wiley Original Publication: Oxford, UK : Blackwell Pub., |
| مواضيع طبية MeSH: | Radioligand Assay*, Adenosine/*analogs & derivatives , Receptor, Adenosine A3/*metabolism, Adenosine/pharmacology ; Animals ; Binding, Competitive ; CHO Cells ; Cricetinae ; Cyclic AMP/biosynthesis ; Cyclic AMP/metabolism ; Guanosine 5'-O-(3-Thiotriphosphate)/pharmacology ; Iodine Radioisotopes ; Ligands ; Magnesium Chloride ; Quinazolines/pharmacology ; Receptor, Adenosine A3/analysis ; Receptor, Adenosine A3/drug effects ; Recombinant Proteins/metabolism ; Transfection ; Triazoles/pharmacology |
| مستخلص: | The binding and functional properties of adenosine receptor ligands were compared in Chinese hamster ovary cells transfected with human adenosine A(3) receptors. Inhibition of [(125)I]-aminobenzyl-5'-N-methylcarboamidoadenosine ([(125)I]-AB-MECA) binding by adenosine receptor ligands was examined in membrane preparations. Inhibition of forskolin-induced cAMP accumulation by agonists was measured using a cAMP enzyme immunoassay. The rank order of agonist potency for both assays was N(6)-(3-iodobenzyl)-adenosine-5'-N-methyluronamide (IB-MECA) > 5'-N-ethylcarboxamidoadenosine (NECA) > (-)-N(6)-[(R)-phenylisopropyl] adenosine (R-PIA) > 4-aminobenzyl-5'-N-methylcarboxamidoadenosine (AB-MECA) > N(6)-cyclopentyl adenosine (CPA) > adenosine. The radioligand binding rank order of antagonist potency was N-[9-chloro-2-(2-furanyl)[1,2,4]-triazolo[1,5-c]quinazolin-5-benzeneacetamide (MRS1220) > 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) > 8-phenyltheophylline (8-PT) > 8-(p-sulfophenyl)-theophylline (8-SPT). MRS1220 competitively inhibited the effect of IB-MECA on cAMP production, with a K(B) value of 0.35 nm. These data are characteristic of adenosine A(3) receptors. The absence of Mg(2+) and presence of guanosine 5'-(gamma-thio)triphosphate (GTPgammaS) significantly reduced agonist binding inhibition potency, indicating binding to high- and low-affinity states. The IB-MECA, NECA and R-PIA IC(50) values were greater for the cAMP assay than for radioligand binding, suggesting an efficient stimulus-response transduction pathway. |
| المشرفين على المادة: | 0 (9-chloro-2-(2-furyl)-5-phenylacetylamino(1,2,4)triazolo(1,5-c)quinazoline) 0 (Iodine Radioisotopes) 0 (Ligands) 0 (N(6)-(4-amino-3-iodophenyl)methyl-5'-N-methylcarboxamidoadenosine) 0 (Quinazolines) 0 (Receptor, Adenosine A3) 0 (Recombinant Proteins) 0 (Triazoles) 02F3473H9O (Magnesium Chloride) 152918-18-8 (N(6)-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine) 37589-80-3 (Guanosine 5'-O-(3-Thiotriphosphate)) 41552-82-3 (N(6)-cyclopentyladenosine) E0399OZS9N (Cyclic AMP) K72T3FS567 (Adenosine) |
| تواريخ الأحداث: | Date Created: 20060324 Date Completed: 20060927 Latest Revision: 20131121 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1111/j.1474-8673.2006.00372.x |
| PMID: | 16553647 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1474-8665 |
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| DOI: | 10.1111/j.1474-8673.2006.00372.x |