Cloning of a chick A3 adenosine receptor: characterization of ligand binding and receptor-effector coupling of chick A1 and A3 adenosine receptors

Naunyn Schmiedebergs Arch Pharmacol. 2001 Jan;363(1):81-6. doi: 10.1007/s002100000340.

Abstract

We have reported previously the cloning and partial characterization of a chick A1 adenosine receptor expressed in the heart. We report herein the cloning of a chick A3 adenosine receptor and a comprehensive characterization of both the A1 and A3 receptors expressed in human embryonic kidney 293 cells. [125I]N6-(p-aminobenzyl)adenosine bound to both receptors with similar affinities and was used in competition studies. Although the selectivities of both agonists and antagonists were less than in other species, two antagonists, 3-ethyl-5-benzyl-2-methyl-6-phenyl-4-phenylethynal-(+/-)-dihydropyridine-3,5-dicarboxylate and 3,6-dichloro-2'-(isopropyloxy)-4'-methylflavone), were at least partially selective for A3 receptors while one antagonist [C8-(N-methylisopropyl)amine-N6-(5'endohydroxy)endonorboman-2-yl-9-methyladenine] was selective for A1 receptors. While both receptors coupled to the inhibition of adenylyl cyclase, we were unable to detect coupling of either receptor to phospholipase C or D.

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / metabolism
  • Adenosine / pharmacology
  • Adenosine-5'-(N-ethylcarboxamide) / pharmacology
  • Amino Acid Sequence
  • Animals
  • Base Sequence
  • Binding, Competitive / drug effects
  • Brain / metabolism
  • Cell Line
  • Chickens / genetics*
  • Cloning, Molecular
  • Cyclic AMP / metabolism
  • DNA, Complementary / chemistry
  • DNA, Complementary / genetics
  • DNA, Complementary / isolation & purification
  • DNA, Recombinant
  • Dihydropyridines / pharmacology
  • Gene Expression
  • Humans
  • Iodine Radioisotopes
  • Iodobenzenes / metabolism
  • Iodobenzenes / pharmacology
  • Ligands
  • Molecular Sequence Data
  • Phospholipase D / metabolism
  • Radioligand Assay
  • Receptor, Adenosine A3
  • Receptors, Purinergic P1 / drug effects
  • Receptors, Purinergic P1 / genetics*
  • Receptors, Purinergic P1 / metabolism
  • Sequence Analysis, DNA
  • Transfection
  • Type C Phospholipases / metabolism
  • Xanthines / pharmacology

Substances

  • DNA, Complementary
  • DNA, Recombinant
  • Dihydropyridines
  • Iodine Radioisotopes
  • Iodobenzenes
  • Ligands
  • MRS 1097
  • Receptor, Adenosine A3
  • Receptors, Purinergic P1
  • Xanthines
  • BW A1433
  • Adenosine-5'-(N-ethylcarboxamide)
  • 3-iodo-N(6)-4-aminobenzyladenosine
  • Cyclic AMP
  • Type C Phospholipases
  • Phospholipase D
  • Adenosine

Associated data

  • GENBANK/AF115332