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ADORA1  -  adenosine A1 receptor

Bos taurus

 
 
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High impact information on ADORA1

  • Guanine nucleotides decrease the binding of the adenosine A1 receptor agonist [3H]N6-cyclohexyladenosine ([3H]CHA) to guinea pig and bovine brain membranes by about 50% at 1--3 microM, while not affecting binding of the antagonist [3H]1,3-diethyl-8-phenylxanthine ([3H]DPX) to A1 receptors in bovine brain [1].
  • On the basis of a model we recently developed for the antagonist binding site of the adenosine A1 receptor (J. Med. Chem. 1990, 33, 1708-1713), it was predicted that 1H-imidazo[4,5-c]quinolin-4-amines would be antagonists of the A1 receptor [2].
  • Clathrin-coated vesicles purified from bovine brain express adenosine A1 receptor binding activity [3].
  • A series of 21 1,3-dialkylpyrazolo[4,3-d]pyrimidin-7-ones substituted in the 5-position with various phenyl substituents has been synthesized and found to have affinity for the adenosine A1 receptor [4].
  • A set of 56 8-phenylxanthines, previously tested for adenosine antagonism (adenosine A1 receptor affinity), was analyzed by quantitative structure-activity relationship (QSAR) techniques [5].
 

Biological context of ADORA1

  • This PKC dependent effect is unlikely to be via modulation of synaptosomal membrane potential or voltage-activated Ca2+ channels and not via a suppression of tonically active inhibitory adenosine A1 receptor, group II/III mGlu receptors or GABA(B) receptors [6].
 

Associations of ADORA1 with chemical compounds

  • An adenosine A2-receptor antagonist, 3,7-dimethyl-1-(2-propynyl) xanthine (DMPX; 1.0 and 100 nM), antagonized significantly the reduction of the TF activity and the adhesion induced by adenosine (1.0 mM), while 8-cyclopentyl-1,3-dimethylxanthine (CPDMX; 1.0 and 100 nM), an adenosine A1-receptor antagonist, did not affect it [7].

References

  1. Guanine nucleotide and cation regulation of the binding of [3H]cyclohexyladenosine and [3H]diethylphenylxanthine to adenosine A1 receptors in brain membranes. Goodman, R.R., Cooper, M.J., Gavish, M., Snyder, S.H. Mol. Pharmacol. (1982) [Pubmed]
  2. 1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. van Galen, P.J., Nissen, P., van Wijngaarden, I., IJzerman, A.P., Soudijn, W. J. Med. Chem. (1991) [Pubmed]
  3. Bovine brain coated vesicles contain adenosine A1 receptors. Presence of adenylate cyclase coupled to the receptor. Gonzalez-Calero, G., Martín, M., Cubero, A., Andrés, A. J. Neurochem. (1990) [Pubmed]
  4. Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists. Hamilton, H.W., Ortwine, D.F., Worth, D.F., Bristol, J.A. J. Med. Chem. (1987) [Pubmed]
  5. Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application. Hamilton, H.W., Ortwine, D.F., Worth, D.F., Badger, E.W., Bristol, J.A., Bruns, R.F., Haleen, S.J., Steffen, R.P. J. Med. Chem. (1985) [Pubmed]
  6. Group I mGlu receptors potentiate synaptosomal [3H]glutamate release independently of exogenously applied arachidonic acid. Reid, M.E., Toms, N.J., Bedingfield, J.S., Roberts, P.J. Neuropharmacology (1999) [Pubmed]
  7. Involvement of adenosine A2 receptors in the changes of tissue factor-dependent coagulant activity induced by polymorphonuclear leukocytes in endothelial cells. Watanabe, T., Tokuyama, S., Yasuda, M., Sasaki, T., Yamamoto, T. Jpn. J. Pharmacol. (2002) [Pubmed]
 
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