Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors

2000 ◽  
Vol 10 (3) ◽  
pp. 209-211 ◽  
Author(s):  
Pier Giovanni Baraldi ◽  
Barbara Cacciari ◽  
Romeo Romagnoli ◽  
Katia Varani ◽  
Stefania Merighi ◽  
...  
Keyword(s):  
Adenosine Receptors ◽  
Biological Evaluation ◽  
High Affinity

Corrigendum to “Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors”

2000 ◽  
Vol 10 (12) ◽  
pp. 1403
Author(s):  
Pier Giovanni Baraldi ◽  
Barbara Cacciari ◽  
Romeo Romagnoli ◽  
Katia Varani ◽  
Stefania Merighi ◽  
...  
Keyword(s):  
Adenosine Receptors ◽  
Biological Evaluation ◽  
High Affinity

Ribose-Modified Nucleosides as Ligands for Adenosine Receptors:  Synthesis, Conformational Analysis, and Biological Evaluation of 1‘-C-Methyl Adenosine Analogues

2002 ◽  
Vol 45 (6) ◽  
pp. 1196-1202 ◽  
Author(s):  
Loredana Cappellacci ◽  
Grazia Barboni ◽  
Micaela Palmieri ◽  
Michela Pasqualini ◽  
Mario Grifantini ◽  
...  
Keyword(s):  
Conformational Analysis ◽  
Adenosine Receptors ◽  
Biological Evaluation ◽  
Modified Nucleosides ◽  
Adenosine Analogues

scholarly journals Adenosine Receptors of Cerebral Microvessels and Choroid Plexus

1986 ◽  
Vol 6 (4) ◽  
pp. 463-470 ◽  
Author(s):  
Rajesh N. Kalaria ◽  
Sami I. Harik
Keyword(s):  
Cerebral Cortex ◽  
Ligand Binding ◽  
Choroid Plexus ◽  
Adenosine Receptors ◽  
Binding Sites ◽  
Specific Binding ◽  
Cerebral Microvessels ◽  
High Affinity ◽  
Receptor Sites ◽  
Ligand Binding Sites

We studied, by ligand binding methods, the two adenosine receptors, A, and A2, in rat and pig cerebral microvessels and pig choroid plexus. Ligand binding to cerebral microvessels was compared with that to membranes of the cerebral cortex. [3H]Cyclohexyladenosine and [3H]l-phenylisopropyladenosine were the ligands used for A1-receptors, and [3H]5'- N-ethylcarboxamide adenosine ([3H]NECA) was used to assess A2-receptors. We report that cerebral microvessels and choroid plexus exhibit specific [3H]NECA binding, but have no appreciable A1-receptor ligand binding sites. Specific binding of [3H]NECA to cerebral microvessels, choroid plexus, and cerebral cortex was saturable and suggested the existence of two classes of A2-receptor sites: high-affinity ( Kd ∼ 250 n M) and low-affinity ( Kd ∼ 1–2 μ M) sites. The Kd and Bmax of NECA binding to cerebral microvessels and cerebral cortex were similar within each species. Our results, indicating the existence of A2-receptors in cerebral microvessels, are consistent with results of increased adenylate cyclase activity by adenosine and some of its analogues in these microvessels.

scholarly journals Functionalized congeners of 1,3-dialkylxanthines: preparation of analogs with high affinity for adenosine receptors

1985 ◽  
Vol 28 (9) ◽  
pp. 1334-1340 ◽  
Author(s):  
Kenneth A. Jacobson ◽  
Kenneth L. Kirk ◽  
William L. Padgett ◽  
John W. Daly
Keyword(s):  
Adenosine Receptors ◽  
High Affinity

8-Cyclopentyl-1,3-dipropylxanthine (DPCPX) ? a selective high affinity antagonist radioligand for A1 adenosine receptors

1987 ◽  
Vol 336 (2) ◽  
pp. 204-210 ◽  
Author(s):  
Martin J. Lohse ◽  
Karl-Norbert Klotz ◽  
Jutta Lindenborn-Fotinos ◽  
Martin Reddington ◽  
Ulrich Schwabe ◽  
...  
Keyword(s):  
Adenosine Receptors ◽  
High Affinity ◽  
A1 Adenosine Receptors

Synthesis and preliminary biological evaluation of a cyclic somatostatin analog with high affinity to sst1–5

2005 ◽  
Author(s):  
Christos Petrou ◽  
Anastasia Nikolopoulou ◽  
Vassiliki Magafa ◽  
Berthold Nock ◽  
Theodosia Maina ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Somatostatin Analog ◽  
High Affinity
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