Influence of the molecular structure of N6-(ω-aminoalkyl)adenosines on adenosine receptor affinity and intrinsic activity

Potent antagonists for the human adenosine A2B receptor. Derivatives of the triazolotriazine adenosine receptor antagonist ZM241385 with high affinity

“…Adenosine A 1 receptor affinities were determined on rat cortical membranes with [ 3 H]DPCPX as radioligand according to a protocol previously described [Pirovano et al, 1989]. Adenosine A 2A receptor affinities were determined on rat striatal membranes with [ 3 H]CGS21680 as radioligand according to Jarvis et al [1989].…”

Search for new antagonist ligands for adenosine receptors from QSAR point of view. How close are we?

“…119 The use of CODESSA software led to QSAR equations based on three descriptors for the adenosine A 1 receptor ligands with good statistical parameters. where MPCN is the minimum partial charge on a N atom and PP/D 2 is the relation between polarity parameter and square distance.…”

Elucidation of structure-activity relationships of 2-amino-3-benzoylthiophenes: Study of their allosteric enhancing vs. antagonistic activity on adenosine A1 receptors

“…Membranes were prepared according to the method of Lohse et al [1984], except that the membranes were incubated with 2 U/ml ADA at 37°C before storage, as described by Pirovano et al [1989]. Protein concentrations were measured with the BCA method [Smith et al, 1985].…”

“…Rat brain cortex membranes (30 µg/ml) were incubated for 1 h at 25°C in Tris/HCl Buffer (50 mM, pH 7.4) in the presence of 0.4 nM [ 1 H]DPCPX (K e 0.28 nM [Pirovano et al, 1989]) and 10 µM test compound. Nonspecific binding was determined in the presence of 10 µM CPA.…”