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A rapid filtration assay for soluble receptors using polyethylenimine-treated filters.
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Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes.
TLDR
The regional distribution of [3H]NECA binding and the affinities of adenosine agonists and antagonists for inhibition of binding indicate that the site labeled by [3NECA belongs to the high affinity, or A2a, subclass of A2 receptor.
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Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes.
TLDR
The binding and functional results are consistent with a model in which the enhancers bind preferentially to the agonist conformation of the A1 receptor, thereby shifting the receptor equilibrium in favor of agonist binding.
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Adenosine receptors and behavioral actions of methylxanthines.
TLDR
The data strongly suggest that the behavioral stimulant effects of methylxanthines involve a blockade of central adenosine receptors.
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Binding of the A1-selective adenosine antagonist 8-cyclopentyl-1,3-dipropylxanthine to rat brain membranes
TLDR
8-Cyclopentyl-1,3-dipropylxanthine (PD 116,948) is a very potent, very A1-selective adenosine antagonist, with a Ki of 0.46 nM involved in 3H-CHA binding to A1 receptors in rat whole brain membranes and 340 nM in3H-NECA binding in rat striatal membranes.
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Subclasses of angiotensin II binding sites and their functional significance.
TLDR
The results suggest the existence of two subclasses of angiotensin II binding sites, which differ in their tissue distribution and affinity for the nonpeptide ligands Dup 763, Exp 6803, and PD 123319.
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Rules for identifying potentially reactive or promiscuous compounds.
TLDR
A set of 275 rules, developed over an 18-year period, used to identify compounds that may interfere with biological assays, allowing their removal from screening sets are described.
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Adenosine receptors in brain membranes: binding of N6-cyclohexyl[3H]adenosine and 1,3-diethyl-8-[3H]phenylxanthine.
TLDR
Potencies of nucleosides and xanthines in competing for [3H]CHA sites indicate that specific binding is entirely to A1 adenosine receptors.
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Adenosine receptors in the central nervous system: relationship to the central actions of methylxanthines.
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Inhibition of protein kinase C by calphostin C is light-dependent.
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