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Measurement of guanine nucleotide-binding protein activation by A1 adenosine receptor agonists in bovine brain membranes: stimulation of guanosine-5'-O-(3-[35S]thio)triphosphate binding.
Signal transduction by A1 adenosine receptors was investigated by measuring the modulation by adenosine agonists of guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTP[S]) binding to guanineExpand
Interaction of full and partial agonists of the A1 adenosine receptor with receptor/G protein complexes in rat brain membranes.
Full and partial agonists of the A1 adenosine receptor were characterized with respect to their influence on G protein activation and their thermodynamic parameters of receptor binding in rat brainExpand
Characterization of a G protein-coupled receptor for nicotinic acid.
Nicotinic acid is a lipid-lowering agent widely used to treat hypertriglyceridemia and to elevate low high density lipoprotein levels. However, the underlying mechanisms are poorly understood. InExpand
Thermodynamically distinct high and low affinity states of the A1 adenosine receptor induced by G protein coupling and guanine nucleotide ligation states of G proteins
The influence of the receptor‐G protein coupling state and the guanine nucleotide ligation state of the G protein on the binding mechanism of A1 adenosine receptor ligands has been investigated inExpand
Affinity of central adenosine A1 receptors is decreased in spontaneously hypertensive rats.
Functional defects in purinergic neurotransmission have been related to the development of arterial hypertension in spontaneously hypertensive rats. In order to elucidate the molecular basis of thisExpand
N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.
A number of cycloalkyl substituents (from C-3 to C-8) have been introduced on the 6-amino group of adenosine, 1-deazaadenosine, and 2'-deoxyadenosine, bearing or not a chlorine atom at theExpand
Synthesis and biological evaluation of disubstituted N6-cyclopentyladenine analogues: the search for a neutral antagonist with high affinity for the adenosine A1 receptor.
Novel 3,8- and 8,9-disubstituted N(6)-cyclopentyladenine derivatives were synthesised in moderate overall yield from 6-chloropurine. The derivatives were made in an attempt to find a new neutralExpand
Pharmacological properties of adenosine receptors and adenosine binding proteins
Two major subtypes of adenosine receptors occur in different tissues which have been distinguished by pharmacological and biochemical criteria. The A1 adenosine receptor has a high‐affinity forExpand
Characterization of Membrane‐Bound and Solubilized High‐Affinity Binding Sites for 5′‐N‐Ethylcarboxamido[3H]adenosine from Bovine Cerebral Cortex
Abstract: A high‐affinity binding site for 5′‐N‐ethylcarboxamido[3H]adenosine ([3H]NECA) from bovine cerebral cortex has been characterized in its membrane‐bound and solubilized state after gelExpand
Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.
Some 8-alkynyladenosines were synthesized and evaluated for their adenosine receptor activity, utilizing radioligand binding studies (A(1), A(2A), A(3)) or adenylyl cyclase activity assays (A(2B)).Expand