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Nomenclature and classification of purinoceptors.
The evidence is now compelling that ATP plays important physiological and/ or pathophysiological roles in a variety of biological systems, and the presence of receptors for ADP and adenosine (presumably A2) receptors exist on platelets is compelling. Expand
Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors.
Development of analgesic agents for the treatment of severe pain requires the identification of compounds that are devoid of opioid receptor liabilities. A potent (inhibition constant = 37 picomolar)Expand
P2 purinergic receptors: modulation of cell function and therapeutic potential.
In addition to its key role in cellular metabolism where it acts as a ubiquitous enzyme cofactor and as the key source of the cellular energy unique to phosphate bond formation, the purine nucleotideExpand
[3H]CGS 21680, a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain.
The present results indicate that [3H]CGS 21680 directly labels the high affinity A2 receptor in rat brain without the need to block binding activity at the A1 receptor. Expand
Towards a revised nomenclature for P1 and P2 receptors.
A revised nomenclature, essentially adopting the Abbracchio and Burnstock proposal, can now be proposed: G protein-coupled receptors termed P2Y purinoceptors, and intrinsic ion channels termed P 2X purinoceptorors. Expand
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.
A novel series of 3-pyridyl ether compounds which possess subnanomolar affinity for brain nA cholinergic channel modulators and differentially activate subtypes of neuronal nAChRs are reported. Expand
The adenosine/neutrophil paradox resolved: human neutrophils possess both A1 and A2 receptors that promote chemotaxis and inhibit O2 generation, respectively.
Evidence is reported that two distinct adenosine receptors are found on neutrophils (presumably the A1 and A2 receptors of other cell types) that modulate chemotaxis and O2- generation. Expand
[3H]CGP 39653: a new N-methyl-D-aspartate antagonist radioligand with low nanomolar affinity in rat brain.
Results suggest that [3H]CGP 39653 selectively binds to the NMDA receptor as an antagonist with high affinity and is currently the ligand of choice for labeling theNMDA receptor. Expand
Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist.
The data obtained indicate that CGS 12066B is a reasonably active 5HT1B site agonist, which due to its selectivity as compared to compounds such as TFMPP, will be a useful tool for evaluating the physiological role of such receptors in the mammalian CNS. Expand
ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors: II. In vivo characterization.
It is demonstrated that ABT-594 is a potent antinociceptive agent with full efficacy in models of acute and persistent pain and that these effects are mediated predominately by an action at central neuronal nAChRs. Expand