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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.
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)…
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 nucleotide…
[3H]CGS 21680, a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain.
- M. Jarvis, R. Schulz, A. Hutchison, U. H. Do, M. Sills, M. Williams
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 December 1989
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.
Towards a revised nomenclature for P1 and P2 receptors.
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.
The adenosine/neutrophil paradox resolved: human neutrophils possess both A1 and A2 receptors that promote chemotaxis and inhibit O2 generation, respectively.
- B. Cronstein, L. Daguma, D. Nichols, A. Hutchison, M. Williams
- Biology, ChemistryThe Journal of clinical investigation
- 1 April 1990
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.
Challenges in the Search for Drugs to Treat Central Nervous System Disorders
Improving the success rate in CNS drug discovery requires a more pharmacometric-based approach, with a renewed emphasis on defining basic CNS function in intact animals and a more systematic in vivo screening of novel structures.
[3H]CGP 39653: a new N-methyl-D-aspartate antagonist radioligand with low nanomolar affinity in rat brain.
ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors: II. In vivo characterization.
- A. Bannon, M. Decker, S. Arneric
- Biology, PsychologyThe Journal of pharmacology and experimental…
- 1 May 1998
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.