Forskolin: unique diterpene activator of adenylate cyclase in membranes and in intact cells.
- K. Seamon, W. Padgett, J. Daly
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 1 June 1981
F Forskolin would appear to activate adenylate cyclase through a unique mechanism involving both direct activation of the enzyme and facilitation or potentiation of the modulation of enzyme activity by receptors or the guanyl nucleotide-binding subunit, or both.
8‐(3‐Chlorostyryl)caffeine (CSC) is a selective A2‐adenosine antagonist in vitro and in vivo
- K. Jacobson, O. Nikodijević, W. Padgett, C. Gallo-Rodriguez, M. Maillard, J. Daly
- BiologyFEBS Letters
- 24 May 1993
Subclasses of adenosine receptors in the central nervous system: Interaction with caffeine and related methylxanthines
- J. Daly, P. Butts-Lamb, W. Padgett
- Biology, ChemistryCellular and molecular neurobiology
- 1 March 1983
Caffeine and other methylxanthines antagonize effectively both A1- and A2-adenosine receptors in brain perparations, while 1-Methylxanthine is more potent than caffeine in rat cerebral cortical membranes, while 3-methylXanthine and 7-methyl Xanthine are less potent than caffeine.
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
- J. Daly, W. Padgett, M. Shamim, P. Butts-Lamb, J. Waters
- Chemistry, BiologyJournal of Medicinal Chemistry
- 1 April 1985
A series of 8-(substituted phenyl) derivatives of theophylline and other 1,3-dialkylxanthines were evaluated for potency and selectivity as antagonists at A1- and A2-adenosine receptors in brain…
A2A adenosine receptors from rat striatum and rat pheochromocytoma PC12 cells: characterization with radioligand binding and by activation of adenylate cyclase.
- I. Hide, W. Padgett, K. Jacobson, J. Daly
- Biology, ChemistryMolecular Pharmacology
- 1 February 1992
It appears that a lower affinity functional receptor, probably an A2B receptor, is present in PC12 cells and PC12 cell membranes, whereas such a functional low affinity receptor is not detectable in striatal membrane.
Cyclic AMP-generating systems: regional differences in activation by adrenergic receptors in rat brain
- J. Daly, W. Padgett, C. Creveling, D. Cantacuzene, K. Kirk
- BiologyJournal of Neuroscience
- 1 January 1981
The results indicate that the interactive control of cyclic AMP-generating systems by alpha-adrenergic, beta- adrenergic, adenosine, and histamine receptors differs significantly among rat brain regions.
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors.
- K. Jacobson, K. Kirk, W. Padgett, J. Daly
- Chemistry, BiologyJournal of Medicinal Chemistry
- 1 September 1985
The potency of 8-phenyl-1,3-dialkylxanthine was markedly affected by structural changes distal to the primary pharmacophore, which resulted in up to 145-fold more active at A1 receptors than at A2 receptors.
Caffeine and theophylline analogues: correlation of behavioral effects with activity as adenosine receptor antagonists and as phosphodiesterase inhibitors.
- O. Choi, M. Shamim, W. Padgett, J. Daly
- Biology, ChemistryLife Science
- 1988
Activation of Cyclic AMP‐Generating Systems in Brain Membranes and Slices by the Diterpene Forskolin: Augmentation of Receptor‐Mediated Responses
- J. Daly, W. Padgett, K. Seamon
- Biology, ChemistryJournal of Neurochemistry
- 1 February 1982
The activation of cyclic AMP systems by forskolin is rapid and reversible, and appears to involve both direct activation of adenylate cyclase and facilitation and/or enhancement of receptor‐mediated activation of the enzyme.
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
- M. Shamim, D. Ukena, W. Padgett, J. Daly
- Chemistry, BiologyJournal of Medicinal Chemistry
- 1 June 1989
8-Cycloalkyl substituents (cyclopentyl, cyclohexyl) markedly increase activity of caffeine and 1,3-dipropyl-7-methylxanthine at the A2 receptor, but is not as selective for the rat PC12 cell A2 receptors.
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