Allosteric modulation of A(2A) adenosine receptors by amiloride analogues and sodium ions.
Allosteric modulation of A(3) adenosine receptors by a series of 3-(2-pyridinyl)isoquinoline derivatives.
- Z. Gao, J. V. van Muijlwijk-Koezen, A. Chen, C. Müller, A. IJzerman, K. Jacobson
- Biology, ChemistryMolecular Pharmacology
- 1 November 2001
Probing of structure-activity relationships suggested that a carbonyl group is essential for allosterism but preferred only for competitive antagonism, suggesting that the structural requirements forallosteric enhancement might be distinct from those forcompetitive antagonism.
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.
The human A(3) receptor is mutated at the site of a critical His residue in TM7, previously proposed to be involved in ligand recognition through interaction with the ribose moiety, to create a unique receptor mutant that would be activated by tailor-made synthetic ligands.
The A3 adenosine receptor agonist CF502 inhibits the PI3K, PKB/Akt and NF-kappaB signaling pathway in synoviocytes from rheumatoid arthritis patients and in adjuvant-induced arthritis rats.
Anti-nicotinic properties of anticholinergic antiparkinson drugs.
- Z. Gao, B. Y. Liu, W. Cui, L. J. Li, Q. Fan, C. Liu
- Biology, ChemistryThe Journal of pharmacy and pharmacology
The experiments demonstrate that the anticholinergic antiparkinson drugs and mecamylamine effectively antagonize nicotine- induced convulsion, but atropine does not; some of these drugs have competitive properties whereas others seem to have both competitive and non-competitive properties in antagonizing nicotine-induced convulsion in mice.
Site-directed mutagenesis studies of human A(2A) adenosine receptors: involvement of glu(13) and his(278) in ligand binding and sodium modulation.
Pharmacology: Anti‐nicotinic Properties of Anticholinergic Antiparkinson Drugs
The anti‐nicotinic properties of the clinically used anticholinergic antiparkinson drugs, benztropine, biperiden, caramiphen, ethopropazine, procyclidine and trihexyphenidyl are described.
Porcine pyridoxal kinase c-DNA cloning, expression and confirmation of its primary sequence.
Constitutive activation of A(3) adenosine receptors by site-directed mutagenesis.
- A. Chen, Z. Gao, D. Barak, B. Liang, K. Jacobson
- Biology, ChemistryBiochemical and Biophysical Research…
The results indicated that specific locations within the TMs proximal to the cytosolic region were responsible for constraining the receptor in a G protein-uncoupled conformation.
Effects of nicotine on 1-methyl-4-phenyl-1,2,5,6-tetrahydropyridine-induced depression of striatal dopamine content and spontaneous locomotor activity in C57 black mice.
It was demonstrated that the lethal effect of MPTP was also partly protected by the chronic Nicotine treatment, and the chronic nicotine treatment also significantly protected MPTP-depressed spontaneous locomotor activity in mice.