Penetration of adenosine antagonists into mouse brain as determined by ex vivo binding.

PubWeight™: 1.17‹?› | Rank: Top 10%

🔗 View Article (PMC 3425645)

Published in Biochem Pharmacol on February 18, 1992

Authors

J Baumgold1, O Nikodijevic, K A Jacobson

Author Affiliations

1: Department of Pharmacology and of Radiology, George Washington University, Washington, DC 20037.

Articles citing this

8-(3-Chlorostyryl)caffeine (CSC) is a selective A2-adenosine antagonist in vitro and in vivo. FEBS Lett (1993) 1.47

Restoring auditory cortex plasticity in adult mice by restricting thalamic adenosine signaling. Science (2017) 1.39

Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists. J Med Chem (1992) 0.97

Adenosine receptor prodrugs: synthesis and biological activity of derivatives of potent, A1-selective agonists. J Pharm Sci (1994) 0.96

Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain. J Med Chem (2013) 0.96

Xanthines as adenosine receptor antagonists. Handb Exp Pharmacol (2011) 0.96

A detailed behavioral analysis of the acute motor effects of caffeine in the rat: involvement of adenosine A1 and A2A receptors. Psychopharmacology (Berl) (2005) 0.93

Anxiolytic activity of adenosine receptor activation in mice. Br J Pharmacol (1995) 0.90

Adenosine mediates decreased cerebral metabolic rate and increased cerebral blood flow during acute moderate hypoxia in the near-term fetal sheep. J Physiol (2003) 0.89

Regulation of hippocampal cannabinoid CB1 receptor actions by adenosine A1 receptors and chronic caffeine administration: implications for the effects of Δ9-tetrahydrocannabinol on spatial memory. Neuropsychopharmacology (2010) 0.88

Characterization of the adenosine receptors mediating hypothermia in the conscious mouse. Br J Pharmacol (1994) 0.85

Adenosine mediates metabolic and cardiovascular responses to hypoxia in fetal sheep. J Physiol (1995) 0.85

Psychostimulant pharmacological profile of paraxanthine, the main metabolite of caffeine in humans. Neuropharmacology (2012) 0.84

Adenosine A(2A) agonist and A(2B) antagonist mediate an inhibition of inflammation-induced contractile disturbance of a rat gastrointestinal preparation. Purinergic Signal (2009) 0.81

Mediation of the neuroprotective action of R-phenylisopropyl-adenosine through a centrally located adenosine A1 receptor. Br J Pharmacol (1993) 0.80

Inhibition by the adenosine analogue, (R-)-N6-phenylisopropyladenosine, of kainic acid neurotoxicity in rat hippocampus after systemic administration. Br J Pharmacol (1993) 0.77

Aminophylline suppresses stress-induced visceral hypersensitivity and defecation in irritable bowel syndrome. Sci Rep (2017) 0.75

Binding of angiotensin antagonists to rat liver and brain membranes measured ex vivo. Br J Pharmacol (1993) 0.75

Poster communications. Br J Pharmacol (1993) 0.75

Alkylxanthine adenosine antagonists and epileptiform activity in rat hippocampal slices in vitro. Exp Brain Res (1997) 0.75

Articles cited by this

Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol (1973) 47.81

Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes. Mol Pharmacol (1986) 4.15

Adenosine receptors and behavioral actions of methylxanthines. Proc Natl Acad Sci U S A (1981) 2.66

Adenosine receptors in the central nervous system: relationship to the central actions of methylxanthines. Life Sci (1981) 2.58

Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors. J Med Chem (1985) 2.52

Binding of the A1-selective adenosine antagonist 8-cyclopentyl-1,3-dipropylxanthine to rat brain membranes. Naunyn Schmiedebergs Arch Pharmacol (1987) 2.36

1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors. J Med Chem (1985) 1.87

[3H]xanthine amine congener of 1,3-dipropyl-8-phenylxanthine: an antagonist radioligand for adenosine receptors. Proc Natl Acad Sci U S A (1986) 1.85

Behavioral effects of A1- and A2-selective adenosine agonists and antagonists: evidence for synergism and antagonism. J Pharmacol Exp Ther (1991) 1.31

3,7-Dimethyl-1-propargylxanthine: a potent and selective in vivo antagonist of adenosine analogs. Life Sci (1988) 1.26

Antagonism of the cardiovascular effects of adenosine by caffeine or 8-(p-sulfophenyl)theophylline. J Pharmacol Exp Ther (1987) 1.13

Theophylline concentration in the extracellular space of the rat brain: measurement by microdialysis and relation to behaviour. Eur J Pharmacol (1990) 1.00

Cerebral ischemia in gerbils: postischemic administration of cyclohexyl adenosine and 8-sulfophenyl-theophylline. J Mol Neurosci (1990) 0.98

Inhibition of rat ventricular automaticity by adenosine. Am J Physiol (1985) 0.87

Nimodipine levels in gerbil brain following parenteral drug administration. J Neurosurg (1985) 0.87

Direct measurement of muscarinic agents in the central nervous system of mice using ex vivo binding. Eur J Pharmacol (1989) 0.85

Caffeine-induced behavioural stimulation is dose- and concentration-dependent. Br J Pharmacol (1990) 0.83

Potent convulsant actions of the adenosine receptor antagonist, xanthine amine congener (XAC). Life Sci (1989) 0.80

Articles by these authors

(truncated to the top 100)

International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors. Pharmacol Rev (2001) 9.90

Nomenclature and classification of purinoceptors. Pharmacol Rev (1994) 5.32

Direct observation of brownian motion of lipids in a membrane. Proc Natl Acad Sci U S A (1991) 3.91

Diffusion of injected macromolecules within the cytoplasm of living cells. Proc Natl Acad Sci U S A (1981) 3.61

125I-4-aminobenzyl-5'-N-methylcarboxamidoadenosine, a high affinity radioligand for the rat A3 adenosine receptor. Mol Pharmacol (1994) 2.65

Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors. J Med Chem (1985) 2.52

Structural mosaicism on the submicron scale in the plasma membrane. Biophys J (1998) 2.50

The Concise Guide to PHARMACOLOGY 2013/14: overview. Br J Pharmacol (2013) 2.48

Unconfined lateral diffusion and an estimate of pericellular matrix viscosity revealed by measuring the mobility of gold-tagged lipids. J Cell Biol (1993) 2.47

Adenosine A3 receptor stimulation and cerebral ischemia. Eur J Pharmacol (1994) 2.33

Spatial Fourier analysis of video photobleaching measurements. Principles and optimization. Biophys J (1991) 2.13

Functionalized congeners of adenosine: preparation of analogues with high affinity for A1-adenosine receptors. J Med Chem (1985) 2.12

2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors. J Med Chem (1994) 2.10

Towards a revised nomenclature for P1 and P2 receptors. Trends Pharmacol Sci (1997) 2.09

Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem (1995) 1.92

A binding site model and structure-activity relationships for the rat A3 adenosine receptor. Mol Pharmacol (1994) 1.87

Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands. J Med Chem (2000) 1.85

[3H]xanthine amine congener of 1,3-dipropyl-8-phenylxanthine: an antagonist radioligand for adenosine receptors. Proc Natl Acad Sci U S A (1986) 1.85

Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate. J Med Chem (1993) 1.84

Competitive and selective antagonism of P2Y1 receptors by N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate. Br J Pharmacol (1998) 1.80

Differential effects of P2-purinoceptor antagonists on phospholipase C- and adenylyl cyclase-coupled P2Y-purinoceptors. Br J Pharmacol (1994) 1.77

Functionalized congeners of 1,3-dipropyl-8-phenylxanthine: potent antagonists for adenosine receptors that modulate membrane adenylate cyclase in pheochromocytoma cells, platelets and fat cells. Life Sci (1986) 1.69

Role of the extracellular loops of G protein-coupled receptors in ligand recognition: a molecular modeling study of the human P2Y1 receptor. Biochemistry (1999) 1.64

A mutational analysis of residues essential for ligand recognition at the human P2Y1 receptor. Mol Pharmacol (1997) 1.63

A physiological role of the adenosine A3 receptor: sustained cardioprotection. Proc Natl Acad Sci U S A (1998) 1.63

Adenosine A1 and A2 receptors: structure--function relationships. Med Res Rev (1992) 1.62

Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors. J Med Chem (1998) 1.61

Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. J Med Chem (1998) 1.61

Direct preconditioning of cultured chick ventricular myocytes. Novel functions of cardiac adenosine A2a and A3 receptors. J Clin Invest (1996) 1.57

A2A adenosine receptors from rat striatum and rat pheochromocytoma PC12 cells: characterization with radioligand binding and by activation of adenylate cyclase. Mol Pharmacol (1992) 1.57

A functionalized congener approach to adenosine receptor antagonists: amino acid conjugates of 1,3-dipropylxanthine. Mol Pharmacol (1986) 1.55

Glutamate residues in the second extracellular loop of the human A2a adenosine receptor are required for ligand recognition. Mol Pharmacol (1996) 1.54

The role of amino acids in extracellular loops of the human P2Y1 receptor in surface expression and activation processes. J Biol Chem (1999) 1.54

Probing the adenosine receptor with adenosine and xanthine biotin conjugates. FEBS Lett (1985) 1.52

Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. J Med Chem (1997) 1.51

Direct measurement of lateral transport in membranes by using time-resolved spatial photometry. Proc Natl Acad Sci U S A (1985) 1.51

Identification of the A2 adenosine receptor binding subunit by photoaffinity crosslinking. Proc Natl Acad Sci U S A (1989) 1.50

Molecular probes for extracellular adenosine receptors. Biochem Pharmacol (1987) 1.47

Apparent affinity of some 8-phenyl-substituted xanthines at adenosine receptors in guinea-pig aorta and atria. Br J Pharmacol (1987) 1.45

Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. J Med Chem (2000) 1.44

Distinct pathways of desensitization of A1- and A2-adenosine receptors in DDT1 MF-2 cells. Mol Pharmacol (1991) 1.42

A new high affinity, iodinated adenosine receptor antagonist as a radioligand/photoaffinity crosslinking probe. Mol Pharmacol (1987) 1.42

Species differences in structure-activity relationships of adenosine agonists and xanthine antagonists at brain A1 adenosine receptors. FEBS Lett (1986) 1.42

G protein-dependent activation of phospholipase C by adenosine A3 receptors in rat brain. Mol Pharmacol (1995) 1.40

Induction of cortical oscillations in spreading cells by depolymerization of microtubules. Cell Motil Cytoskeleton (2001) 1.35

Modelling the P2Y purinoceptor using rhodopsin as template. Drug Des Discov (1995) 1.35

Hydrophilic side chains in the third and seventh transmembrane helical domains of human A2A adenosine receptors are required for ligand recognition. Mol Pharmacol (1996) 1.33

Cloning, expression, and characterization of the unique bovine A1 adenosine receptor. Studies on the ligand binding site by site-directed mutagenesis. J Biol Chem (1992) 1.32

Acyclic and cyclopropyl analogues of adenosine bisphosphate antagonists of the P2Y1 receptor: structure-activity relationships and receptor docking. J Med Chem (2001) 1.32

The A2 adenosine receptor: guanine nucleotide modulation of agonist binding is enhanced by proteolysis. Mol Pharmacol (1991) 1.32

Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists. J Med Chem (1998) 1.32

Behavioral effects of A1- and A2-selective adenosine agonists and antagonists: evidence for synergism and antagonism. J Pharmacol Exp Ther (1991) 1.31

Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. J Med Chem (1998) 1.31

Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. J Med Chem (1996) 1.31

Activation of hippocampal adenosine A3 receptors produces a desensitization of A1 receptor-mediated responses in rat hippocampus. J Neurosci (1997) 1.29

Identification of potent P2Y-purinoceptor agonists that are derivatives of adenosine 5'-monophosphate. Br J Pharmacol (1996) 1.27

A novel cardioprotective function of adenosine A1 and A3 receptors during prolonged simulated ischemia. Am J Physiol (1997) 1.27

Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications. Bioorg Med Chem Lett (2001) 1.26

Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors. J Med Chem (1995) 1.26

[3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochem Pharmacol (2001) 1.25

Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists. J Med Chem (1999) 1.25

Molecular modeling of adenosine receptors. I. The ligand binding site on the A1 receptor. Drug Des Discov (1992) 1.25

Induction of apoptosis in HL-60 human promyelocytic leukemia cells by adenosine A(3) receptor agonists. Biochem Biophys Res Commun (1996) 1.23

Use of the triazolotriazine [3H]ZM 241385 as a radioligand at recombinant human A2B adenosine receptors. Drug Des Discov (1999) 1.21

Conjugates of catecholamines. 1. N-alkyl-functionalized carboxylic acid congeners and amides related to isoproterenol. J Med Chem (1983) 1.20

A mouse model for vitiligo. J Invest Dermatol (1986) 1.19

Studies on the mechanism of polyethylene glycol-mediated cell fusion using fluorescent membrane and cytoplasmic probes. J Cell Biol (1983) 1.18

Allosteric modulation of A(3) adenosine receptors by a series of 3-(2-pyridinyl)isoquinoline derivatives. Mol Pharmacol (2001) 1.18

High affinity acylating antagonists for the A1 adenosine receptor: identification of binding subunit. Mol Pharmacol (1988) 1.17

Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors. J Biol Chem (1994) 1.16

A [3H]amine congener of 1,3-dipropyl-8-phenylxanthine. A new radioligand for A2 adenosine receptors of human platelets. FEBS Lett (1986) 1.16

Activation of A3 adenosine receptors on human eosinophils elevates intracellular calcium. Blood (1996) 1.14

125I-4-(2-[7-amino-2-[2-furyl][1,2,4]triazolo[2,3-a][1,3,5] triazin-5-yl-amino]ethyl)phenol, a high affinity antagonist radioligand selective for the A2a adenosine receptor. Mol Pharmacol (1995) 1.13

Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem (1996) 1.13

Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors. J Med Chem (2001) 1.12

Distinct cardioprotective effects of adenosine mediated by differential coupling of receptor subtypes to phospholipases C and D. FASEB J (2000) 1.12

Cardioprotective effects of adenosine A1 and A3 receptor activation during hypoxia in isolated rat cardiac myocytes. Mol Cell Biochem (2001) 1.11

Postischemic administration of adenosine amine congener (ADAC): analysis of recovery in gerbils. Eur J Pharmacol (1996) 1.11

Site-directed mutagenesis studies of human A(2A) adenosine receptors: involvement of glu(13) and his(278) in ligand binding and sodium modulation. Biochem Pharmacol (2000) 1.11

Chronic administration of selective adenosine A1 receptor agonist or antagonist in cerebral ischemia. Eur J Pharmacol (1994) 1.11

The A3 adenosine receptor mediates cell spreading, reorganization of actin cytoskeleton, and distribution of Bcl-XL: studies in human astroglioma cells. Biochem Biophys Res Commun (1997) 1.10

Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists. J Med Chem (1997) 1.09

Reply to: 'the discovery of a new class of synaptic transmitters in smooth muscle fifty years ago and amelioration of coronary artery thrombosis'. Acta Physiol (Oxf) (2013) 1.09

Demonstration of distinct agonist and antagonist conformations of the A1 adenosine receptor. J Biol Chem (1989) 1.09

Characterization of the locomotor depression produced by an A2-selective adenosine agonist. FEBS Lett (1990) 1.08

Effects of chronic administration of adenosine A1 receptor agonist and antagonist on spatial learning and memory. Eur J Pharmacol (1993) 1.08

Acyclic analogues of deoxyadenosine 3',5'-bisphosphates as P2Y(1) receptor antagonists. J Med Chem (2000) 1.08

Conjugates of catecholamines. II. In vitro and in vivo pharmacological activity of N-alkyl-functionalized carboxylic acid congeners and amides related to isoproterenol. Mol Pharmacol (1983) 1.08

Demonstration of both A1 and A2 adenosine receptors in DDT1 MF-2 smooth muscle cells. Mol Pharmacol (1990) 1.07

Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists. J Med Chem (1999) 1.07

6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem (1996) 1.06

The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family. Bioorg Med Chem Lett (2000) 1.06

Selective ligands for rat A3 adenosine receptors: structure-activity relationships of 1,3-dialkylxanthine 7-riboside derivatives. J Med Chem (1994) 1.05

Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor. FASEB J (1998) 1.04

A1 adenosine-receptor antagonists activate chloride efflux from cystic fibrosis cells. Proc Natl Acad Sci U S A (1992) 1.03

18F-labeled insulin: a prosthetic group methodology for incorporation of a positron emitter into peptides and proteins. Biochemistry (1989) 1.03

Induction of apoptosis in cardiac myocytes by an A3 adenosine receptor agonist. Exp Cell Res (1998) 1.03

Activation of the A3 adenosine receptor affects cell cycle progression and cell growth. Naunyn Schmiedebergs Arch Pharmacol (2000) 1.02

Cerebral ischemia in gerbils: effects of acute and chronic treatment with adenosine A2A receptor agonist and antagonist. Eur J Pharmacol (1995) 1.02

Chronic caffeine alters the density of adenosine, adrenergic, cholinergic, GABA, and serotonin receptors and calcium channels in mouse brain. Cell Mol Neurobiol (1993) 1.02