scholarly journals Synthesis and Pharmacological Evaluation of Identified and Putative Metabolites of the A1 Adenosine Receptor Antagonist 8-Cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine (CPFPX)

ChemMedChem ◽  
2017 ◽  
Vol 12 (10) ◽  
pp. 770-784
Author(s):  
Marcus H. Holschbach ◽  
Dirk Bier ◽  
Wiebke Sihver ◽  
Annette Schulze ◽  
Bernd Neumaier
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist ◽  
Pharmacological Evaluation

CPX, a selective A1-adenosine-receptor antagonist, regulates intracellular pH in cystic fibrosis cells

1995 ◽  
Vol 269 (1) ◽  
pp. C226-C233 ◽  
Author(s):  
V. Casavola ◽  
R. J. Turner ◽  
C. Guay-Broder ◽  
K. A. Jacobson ◽  
O. Eidelman ◽  
...  
Keyword(s):  
Cystic Fibrosis ◽  
Receptor Antagonist ◽  
Intracellular Ph ◽  
Adenosine Receptor ◽  
Ph Regulation ◽  
Cystic Fibrosis Transmembrane Regulator ◽  
Wild Type ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist ◽  
Cystic Fibrosis Transmembrane

The selective A1-adenosine-receptor antagonist, 8-cyclopentyl-1,3-dipropylxanthine (CPX), has been reported to activate Cl- efflux from cystic fibrosis cells, such as pancreatic CFPAC-1 and lung IB3 cells bearing the cystic fibrosis transmembrane regulator(delta F508) mutation, but has little effect on the same process in cells repaired by transfection with wild-type cystic fibrosis transmembrane regulator (O. Eidelman, C. Guay-Broder, P. J. M. van Galen, K. A. Jacobson, C. Fox, R. J. Turner, Z. I. Cabantchik, and H. B. Pollard. Proc. Natl. Acad. Sci. USA 89: 5562-5566, 1992). We report here that CPX downregulates Na+/H+ exchange activity in CFPAC-1 cells but has a much smaller effect on cells repaired with the wild-type gene. CPX also mildly decreases resting intracellular pH. In CFPAC-1 cells, this downregulation is dependent on the presence of adenosine, since pretreatment of the cells with adenosine deaminase blocks the CPX effect. We also show that, by contrast, CPX action on these cells does not lead to alterations in intracellular free Ca2+ concentration. We conclude that CPX affects pH regulation in CFPAC-1 cells, probably by antagonizing the tonic action of endogenous adenosine.

Improving cold resistance by selective A1 adenosine receptor antagonist in rats

1990 ◽  
Vol 183 (3) ◽  
pp. 681
Author(s):  
T.-F. Lee ◽  
D.-J. Li ◽  
K.A. Jacobson ◽  
C.-H. Wang
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
Cold Resistance ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist

Evaluation of radioiodinated 8-Cyclopentyl-3-[(E)-3-iodoprop-2-en-1-yl]-1-propylxanthine ([*I]CPIPX) as a new potential A1 adenosine receptor antagonist for SPECT

2003 ◽  
Vol 30 (6) ◽  
pp. 661-668 ◽  
Author(s):  
W. Sihver ◽  
M.H. Holschbach ◽  
D. Bier ◽  
W. Wutz ◽  
A. Schulze ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist

Synthesis of an o-Nitrobenzyl Attached A1 Adenosine Receptor Antagonist, a Prodrug Approach.

ChemInform ◽  
2003 ◽  
Vol 34 (47) ◽  
Author(s):  
HeXi Chang ◽  
Carol Ensinger ◽  
Robert D. McCargar ◽  
Bruno M. Vittimberga
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist

Sustained A1 Adenosine Receptor Antagonist Drug Release from Nanoparticles Functionalized by a Neural Tracing Protein

2021 ◽  
Author(s):  
Md. Musfizur Hassan ◽  
Malsha Hettiarachchi ◽  
Mohamed Kilani ◽  
Xiaohua Gao ◽  
Abdulghani Sankari ◽  
...  
Keyword(s):  
Drug Release ◽  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist ◽  
Neural Tracing

Characterization and Biodistribution of the Novel A1-Adenosine Receptor Antagonist [18F]CPFPX: Preclinical Studies Using Autoradioraphy and PET

NeuroImage ◽  
1998 ◽  
Vol 7 (4) ◽  
pp. A3
Author(s):  
M. Holschbach ◽  
C. Boy ◽  
H. Mühlensiepen ◽  
H. Herzog ◽  
J. Shah ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
Preclinical Studies ◽  
The Novel ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist

scholarly journals Quantitative analysis of the formation and diffusion of A1-adenosine receptor-antagonist complexes in single living cells

2004 ◽  
Vol 101 (13) ◽  
pp. 4673-4678 ◽  
Author(s):  
S. J. Briddon ◽  
R. J. Middleton ◽  
Y. Cordeaux ◽  
F. M. Flavin ◽  
J. A. Weinstein ◽  
...  
Keyword(s):  
Quantitative Analysis ◽  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
Living Cells ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist ◽  
Single Living Cells ◽  
And Diffusion ◽  
Single Living

Adenosine Reduces Glutamate Release in Rat Spinal Synaptosomes

2005 ◽  
Vol 103 (5) ◽  
pp. 1060-1065 ◽  
Author(s):  
Xinhui Li ◽  
James C. Eisenach
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
Glutamate Release ◽  
Receptor Activation ◽  
Spinal Nerve ◽  
Spinal Nerve Ligation ◽  
Dependent Manner ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist ◽  
Adenosine A1

Background A1 adenosine receptor activation reduces hypersensitivity in animal models of chronic pain, but intrathecal adenosine does not produce analgesia to acute noxious stimuli. Here, the authors test whether increased inhibition by adenosine of glutamate release from afferents after injury accounts for this difference. Methods Synaptosomes were prepared from the dorsal half of the lumbar spinal cord of normal rats or those with spinal nerve ligation. Glutamate release evoked by the TRPV-1 receptor agonist, capsaicin, was measured. Adenosine with or without adenosine A1 and A2 receptor antagonists was applied to determine the efficacy and mechanism of adenosine to reduce capsaicin-evoked glutamate release. Results Capsaicin produced a concentration-dependent glutamate release similarly in normal and nerve-injured rats. Capsaicin-evoked glutamate release was inhibited by adenosine or R-PIA (R-N6-(2- phenylisopropyl)-adenosine) in a concentration-dependent manner, with a threshold of 10 nm in both normal and nerve-ligated synaptosomes. Blockade of capsaicin-evoked glutamate release by adenosine was reversed similarly in synaptosomes from normal and spinal nerve-ligated animals by an A1 adenosine receptor antagonist DPCPX (8-cyclopentyl-1,3-dipropylxanthine) but not by an A2 adenosine receptor antagonist DMPX (3'7-dimethyl-1-proparaglyxanthine). Capsaicin-evoked glutamate release, as well as its inhibition by adenosine, did not differ between synaptosomes prepared from tissue ipsilateral and contralateral to spinal nerve ligation. Conclusion These observations confirm previous neurophysiologic studies that presynaptic adenosine A1 receptor activation inhibits glutamate release from primary afferents. This effect is unaltered after peripheral nerve injury and thereby is unlikely to account for the enhanced analgesic efficacy of intrathecal adenosine in this setting.

Sign in / Sign up

Export Citation Format

Share Document