Characterization of the human brain putative A2B adenosine receptor expressed in Chinese hamster ovary (CHO.A2B4) cells

British Journal of Pharmacology
S P AlexanderS J Hill

Abstract

1. An [3H]-adenine pre-labelling methodology was employed to assay cyclic AMP generation by adenosine analogues in Chinese hamster ovary (CHO.A2B4) cells, transfected with cDNA which has been proposed to code for the human brain A2B adenosine receptor, and in guinea-pig cerebral cortical slices. 2. Adenosine analogues showing the following rank order of potency in the CHO.A2B4 cells (pD2 value): 5'-N-ethylcarboxamidoadenosine (NECA, 5.91) > adenosine (5.69) > 2-chloroadenosine (5.27) > N6-(2-(4-aminophenyl)-ethylamino)adenosine (APNEA, 4.06). The purportedly A2A-selective agonist, CGS 21680, failed to elicit a significant stimulation of cyclic AMP generation at concentrations up to 10 microM in CHO.A2B4 cells. In the guinea-pig cerebral cortex, NECA was more potent than APNEA with pD2 values of 5.91 and 4.60, respectively. 3. Of these agents, NECA was observed to exhibit the greatest intrinsic activity in CHO.A2B4 cells (ca. 10 fold stimulation of cyclic AMP), while, in comparison, maximal responses to adenosine (32% NECA response), 2-chloroadenosine (61%), and APNEA (73%) were reduced. 4. Antagonists of NECA-evoked cyclic AMP generation showed the rank order of apparent affinity (apparent pA2 value in CHO.A2B4 cells: guinea-pi...Continue Reading

References

Apr 1, 1992·British Journal of Pharmacology·D A KendallJ L Firth
Aug 31, 1992·Biochemical and Biophysical Research Communications·K D PierceJ Shine
Aug 1, 1987·Naunyn-Schmiedeberg's Archives of Pharmacology·M J LohseR A Olsson
Jan 1, 1987·Naunyn-Schmiedeberg's Archives of Pharmacology·R F BrunsC C Huang
Jan 1, 1987·Naunyn-Schmiedeberg's Archives of Pharmacology·R F BrunsS J Hays
Apr 1, 1974·Analytical Biochemistry·Y SalomonM Rodbell
Jan 1, 1994·British Journal of Pharmacology·M C Peakman, S J Hill
Nov 1, 1993·British Journal of Pharmacology·F HernándezS P Alexander
Nov 1, 1995·British Journal of Pharmacology·A Losinski, S P Alexander

❮ Previous
Next ❯

Citations

Feb 1, 2003·European Journal of Pharmacology·Carmen DinizJorge Gonçalves
Sep 5, 2003·European Journal of Pharmacology·John R FozardCedric Wolber
Dec 24, 1997·British Journal of Pharmacology·M MirabetR Franco
Oct 8, 1999·British Journal of Pharmacology·Z AnwarM R Boarder
Jan 11, 2003·British Journal of Pharmacology·C Jane DixonMichael R Boarder
Mar 21, 1998·Journal of Veterinary Pharmacology and Therapeutics·J Elliott, F E Brady
Nov 26, 2013·Purinergic Signalling·Geoffrey Burnstock
Mar 9, 2005·British Journal of Pharmacology·Mojtaba PanjehpourKarl-Norbert Klotz
Apr 4, 2006·European Journal of Pharmacology·P Tara PhelpsCraig C Correll
Jul 31, 2004·American Journal of Physiology. Heart and Circulatory Physiology·Yinghong ChenFrancisco Villarreal
Jul 19, 2006·Medicinal Research Reviews·Margot W BeukersAdriaan P Ijzerman
Feb 13, 2014·British Journal of Pharmacology·Stephen P H AlexanderUNKNOWN CGTP Collaborators
May 21, 2004·The Journal of Pharmacology and Experimental Therapeutics·C Jane DixonMichael R Boarder
Sep 24, 2014·Bioconjugate Chemistry·María Isabel BahamondeFrancisco Ciruela

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.