Adenosine A<sub>2B</sub>‐receptor‐mediated cyclic AMP accumulation in primary rat astrocytes

Peakman, Marie‐Claire; Hill, Stephen J.

doi:10.1111/j.1476-5381.1994.tb14043.x

Cited by 92 publications

(66 citation statements)

References 38 publications

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“…The A 2B AR is positively coupled to both adenylyl cyclase and PLC [17][18][19][20] . Results indicate that the activation of PLC, through G q proteins, mediates many of the important functions of A 2B ARs 21,22 .…”

Section: Ar Signalling Pathways and Regulationmentioning

confidence: 99%

Adenosine receptors as therapeutic targets

Jacobson

Gao

2006

Nat Rev Drug Discov

1,276

1,361

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Adenosine receptors are major targets of caffeine, the most commonly consumed drug in the world. There is growing evidence that they could also be promising therapeutic targets in a wide range of conditions, including cerebral and cardiac ischaemic diseases, sleep disorders, immune and inflammatory disorders and cancer. After more than three decades of medicinal chemistry research, a considerable number of selective agonists and antagonists of adenosine receptors have been discovered, and some have been clinically evaluated, although none has yet received regulatory approval. However, recent advances in the understanding of the roles of the various adenosine receptor subtypes, and in the development of selective and potent ligands, as discussed in this review, have brought the goal of therapeutic application of adenosine receptor modulators considerably closer.

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Section: Ar Signalling Pathways and Regulationmentioning

confidence: 99%

Adenosine receptors as therapeutic targets

Jacobson

Gao

2006

Nat Rev Drug Discov

1,276

1,361

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“…The the human homologue of the A2B adenosine receptor preisfected human viously identified pharmacologically in the guinea-pig brain, I to the values guinea-pig aorta and rat astrocytes (Hema'ndez et al, 1993; .96-4.89, HerAlexander et al, 1994b;Peakman & Hill, 1994 …”

Section: _3mentioning

confidence: 99%

“…Chinese hamster ovary (CHO.K1) cells transfected with cDNA coding for the putative human A2B adenosine receptor were generated as previously described (Pierce et al, 1992) (Peakman & Hill, 1994 (Lupica et al, 1990) failed to stimulate cyclic AMP generation significantly at concentrations below 10 gM (Figure la). Analysis of concentrationresponse profiles to adenosine in the presence of the purine nucleoside uptake inhibitor, dipyrimadole (1 uM), showed no change in basal cyclic AMP levels (control 0.26+0.02; dipyrimadole 0.26 + 0.02% conversion; n = 3), pD2 (control 5.38+0.56; dipyrimadole 5.76+0.18; n=3) or maximal response to adenosine (control 39+6; dipyrimadole 49+5% 100 gM NECA response; n = 3).…”

Section: Cell Culturementioning

confidence: 99%

“…ceptors which we have recently characterized in rat astrocytes and guinea-pig brain mediating a stimulation of cyclic AMP accumulation were unresponsive to concentrations of CGS 21680 below 10 gM (Hernandez et al, 1993;Alexander et al, 1994b;Peakman & Hill, 1994). Similarly, PD 155,199 (A1: A2A-selective) and DPCPX (Al-selective) were poor antagonists at these receptors.…”

Section: Introductionmentioning

confidence: 99%

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Characterization of the human brain putative A_2B adenosine receptor expressed in Chinese hamster ovary (CHO.A_2B4) cells

Alexander

Cooper

Shine

et al. 1996

British J Pharmacology

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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. 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-pig cerebral cortex): XAC (7.89: 7.46)> CGS 15943 (7.75: 7.33)>DPCPX (7.16: 6.91)>PD 115,199 (6.95: 6.39)>8FB-PTP (6.52: 6.55)>3-propylxanthine (4.63: 4.59).5 We conclude that, using the agents tested, the A2B adenosine receptor cloned from human brain expressed in Chinese hamster ovary cells exhibits an identical pharmacological profile to native A2B receptors in guinea-pig brain.

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“…Accumulation of [3H]-cyclic AMP Cyclic AMP accumulation was investigated by the method of Peakman & Hill (1994). Cells were washed twice with Hanks HEPES buffer and then incubated for 2 h at 37C in 1 ml per well buffer containing 2 yICi per well 8-[3H]-adenine.…”

Section: Inositol Phospholipid Hydrolysismentioning

confidence: 99%

Endogenous expression of histamine H₁ receptors functionally coupled to phosphoinositide hydrolysis in C6 glioma cells: regulation by cyclic AMP

Peakman

Hill

1994

British J Pharmacology

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4 Elevation of intracellular cyclic AMP accumulation with forskolin (10 gM, EC50 = 0.3 ItM), isoprenaline (1 gtM, EC0=4 nM) or rolipram (0.5 mM), significantly reduced the histamine-mediated (0.1 mM) inositol phosphate response by 37%, 43% and 26% respectively. In contrast, 1,9-dideoxyforskolin did not increase cyclic AMP accumulation and had no effect on the phosphoinositide response to histamine.5 These data indicate the presence of functionally coupled, endogenous histamine HI receptors in C6 glioma cells. Furthermore, the results also indicate that HI receptor-mediated phospholipid hydrolysis is inhibited by the elevation of cyclic AMP levels in these cells.

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Adenosine A_2B‐receptor‐mediated cyclic AMP accumulation in primary rat astrocytes

Cited by 92 publications

References 38 publications

Adenosine receptors as therapeutic targets

Adenosine receptors as therapeutic targets

Characterization of the human brain putative A_2B adenosine receptor expressed in Chinese hamster ovary (CHO.A_2B4) cells

Endogenous expression of histamine H₁ receptors functionally coupled to phosphoinositide hydrolysis in C6 glioma cells: regulation by cyclic AMP

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Adenosine A2B‐receptor‐mediated cyclic AMP accumulation in primary rat astrocytes

Cited by 92 publications

References 38 publications

Adenosine receptors as therapeutic targets

Adenosine receptors as therapeutic targets

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

Endogenous expression of histamine H1 receptors functionally coupled to phosphoinositide hydrolysis in C6 glioma cells: regulation by cyclic AMP

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Adenosine A_2B‐receptor‐mediated cyclic AMP accumulation in primary rat astrocytes

Characterization of the human brain putative A_2B adenosine receptor expressed in Chinese hamster ovary (CHO.A_2B4) cells

Endogenous expression of histamine H₁ receptors functionally coupled to phosphoinositide hydrolysis in C6 glioma cells: regulation by cyclic AMP