Differentiation by pyridoxal 5‐phosphate, PPADS and IsoPPADS between responses mediated by UTP and those evoked by α,β‐methylene‐ATP on rat sympathetic ganglia

Connolly, G.P.

doi:10.1111/j.1476-5381.1995.tb17199.x

Cited by 43 publications

(22 citation statements)

References 17 publications

(23 reference statements)

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“…Trezise et al, 1994;Connolly et al, 1995). In the present paper we show that PPADS is an effective antagonist, within this concentration-range, of the action of ATP on the P2Y-purinoceptor of BAE cells, while remaining totally ineffective at the BAE cell P2u-purinoceptor.…”

Section: Introductionmentioning

confidence: 75%

PPADS: an antagonist at endothelial P_2Y‐purinoceptors but not P_2U‐purinoceptors

Brown

Tanna

Boarder

1995

British J Pharmacology

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Section: Introductionmentioning

confidence: 75%

PPADS: an antagonist at endothelial P_2Y‐purinoceptors but not P_2U‐purinoceptors

Brown

Tanna

Boarder

1995

British J Pharmacology

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“…Recent electrophysiological data suggested the presence of distinct receptors for ATP and UTP in rat superior cervical ganglia (see e.g. Connolly, 1995).…”

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confidence: 99%

UTP‐ and ATP‐triggered transmitter release from rat sympathetic neurones via separate receptors

Boehm

Huck

Illéš

1995

British J Pharmacology

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In rat cultured sympathetic neurones, UDP, UTP and ATP at micromolar concentrations triggered Ca2"-dependent and tetrodotoxin-sensitive [3H]-noradrenaline release. The overflow evoked by UTP or ATP was similar at 100 ,umol I', the concentration used in all subsequent experiments. Pre-exposure of the neurones to 100 pumol I' UTP significantly reduced ensuing secretory effects of UTP but not of ATP. Conversely, pre-exposure to ATP diminished the overflow due to ATP but not that due to UTP. In the presence of 10 pmol I`pyridoxal-5'-phosphate or 30 pmol 1' suramin, the secretory response to ATP was reduced, but the effect of UTP was unaltered. Zn2+ (10 imol I-') reduced the overflow triggered by UTP, but increased the overflow due to ATP. These results indicate the presence of separate receptors for pyrimidine nucleotides and for purine nucleotides which both trigger transmitter release.

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“…Antagonists such as suramin, pyridoxal-5-phosphate-6-azophenyl-2Ј,4Ј-disulfonic acid, reactive blue 2, and their analogs have traditionally been used as P2X receptor antagonists (Connolly, 1995;Bultmann et al, 1996). However, these compounds are relatively nonselective and exhibit high nanomolar-to-high micromolar affinities for P2X receptors (Bianchi et al, 1999).…”

mentioning

confidence: 99%

Competitive Antagonism of Recombinant P2X_2/3Receptors by 2′,3′-O-(2,4,6-Trinitrophenyl) Adenosine 5′-Triphosphate (TNP-ATP)

et al. 2000

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TNP-ATP has become widely recognized as a potent and selective P2X receptor antagonist, and is currently being used to discriminate between subtypes of P2X receptors in a variety of tissues. We have investigated the ability of TNP-ATP to inhibit ␣,␤-methylene ATP (␣,␤-meATP)-evoked responses in 1321N1 human astrocytoma cells expressing recombinant rat or human P2X 2/3 receptors. Pharmacological responses were measured using electrophysiological and calcium imaging techniques. TNP-ATP was a potent inhibitor of P2X 2/3 receptors, blocking both rat and human receptors with IC 50 values of 3 to 6 nM. In competition studies, 10 to 1000 M ␣,␤-meATP was able to overcome TNP-ATP inhibition. Schild analysis revealed that TNP-ATP was a competitive antagonist with pA 2 values of Ϫ8.7 and Ϫ8.2. Inhibition of P2X 2/3 receptors by TNP-ATP was rapid in onset, reversible, and did not display use dependence. Although the onset kinetics of inhibition were concentration-dependent, the TNP-ATP off-kinetics were concentration-independent and relatively slow. Full recovery from TNP-ATP inhibition did not occur until Ն5 s after removal of the antagonist. Because of the slow off-kinetics of TNP-ATP, full competition with ␣,␤-meATP for receptor occupancy could be seen only after both ligands had reached a steady-state condition. It is proposed that the slowly desensitizing P2X 2/3 receptor allowed this competitive interaction to be observed over time, whereas the rapid desensitization of other P2X receptors (P2X 3 ) may mask the detection of competitive inhibition by TNP-ATP.

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Differentiation by pyridoxal 5‐phosphate, PPADS and IsoPPADS between responses mediated by UTP and those evoked by α,β‐methylene‐ATP on rat sympathetic ganglia

Cited by 43 publications

References 17 publications

PPADS: an antagonist at endothelial P_2Y‐purinoceptors but not P_2U‐purinoceptors

PPADS: an antagonist at endothelial P_2Y‐purinoceptors but not P_2U‐purinoceptors

UTP‐ and ATP‐triggered transmitter release from rat sympathetic neurones via separate receptors

Competitive Antagonism of Recombinant P2X_2/3Receptors by 2′,3′-O-(2,4,6-Trinitrophenyl) Adenosine 5′-Triphosphate (TNP-ATP)

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Differentiation by pyridoxal 5‐phosphate, PPADS and IsoPPADS between responses mediated by UTP and those evoked by α,β‐methylene‐ATP on rat sympathetic ganglia

Cited by 43 publications

References 17 publications

PPADS: an antagonist at endothelial P2Y‐purinoceptors but not P2U‐purinoceptors

PPADS: an antagonist at endothelial P2Y‐purinoceptors but not P2U‐purinoceptors

UTP‐ and ATP‐triggered transmitter release from rat sympathetic neurones via separate receptors

Competitive Antagonism of Recombinant P2X2/3Receptors by 2′,3′-O-(2,4,6-Trinitrophenyl) Adenosine 5′-Triphosphate (TNP-ATP)

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Product

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About

PPADS: an antagonist at endothelial P_2Y‐purinoceptors but not P_2U‐purinoceptors

PPADS: an antagonist at endothelial P_2Y‐purinoceptors but not P_2U‐purinoceptors

Competitive Antagonism of Recombinant P2X_2/3Receptors by 2′,3′-O-(2,4,6-Trinitrophenyl) Adenosine 5′-Triphosphate (TNP-ATP)