European Journal of Pharmacology: Molecular Pharmacology
Characterisation of a recombinant P2Y purinoceptor
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P2X3 receptors participate in purinergic inhibition of gastrointestinal smooth muscle
2021, Autonomic Neuroscience: Basic and ClinicalCitation Excerpt :The P2Y1 receptor is a membrane-inserted heptahelical protein which couples to a heterotrimeric G-protein (Gq/11) and raises the activity of the intracellular signalling enzyme phospholipase C (PLCβ) when expressed in host cells. In turn, PLCβ generates inositol trisphosphate (IP3) and afterwards IP3 releases Ca2+ from intracellular stores (Webb et al., 1993; Filtz et al., 1994; Simon et al., 1995). Inhibitory P2Y1 receptors in the gut work through the same Gqα/PLCβ/IP3/Ca2+i signalling pathway which leads to the downstream activation of Ca2+-dependent and apamin-sensitive K+-channels (KCa, SK-type), followed afterwards by the closure of voltage-sensitive Ca2+-channels (CaV, L-type) and the relaxation of smooth muscle tone (Beyder and Farrugia, 2012; Goyal et al., 2013; Burnstock, 2014; Sanders et al., 2014; Kennedy, 2015; King, 2015, 2021; Mader et al., 2016).
Purinergic signalling in the enteric nervous system (An overview of current perspectives)
2015, Autonomic Neuroscience: Basic and ClinicalCitation Excerpt :The originally-defined pharmacological profile for P2Y receptors gave an agonist potency order of 2-MeSATP > > ATP > α,β-meATP for NANC relaxations in guinea-pig taenia coli (Burnstock and Kennedy, 1985). 2-MeSATP and ATP are agonists at recombinant P2Y1 receptors but, perplexingly, α,β-meATP is ineffective (Webb et al., 1993; Burnstock et al., 1994; Filtz et al., 1994; Simon et al., 1995; Tokuyama et al., 1995). However, α,β-meATP is a potent stimulant at some P2X ion-channels found in the ENS (Galligan and North, 2004; Burnstock, 2014).
Pharmacological profiles of cloned mammalian P2Y-receptor subtypes
2006, Pharmacology and TherapeuticsEvaluation of reactive blue 2 derivatives as selective antagonists for P2Y receptors
2002, Vascular PharmacologyKinetic analysis of [<sup>35</sup>S]dATPαS interaction with P2y<inf>1</inf> nucleotide receptor
2002, Neurochemistry InternationalEctonucleotidases as bridge between the ATP and adenosine world: reflections on Geoffrey Burnstock
2022, Purinergic Signalling
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Present address: Glaxo Institute of Applied Pharmacology, Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge CB2 1QJ, UK.