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A new class of ligand-gated ion channel defined by P2X receptor for extracellular ATP
A complementary DNA encoding of the P2x receptor from rat vas deferens is cloned and expressed in Xenopus oocytes and mammalian cells, defining a new family of ligand-gated ion channels.
Ionic permeability of, and divalent cation effects on, two ATP‐gated cation channels (P2X receptors) expressed in mammalian cells.
Complementary DNAs for the ATP‐gated ion channel subunits P2x1 and P2X2 were used to express the receptors in human embryonic kidney cells by stable transfection, and in Chinese hamster ovary cells by viral infection.
Pharmacological characterization of heterologously expressed ATP-gated cation channels (P2x purinoceptors).
- R. Evans, C. Lewis, G. Buell, S. Valera, R. North, A. Surprenant
- Chemistry, MedicineMolecular pharmacology
- 1 August 1995
The pharmacological properties of homo-oligomeric forms of these two types of cloned P2x receptor channels are defined.
The Role of Positively Charged Amino Acids in ATP Recognition by Human P2X1 Receptors*
Mutations at residues K68A and K309A reduced the potency of ATP by >1400-fold and prolonged the time course of the P2X1 receptor current but had no effect on suramin antagonism.
ATP Binding at Human P2X1 Receptors
It is suggested that residues Lys-68, Phe-185, PHE-291, Arg-292, and Lys-309 contribute to ligand binding at P2X1 receptors, with P he-185 and Phe the291 coordinating the binding of the adenine ring of ATP.
Reduced vas deferens contraction and male infertility in mice lacking P2X1 receptors
The results show that P2X1 receptors are essential for normal male reproductive function and suggest that the development of selective P1X1 receptor antagonists may provide an effective non-hormonal male contraceptive pill and agents that potentiate the actions of ATP at P2x1 receptors may be useful in the treatment of male infertility.
2′,3′‐O‐(2,4,6‐ trinitrophenyl) adenosine 5′‐triphosphate (TNP‐ATP)–a nanomolar affinity antagonist at rat mesenteric artery P2X receptor ion channels
TNP‐ATP is of limited use in whole tissue experiments as a P2X receptor antagonist and its reduced potency probably reflects the breakdown of TNP‐ ATP by nucleotidases.
Molecular properties of P2X receptors
This review aims to give an account of recent work on the molecular basis of the properties of P2X receptors, to consider emerging information on the assembly of P 2X receptor subunits, channel regulation and desensitisation, targeting, the Molecular basis of drug action and the functional contribution of P1X receptors to physiological processes.
Molecular properties of ATP-gated P2X receptor ion channels.
- C. Vial, Jonathan A. Roberts, R. Evans
- Biology, MedicineTrends in pharmacological sciences
- 1 September 2004
Molecular techniques have provided insight into the properties of P2X receptors: mutagenesis and biochemical studies have identified regions associated with ATP binding, ionic conduction, channel gating and regulation.
ATP mediates fast synaptic transmission in mammalian neurons
It is concluded that ATP is the neurotransmitter at this neuro–neuronal synapse, unaffected by antagonists acting at nicotine, 5-hydroxytryptamine, N-methyl-D-aspartate (NMDA), non-NMDA glutamate, γ-aminobutyric acid (GABA), noradrenaline or adenosine receptors.