Results 181 to 190 of about 1,544,426 (289)

Neuronal and ion channel mechanisms of noxious heat sensing in mammals: A puzzle of sensory physiology and pharmacology

open access: yesBritish Journal of Pharmacology, EarlyView.
Transient receptor potential vanilloid 1 (TRPV1) was the first noxious heat‐sensitive channel discovered. In rodents, its role is robust in the heat response of the cell body of polymodal nociceptors, but surprisingly small in that of the peripheral terminals in the skin.
Gábor Pethő, Peter W. Reeh
wiley   +1 more source

Potentiation effects of the positive allosteric modulator PTC‐174 on NMDA receptors in neonatal male rat substantia nigra dopaminergic neurons

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Positive allosteric modulators bind to secondary binding sites on the receptor and alter receptor conformation and activation, changing agonist potency and efficacy. PTC‐174 is a novel NMDA receptor positive allosteric modulator that particularly enhances activity of receptors containing GluN2C or GluN2D subunits.
Bangyuan Liu, Alasdair J. Gibb
wiley   +1 more source

NMDA receptor subunit‐dependent analysis of radiprodil inhibition in neonatal male rat substantia nigra dopaminergic neurons

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Radiprodil is a GluN2B subunit selective NMDA receptor negative allosteric modulator which is currently under clinical investigation as a possible anti‐epileptic drug for paediatric use. Our goal was to investigate the inhibition of dopaminergic neuron NMDA responses by radiprodil.
Bangyuan Liu, Alasdair J. Gibb
wiley   +1 more source

Selective excitatory effects of γ‐glutamyl‐glycine, a glutathione metabolite, on GluN1 NMDA and mGlu5 receptors impacting synaptic plasticity

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Gamma‐glutamyl dipeptides are essentially produced after glutathione (GSH) degradation. While several γ‐glutamyl dipeptides have been detected in different organs and body fluids, their biological activity remains elusive. This is the case for γ‐Glutamyl‐Glycine (γ‐Glu‐Gly) which has been found in different brain areas.
Sandro Andreu   +20 more
wiley   +1 more source

Ploidy‐Dependent Response to Anticancer Drugs of Human Embryonic Stem Cells

open access: yesCell Proliferation, EarlyView.
Using isogenic hESCs, differing only in their ploidy level, we show the effect of ploidy on the resistance to anticancer drugs. We demonstrate that polyploidy, by itself, confers sensitivity to chemotherapies, leading to higher apoptosis and delayed proliferation, while the loss of p53 reverses the phenotype, demonstrating higher resistance.
Guy Haim‐Abadi, Nissim Benvenisty
wiley   +1 more source

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