Clinical Formulation Bridging of Gefapixant, a P2X3‐Receptor Antagonist, for the Treatment of Chronic Cough
Sign Up to like & getrecommendations! Published in 2022 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.1105
Abstract: Gefapixant is a P2X3‐receptor antagonist being developed for treatment of refractory or unexplained chronic cough. Four phase 1 studies were conducted in healthy participants that bridged the early‐phase gefapixant formulation (F01) to the phase 3… read more here.
Keywords: receptor antagonist; formulation; chronic cough; p2x3 receptor ... See more keywords
Erratum to: The effect of sinomenine in diabetic neuropathic pain mediated by the P2X3 receptor in dorsal root ganglia
Sign Up to like & getrecommendations! Published in 2017 at "Purinergic Signalling"
DOI: 10.1007/s11302-017-9560-9
Abstract: Type 2 diabetes mellitus (T2DM) accounts for more than 90% of all cases of diabetes mellitus (DM). Diabetic neuropathic pain (DNP) is a common complication of T2DM. Sinomenine is a natural bioactive component extracted from… read more here.
Keywords: t2dm; sinomenine; diabetic neuropathic; p2x3 receptor ... See more keywords
Knockdown the P2X3 receptor in the stellate ganglia of rats relieved the diabetic cardiac autonomic neuropathy
Sign Up to like & getrecommendations! Published in 2018 at "Neurochemistry International"
DOI: 10.1016/j.neuint.2018.09.002
Abstract: &NA; Diabetic cardiac autonomic neuropathy (DCAN) is a common and serious complication of diabetes mellitus (DM), is manifested by nerve fiber injury in the sympathetic and parasympathetic nerve of the autonomic nervous system, and causes… read more here.
Keywords: p2x3 shrna; p2x3; heart rate; p2x3 receptor ... See more keywords
1,8-cineole decreases neuropathic pain probably via a mechanism mediating P2X3 receptor in the dorsal root ganglion
Sign Up to like & getrecommendations! Published in 2018 at "Neurochemistry International"
DOI: 10.1016/j.neuint.2018.09.007
Abstract: ABSTRACT 1,8‐cineole is a natural monoterpene cyclic ether present in eucalyptus and has been reported to exhibit anti‐inflammatory and antioxidant effects. The therapeutic effects of 1,8‐cineole on neuropathic pain and the molecular mechanisms of its… read more here.
Keywords: neuropathic pain; dorsal root; pain; p2x3 receptor ... See more keywords
Investigation on 2',3'-O-Substituted ATP Derivatives and Analogs as Novel P2X3 Receptor Antagonists.
Sign Up to like & getrecommendations! Published in 2019 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.8b00524
Abstract: Antagonists of the purinergic P2X3 receptors represent promising drugs for the treatment of inflammation and pain. The ATP derivative 2',3'-O-(2,4,6-trinitrophenyl)-ATP (TNP-ATP) has been described as a potent competitive inhibitor of this receptor. In this work,… read more here.
Keywords: investigation substituted; receptor; p2x3; p2x3 receptor ... See more keywords
Role of hesperidin in P2X3 receptor-mediated neuropathic pain in the dorsal root ganglia
Sign Up to like & getrecommendations! Published in 2019 at "International Journal of Neuroscience"
DOI: 10.1080/00207454.2019.1567512
Abstract: Abstract Aim: This study investigated whether the neuronal P2X3 receptor in rat dorsal root ganglia (DRG) mediated the effects of hesperidin on neuropathic pain. Materials and methods: The chronic constriction injury (CCI) model was used… read more here.
Keywords: neuropathic pain; cci rats; cci; p2x3 receptor ... See more keywords
First‐in‐human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics
Sign Up to like & getrecommendations! Published in 2022 at "British Journal of Clinical Pharmacology"
DOI: 10.1111/bcp.15358
Abstract: Neuronal hypersensitisation due to adenosine triphosphate‐dependent P2X3 receptor signalling plays a significant role in several disorders including chronic cough and endometriosis. This first‐in‐human study of eliapixant (BAY 1817080) investigated the tolerability, safety and pharmacokinetics (PK)… read more here.
Keywords: eliapixant bay; bay 1817080; p2x3 receptor; study eliapixant ... See more keywords
P2X3 Receptor in Primary Afferent Neurons Mediates the Relief of Visceral Hypersensitivity by Electroacupuncture in an Irritable Bowel Syndrome Rat Model
Sign Up to like & getrecommendations! Published in 2020 at "Gastroenterology Research and Practice"
DOI: 10.1155/2020/8186106
Abstract: Background Electroacupuncture (EA) has been confirmed effectiveness in the treatment of irritable bowel syndrome (IBS), and P2X3 receptors in the peripheral and central neurons participate in the acupuncture-mediated relief of the visceral pain in IBS.… read more here.
Keywords: receptor; rat model; visceral hypersensitivity; p2x3 receptor ... See more keywords
TNF-α enhances sensory DRG neuron excitability through modulation of P2X3 receptors in an acute colitis model
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Immunology"
DOI: 10.3389/fimmu.2022.872760
Abstract: Previous studies have demonstrated that acute colonic inflammation leads to an increase in dorsal root ganglia (DRG) neuronal excitability. However, the signaling elements implicated in this hyperexcitability have yet to be fully unraveled. Extracellular adenosine… read more here.
Keywords: p2x3; p2x3 receptor; excitability; tnf enhances ... See more keywords
The Locus Coeruleus–Norepinephrine System Mediates Empathy for Pain through Selective Up-Regulation of P2X3 Receptor in Dorsal Root Ganglia in Rats
Sign Up to like & getrecommendations! Published in 2017 at "Frontiers in Neural Circuits"
DOI: 10.3389/fncir.2017.00066
Abstract: Empathy for pain (vicariously felt pain), an ability to feel, recognize, understand and share the painful emotions of others, has been gradually accepted to be a common identity in both humans and rodents, however, the… read more here.
Keywords: empathy pain; system; pain; p2x3 receptor ... See more keywords
P2X3 Receptor Ligands: Structural Features and Potential Therapeutic Applications
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2021.653561
Abstract: The ionotropic P2X3 receptor (P2X3R) subtype is one of the seven mammalian P2X1-7 receptor belonging to the P2 purinergic receptor family together with the metabotropic P2Y1-2, 4-6,11-14 ones (Fredholm et al., 2011). As the other… read more here.
Keywords: structural features; receptor ligands; p2x3 receptor; receptor ... See more keywords