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P2RX3
P2X purinoceptor 3 is a protein that in humans is encoded by the ''P2RX3'' gene. The product of this gene belongs to the family of purinoceptors for ATP. This receptor functions as a ligand-gated ion channel and may transduce ATP-evoked nociceptor activation. Mouse studies suggest that this receptor is important for peripheral pain responses, and also participates in pathways controlling urinary bladder volume reflexes, platelet aggregation, macrophage activation, apoptosis and neuronal–glial interactions. It is possible that the development of selective antagonists for this receptor may have a therapeutic potential in pain relief and in the treatment of disorders of urine storage. Ligands ;Antagonists * BLU-5937 * Gefapixant * Opiranserin See also * P2X purinoreceptor * Purinergic receptor * Ligand-gated ion channel * Nociceptor A nociceptor ("pain receptor" from Latin ''nocere'' 'to harm or hurt') is a sensory neuron that responds to damaging or potentially damaging stimul ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
P2X Purinoreceptor
The ATP-gated P2X receptor cation channel familyTC# 1.A.7, or simply P2X receptor family, consists of cation-permeable ligand-gated ion channels that open in response to the binding of extracellular adenosine 5'-triphosphate ( ATP). They belong to a larger family of receptors known as the ENaC/P2X superfamily. ENaC and P2X receptors have similar 3-D structures and are homologous. P2X receptors are present in a diverse array of organisms including humans, mouse, rat, rabbit, chicken, zebrafish, bullfrog, fluke, and amoeba. Physiological roles P2X receptors are involved in a variety of physiological processes, including: * Modulation of cardiac rhythm and contractility * Modulation of vascular tone * Mediation of nociception, especially chronic pain * Contraction of the vas deferens during ejaculation * Contraction of the urinary bladder during micturition * Platelet aggregation * Macrophage activation * Apoptosis * Neuronal- glial integration Tissue distribution P2X receptors ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ligand-gated Ion Channel
Ligand-gated ion channels (LICs, LGIC), also commonly referred to as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow ions such as Na+, K+, Ca2+, and/or Cl− to pass through the membrane in response to the binding of a chemical messenger (i.e. a ligand), such as a neurotransmitter. When a presynaptic neuron is excited, it releases a neurotransmitter from vesicles into the synaptic cleft. The neurotransmitter then binds to receptors located on the postsynaptic neuron. If these receptors are ligand-gated ion channels, a resulting conformational change opens the ion channels, which leads to a flow of ions across the cell membrane. This, in turn, results in either a depolarization, for an excitatory receptor response, or a hyperpolarization, for an inhibitory response. These receptor proteins are typically composed of at least two different domains: a transmembrane domain which includes the ion pore, and an extracellular domain wh ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gefapixant
Gefapixant (MK-7264) is a drug which acts as an antagonist of the P2RX3 receptor, and may be useful in the treatment of chronic cough Chronic cough is long-term coughing, sometimes defined as more than several weeks or months. The term can be used to describe the different causes related to coughing, the three main ones being upper airway cough syndrome, asthma and gastroesopha .... It was named in honour of Geoff Burnstock. References {{respiratory-system-drug-stub Benzosulfones Sulfonamides Diaryl ethers ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, responding to stimuli, providing structure to cells and organisms, and transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the nucleotide sequence of their genes, and which usually results in protein folding into a specific 3D structure that determines its activity. A linear chain of amino acid residues is called a polypeptide. A protein contains at least one long polypeptide. Short polypeptides, containing less than 20–30 residues, are rarely considered to be proteins and are commonly called peptides. The individual amino acid residues are bonded together by peptide bonds and adjacent amino acid residues. The sequence of amino acid residue ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gene
In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a basic unit of heredity and the molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protein-coding genes and noncoding genes. During gene expression, the DNA is first copied into RNA. The RNA can be directly functional or be the intermediate template for a protein that performs a function. The transmission of genes to an organism's offspring is the basis of the inheritance of phenotypic traits. These genes make up different DNA sequences called genotypes. Genotypes along with environmental and developmental factors determine what the phenotypes will be. Most biological traits are under the influence of polygenes (many different genes) as well as gen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opiranserin
Opiranserin (; developmental code name VVZ-149) is a selective and combined glycine GlyT2 transporter blocker ( = 0.86 μM), purine P2X3 receptor antagonist ( = 0.87 μM), and serotonin 5-HT2A receptor antagonist ( = 1.3 μM) which is under development by Vivozon for the intravenous treatment of postoperative pain. As of April 2017, it is in phase II clinical trial Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietar ...s for this indication. The of the drug was issued in 2017. References {{Serotonin receptor modulators 5-HT2A antagonists Dimethylamino compounds Analgesics Benzamides Experimental drugs Glycine reuptake inhibitors Receptor antagonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Purinergic Receptor
Purinergic receptors, also known as purinoceptors, are a family of plasma membrane molecules that are found in almost all mammalian tissues. Within the field of purinergic signalling, these receptors have been implicated in learning and memory, locomotor and feeding behavior, and sleep. More specifically, they are involved in several cellular functions, including proliferation and migration of neural stem cells, vascular reactivity, apoptosis and cytokine secretion. These functions have not been well characterized and the effect of the extracellular microenvironment on their function is also poorly understood. The term ''purinergic receptor'' was originally introduced to illustrate specific classes of membrane receptors that mediate relaxation of gut smooth muscle as a response to the release of ATP (P2 receptors) or adenosine (P1 receptors). P2 receptors have further been divided into five subclasses: P2X, P2Y, P2Z, P2U, and P2T. To distinguish P2 receptors further, the subclass ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nociceptor
A nociceptor ("pain receptor" from Latin ''nocere'' 'to harm or hurt') is a sensory neuron that responds to damaging or potentially damaging stimuli by sending "possible threat" signals to the spinal cord and the brain. The brain creates the sensation of pain to direct attention to the body part, so the threat can be mitigated; this process is called nociception. History Nociceptors were discovered by Charles Scott Sherrington in 1906. In earlier centuries, scientists believed that animals were like mechanical devices that transformed the energy of sensory stimuli into motor responses. Sherrington used many different experiments to demonstrate that different types of stimulation to an afferent nerve fiber's receptive field led to different responses. Some intense stimuli trigger reflex withdrawal, certain autonomic responses, and pain. The specific receptors for these intense stimuli were called nociceptors. Location In mammals, nociceptors are found in any area of the body tha ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
