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Prostaglandin F Receptor
Prostaglandin F receptor (FP) is a receptor belonging to the prostaglandin (PG) group of receptors. FP binds to and mediates the biological actions of prostaglandin F2α (PGF2α). It is encoded in humans by the ''PTGFR'' gene. Gene The ''PTGFR'' gene is located on human chromosome 1 at position p31.1 (i.e. 1p31.1), contains 7 exons, and codes for a G protein coupled receptor (GPCR) of the rhodopsin-like receptor family, Subfamily A14 (see rhodopsin-like receptors#Subfamily A14). ''PTGFR'' is expressed as two alternatively spliced transcript variants encoding different isoforms, FPA and FPB, which have different C-terminal lengths. MicroRNA miR-590-3p binds to the Three prime untranslated region of the FP gene to repress its translation. miR-590-3p thus appears to be a negative regulator of FP expression in various cell types. Expression In humans, FP mRNA and/or protein is highly expressed in the uterine myometrium; throughout the eye (endothelium and smooth muscle cell ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and Signal_transduction, transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and produce physiological responses, such as a change in the electrophysiology, electrical activity of a cell. For example, GABA, an inhibitory neurotransmitter, inhibits electrical activity of neurons by binding to GABAA receptor, GABA receptors. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand (biochemistry), ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Cell surface receptors, also known as transmembrane receptors, include ligand-gated ion channels, G prote ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ligand (biochemistry)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Iloprost
Iloprost, sold under the brand name Ventavis among others, is a medication used to treat pulmonary arterial hypertension (PAH), scleroderma, Raynaud's phenomenon, frostbite, and other conditions in which the blood vessels are constricted and blood cannot flow to the tissues. Iloprost is a prostacyclin mimetic. For pulmonary arterial hypertension, iloprost is given via inhalation. Iloprost works by opening (dilating) the blood vessels to allow the blood to flow through them. It was developed by the pharmaceutical company Schering AG and is marketed by Bayer Schering Pharma AG in the European Union and by Actelion Pharmaceuticals in the US. Medical uses In the US, iloprost is indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) to improve a composite endpoint consisting of exercise tolerance, symptoms (NYHA Class), and lack of deterioration. In the EU, iloprost is indicated for the treatment of people with primary pulmonary hypertension, classif ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
U46619
U46619 is a stable synthetic Structural analog, analog of the endoperoxide prostaglandin PGH2 first prepared in 1975, and acts as a thromboxane A2 (TP) receptor agonist. It potently stimulates TP receptor-mediated, but not other prostaglandin receptor-mediated responses in various in vitro preparations and exhibits many properties similar to thromboxane A2, including shape change and aggregation of platelets and smooth muscle contraction. U46619 is a vasoconstrictor that mimics the hydroosmotic effect of vasopressin. References Prostaglandins {{Molecular-biology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sulprostone
Sulprostone is an analogue of prostaglandin E2 (PGE2) that has oxytocic activity in assays of rat kidney cells and tissues. There are four known receptors which mediate various but often different cellular and tissue responses to PGE2: prostaglandin EP1 receptor, prostaglandin EP2 receptor, prostaglandin EP3 receptor, and prostaglandin EP4 receptor. Sulprosotone binds to and activates the prostaglandin EP3 receptor with far greater efficacy than the other PGE2 receptors and also has the advantage of being relatively resistant, compared with PGE2, to becoming metabolically degraded. It is listed as a comparatively weak receptor agonist of the prostaglandin EP1 receptor. In all events, this as well as other potent synthetic EP3 receptor antagonists have the realized or potential ability to promote the beneficial effects of prostaglandin EP3 receptor activation. Sulprostone (as well as other prostanoids receptor agonists) is in use for inducing medical abortion and ending pregnancy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enprostil
Enprostil is a synthetic prostaglandin designed to resemble dinoprostone. Enprostil was found to be a highly potent inhibitor of gastric HCl secretion. It is an analog of prostaglandin E2 but unlike this prostaglandin, which binds to and activates all four cellular receptors viz., EP1, EP2, EP3, and EP4 receptors, enprostil is a more selective receptor agonist in that it binds to and activates primarily the EP3 receptor. Consequently, enprostil is expected to have a narrower range of actions that may avoid some of the unwanted side-effects and toxicities of prostaglandin E2. A prospective multicenter randomized controlled trial conducted in Japan found combining enprostil with cimetidine was more effective than cimetidine alone in treating gastric ulcer. See also *Prostaglandin receptors Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane Receptor (biochemistry), receptors that are regarded as the primary receptors for one or more o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tafluprost
Tafluprost (trade names Taflotan by Santen Pharmaceutical, Zioptan by Merck in the US and Saflutan by Mundipharma in Australia) is a prostaglandin analogue. It is used topically (as eye drops) to control the progression of open-angle glaucoma and in the management of ocular hypertension, alone or in combination with other medication. It reduces intraocular pressure by increasing the outflow of aqueous fluid from the eyes. Adverse effects The most common side effect is conjunctival hyperemia, which occurs in 4 to 20% of patients. Less common side effects include stinging of the eyes, headache, and respiratory infections. Rare side effects are dyspnoea (breathing difficulties), worsening of asthma, and macular oedema. Interactions Nonsteroidal anti-inflammatory drugs (NSAIDs) can either reduce or increase the effect of tafluprost. Timolol eye drops, a common kind of glaucoma medication, does not negatively interact with this drug. No interactions with systemic (for example ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Latanoprost
Latanoprost, sold under the brand name Xalatan among others, is a medication used to treat increased pressure inside the eye (intraocular pressure). This includes ocular hypertension and open-angle glaucoma. Latanaprost is applied as eye drops to the eyes. Onset of effects is usually within four hours, and they last for up to a day. Common side effects include blurry vision, redness of the eye, itchiness, and darkening of the iris. Latanoprost is in the prostaglandin analogue family of medications. It works by increasing the outflow of aqueous fluid from the eyes through the uveoscleral tract. Latanoprost was approved for medical use in the United States and the European Union in 1996. It is on the World Health Organization's List of Essential Medicines. Latanoprost is available as a generic medication. In 2022, it was the 67th most commonly prescribed medication in the United States, with more than 9million prescriptions. It is available as a fixed-dose combinat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cloprostenol
Cloprostenol is a synthetic analogue of prostaglandin F2α (PGF2α). It is a potent luteolytic agent; this means that, within hours of administration, it causes the corpus luteum to stop production of progesterone, and to reduce in size over several days. This effect is used in animals to induce estrus The estrous cycle (, originally ) is a set of recurring physiological changes induced by reproductive hormones in females of mammalian subclass Theria. Estrous cycles start after sexual maturity in females and are interrupted by anestrous phas ... and to cause abortion. References Veterinary drugs Cyclopentanes {{Veterinary-med-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Agonists
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive." Types of agonists can be activated by either ...[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Molar Concentration
Molar concentration (also called molarity, amount concentration or substance concentration) is the number of moles of solute per liter of solution. Specifically, It is a measure of the concentration of a chemical species, in particular, of a solute in a solution, in terms of amount of substance per unit volume of solution. In chemistry, the most commonly used unit for molarity is the number of moles per liter, having the unit symbol mol/L or mol/ dm3 (1000 mol/ m3) in SI units. A solution with a concentration of 1 mol/L is said to be 1 molar, commonly designated as 1 M or 1 M. Molarity is often depicted with square brackets around the substance of interest; for example, the molarity of the hydrogen ion is depicted as + Definition Molar concentration or molarity is most commonly expressed in units of moles of solute per litre of solution. For use in broader applications, it is defined as amount of substance of solute per unit volume of solution, or ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TXA2
Thromboxane A2 (TXA2) is a type of thromboxane that is produced by activated platelets during hemostasis and has prothrombotic properties: it stimulates activation of new platelets as well as increases platelet aggregation. This is achieved by activating the thromboxane receptor, which results in platelet-shape change, inside-out activation of integrins, and degranulation. Circulating fibrinogen binds these receptors on adjacent platelets, further strengthening the clot. TXA2 is also a known vasoconstrictor and is especially important during tissue injury and inflammation. It is also regarded as responsible for Prinzmetal's angina. Receptors that mediate TXA2 actions are thromboxane receptor, thromboxane A2 receptors. The human TXA2 receptor (TP) is a typical G protein-coupled receptor (GPCR) with seven transmembrane segments. In humans, two TP receptor splice variants – TPα and TPβ – have so far been cloned. Synthesis and breakdown Thromboxane A2 (TXA2) is generated from ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
