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Ulimorelin
Ulimorelin (INN, USAN) (developmental code name TZP-101) is a drug with a modified cyclic peptide structure which acts as a selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR-1a). Unlike many related drugs, ulimorelin has little or no effect on growth hormone (GH) release in rats. However, like ghrelin and other ghrelin agonists, ulimorelin does stimulate GH release with concomitant increases in insulin-like growth factor 1 (IGF-1) in humans. It has been researched for enhancing gastrointestinal motility, especially in gastroparesis and in aiding recovery of bowel function following gastrointestinal surgery, where opioid analgesic drugs used for post-operative pain relief may worsen existing constipation. While ulimorelin has been shown to increase both upper and lower gastrointestinal motility in rats, and showed promising results initially in humans, it failed in pivotal clinical trials in post operative ileus. A common side effect of ghrelin is reduc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Growth Hormone Secretagogue Receptor
Growth hormone secretagogue receptor(GHS-R), also known as ghrelin receptor, is a G protein-coupled receptor that binds growth hormone secretagogues (GHSs), such as ghrelin, the "hunger hormone". The role of GHS-R is thought to be in regulating energy homeostasis and body weight. In the brain, they are most highly expressed in the hypothalamus, specifically the ventromedial nucleus and arcuate nucleus. GSH-Rs are also expressed in other areas of the brain, including the ventral tegmental area, hippocampus, and substantia nigra. Outside the central nervous system, too, GSH-Rs are also found in the liver, in skeletal muscle, and even in the heart. Structure Two identified transcript variants are expressed in several tissues and are evolutionarily conserved in fish and swine. One transcript, 1a, excises an intron and encodes the functional protein; this protein is the receptor for the ghrelin ligand and defines a neuroendocrine pathway for growth hormone release. The second transcr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ileus
Ileus is a disruption of the normal propulsive ability of the intestine. It can be caused by lack of peristalsis or by mechanical obstruction. The word 'ileus' derives . The term 'subileus' refers to a partial obstruction. Signs and symptoms Symptoms of ileus include, but are not limited to: * moderate to severe, diffuse abdominal pain * constipation * abdominal distension * nausea/vomiting, especially after meals * vomiting of bilious fluid (green or yellowish-green in colour) * flatulence and/or lack of bowel movement * excessive belching Cause Decreased propulsive ability may be broadly classified as caused either by bowel obstruction or by intestinal atony or paralysis. However, instances with symptoms and signs of a bowel obstruction occur, but with the absence of a mechanical obstruction, mainly in acute colonic pseudo-obstruction, Ogilvie's syndrome. In 2023 the US FDA reported gastrointestinal ileus as an adverse effect of the medication semaglutide, with frequenc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclic Peptides
Cyclic peptides are polypeptide chains which contain a circular sequence of bonds. This can be through a connection between the amino and carboxyl ends of the peptide, for example in cyclosporin; a connection between the amino end and a side chain, for example in bacitracin; the carboxyl end and a side chain, for example in colistin; or two side chains or more complicated arrangements, for example in alpha-amanitin. Many cyclic peptides have been discovered in nature and many others have been synthesized in the laboratory. Their length ranges from just two amino acid residues to hundreds. In nature they are frequently antimicrobial or toxic; in medicine they have various applications, for example as antibiotics and immunosuppressive agents. Thin-Layer Chromatography (TLC) is a convenient method to detect cyclic peptides in crude extract from bio-mass. Classification Cyclic peptides can be classified according to the types of bonds that comprise the ring. *Homodetic cyclic pept ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peripherally Selective Drugs
Periphery or peripheral may refer to: Music *Periphery (band), American progressive metal band * ''Periphery'' (album), released in 2010 by Periphery *"Periphery", a song from Fiona Apple's album '' The Idler Wheel...'' Gaming and entertainment *Periphery, a group of political entities in BattleTech, a wargaming franchise *'' The Peripheral'', a 2014 novel by William Gibson ** ''The Peripheral'' (TV series), a streaming series based on Gibson's novel Mathematics *Peripheral, an alternate mathematical term for boundary parallel in manifold theory * Peripheral cycle, a mathematical term in graph theory Computing *Peripheral, a device connected to a computer Political *Periphery countries, the least developed countries in world systems theory *Periphery (France), statistical area designating a commuter belt around an urban unit *Peripheries of Greece or ''administrative regions of Greece'' (Greek: , '), the country's first-level administrative divisions **Peripheral unit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Motility Stimulants
Motility is the ability of an organism to move independently using metabolic energy. This biological concept encompasses movement at various levels, from whole organisms to cells and subcellular components. Motility is observed in animals, microorganisms, and even some plant structures, playing crucial roles in activities such as foraging, reproduction, and cellular functions. It is genetically determined but can be influenced by environmental factors. In multicellular organisms, motility is facilitated by systems like the nervous and musculoskeletal systems, while at the cellular level, it involves mechanisms such as amoeboid movement and flagellar propulsion. These cellular movements can be directed by external stimuli, a phenomenon known as taxis. Examples include chemotaxis (movement along chemical gradients) and phototaxis (movement in response to light). Motility also includes physiological processes like gastrointestinal movements and peristalsis. Understanding mo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ghrelin Receptor Agonists
Ghrelin (; or lenomorelin, INN) is a hormone primarily produced by enteroendocrine cells of the gastrointestinal tract, especially the stomach, and is often called a "hunger hormone" because it increases the drive to eat. Blood levels of ghrelin are highest before meals when hungry, returning to lower levels after mealtimes. Ghrelin may help prepare for food intake by increasing gastric motility and stimulating the secretion of gastric acid. Ghrelin activates cells in the anterior pituitary gland and hypothalamic arcuate nucleus, including neuropeptide Y neurons that initiate appetite. Ghrelin stimulates brain structures having a specific receptor – the growth hormone secretagogue receptor 1A (GHSR-1A). Ghrelin also participates in regulation of reward cognition, learning and memory, the sleep-wake cycle, taste sensation, reward behavior, and glucose metabolism. History and name Ghrelin was discovered after the ghrelin receptor (called growth hormone secretagogue type 1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drugs Acting On The Gastrointestinal System And Metabolism
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic disorders. Classification Pharmaceutical drugs are often classified into drug classes—groups of related drugs that have sim ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-1 Blockers
Alpha 1 or Alpha-1 may refer to: *Alpha-1 adrenergic receptor, a G protein-coupled receptor *Alpha-1 antitrypsin, a protein **Alpha-1 antitrypsin deficiency Alpha-1 antitrypsin deficiency (A1AD or AATD) is a genetic disorder that may result in lung disease or liver disease. Onset of lung problems is typically between 20 and 50 years of age. This may result in shortness of breath, wheezing, or an inc ..., a genetic disorder * Alpha-1-fetoprotein or Alpha-fetoprotein, a protein *Alpha-One, a fictional spacecraft in '' Buzz Lightyear of Star Command: The Adventure Begins'' * ''Alpha 1'' (Robert Silverberg anthology), a 1970 book * Alpha-1 Wrestling, a professional wrestling promotion See also * * * A1 (other) * Alpha (other) * AMY1A or Alpha-1A or, an enzyme found in humans and other mammals * List of A1 genes, proteins or receptors {{disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methoxamine
Methoxamine, sold under the brand names Vasoxine, Vasoxyl, and Vasylox among others, is a sympathomimetic medication used as an antihypotensive agent. It has mostly or entirely been discontinued. The drug is an α1- adrenergic receptor agonist. Medical uses The long duration of action of methoxamine has been said to have rendered it obsolete in modern clinical practice. Pharmacology Methoxamine is an α1-adrenergic receptor agonist. It is described as a long-acting α1-adrenergic receptor agonist and this is contrasted with phenylephrine which is said to be short-acting. Phenylephrine is 5 to 10times more potent than methoxamine and has a 3-fold higher maximal effect. Chemistry Methoxamine, also known as 2,6-dimethoxy-β-hydroxy-α-methylphenethylamine or as 2,6-dimethoxy-β-hydroxyamphetamine, is a substituted phenethylamine and amphetamine derivative. It is somewhat similar in chemical structure to those of desglymidodrine (3,6-dimethoxy-β-hydroxyphenethylamine), dim ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenylephrine
Phenylephrine, sold under the brand names Neosynephrine and Sudafed PE among others, is a medication used as a decongestant for uncomplicated nasal congestion in the form of a nasal spray or oral tablet, to dilate the pupil, to increase blood pressure given intravenously in cases of low blood pressure, and to relieve hemorrhoids as a suppository. It can also be applied to the skin. Common side effects when taken by mouth or injected include nausea, vomiting, headache, and anxiety. Use on hemorrhoids is generally well tolerated. Severe side effects may include a slow heart rate, intestinal ischemia, chest pain, kidney failure, and tissue death at the site of injection. It is unclear whether its use during pregnancy and breastfeeding is safe. Phenylephrine is a selective α1-adrenergic receptor agonist with minimal to no β-adrenergic receptor agonist activity or induction of norepinephrine release. It causes constriction of both arteries and veins. Phenylephrine ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-1 Adrenergic Receptor
alpha-1 (α1) adrenergic are G protein-coupled receptors (GPCRs) associated with the Gq alpha subunit, Gq heterotrimeric G protein. α1-adrenergic receptors are subdivided into three highly homologous subtypes, i.e., α1A-adrenergic, α1A-, α1B-adrenergic, α1B-, and α1D-adrenergic, α1D-adrenergic receptor subtypes. There is no α1C receptor. At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. To avoid confusion, naming was continued with the letter D. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α1-adrenergic receptors in the central nervous system, central and peripheral nervous systems. The crystal structure of the α1B-adrenergic receptor subtype has been determined in complex with the inverse agonist (+)-cyclazosin. Effects The α1-adrenergic receptor has several general functions in common with the Alpha-2 adrenergic receptor, α2-adrene ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
