Glucagon Receptor Agonist
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Glucagon Receptor Agonist
Glucagon receptor agonists are a class of drugs under development for the treatment of obesity, non-alcoholic fatty liver disease, and congenital hyperinsulinism. Background Glucagon is a hormone that generally opposes the action of insulin. It increases blood glucose by stimulating the production of glucose in the liver via glycogenolysis (breakdown of glycogen) and gluconeogenesis (production of glucose from non-carbohydrate sources). Glucagon also increases the breakdown of lipids and amino acids and the production of ketones. In healthy people, a low dose of exogenous glucagon increases energy expenditure and reduces energy intake without causing hyperglycemia. Glucagon is often elevated in type 2 diabetes; glucagon receptor antagonists were developed for the treatment of this disease but most were abandoned due to safety and adverse effects. Therapeutic uses Rescue glucagon has been a preferred treatment for hypoglycemic shocks in insulin-dependent diabetes since the 1960s ...
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Non-alcoholic Fatty Liver Disease
An alcohol-free or non-alcoholic drink, also known as a temperance drink, is a version of an alcoholic drink made without alcohol, or with the alcohol removed or reduced to almost zero. These may take the form of a non-alcoholic mixed drink or non-alcoholic beer, and are widely available where alcoholic drinks are sold. Scientific definition Low-alcoholic drink Sparkling apple cider, soft drinks, and juice naturally contain trace amounts or no alcohol. Some fresh orange juices are above the UK 'alcohol free' limit of 0.05% ABV, as are some yogurts and rye bread. Ethanol distillation is used to separate alcoholic drinks into what are advertised as non-alcoholic drinks and spirits. Distilled wine produces low alcohol wine and brandy (from brandywine, derived from Dutch ''brandewijn'', "burning wine"). Distilled beer may be used to produce low-alcohol beer and whisky. However, alcoholic drinks cannot be further purified to 0.00% alcohol by volume by distillation, although sev ...
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Type 2 Diabetes
Type 2 diabetes (T2D), formerly known as adult-onset diabetes, is a form of diabetes mellitus that is characterized by high blood sugar, insulin resistance, and relative lack of insulin. Common symptoms include increased thirst, frequent urination, fatigue and unexplained weight loss. Other symptoms include increased hunger, having a sensation of pins and needles, and sores (wounds) that heal slowly. Symptoms often develop slowly. Long-term complications from high blood sugar include heart disease, stroke, diabetic retinopathy, which can result in blindness, kidney failure, and poor blood flow in the lower limbs, which may lead to amputations. A sudden onset of hyperosmolar hyperglycemic state may occur; however, ketoacidosis is uncommon. Type 2 diabetes primarily occurs as a result of obesity and lack of exercise. Some people are genetically more at risk than others. Type 2 diabetes makes up about 90% of cases of diabetes, with the other 10% due primar ...
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Thyroid Hormones
File:Thyroid_system.svg, upright=1.5, The thyroid system of the thyroid hormones T3 and T4 rect 376 268 820 433 Thyroid-stimulating hormone rect 411 200 849 266 Thyrotropin-releasing hormone rect 297 168 502 200 Hypothalamus rect 66 216 386 256 Anterior pituitary gland rect 66 332 342 374 Negative feedback rect 308 436 510 475 Thyroid gland rect 256 539 563 635 Thyroid hormones rect 357 827 569 856 Catecholamine rect 399 716 591 750 Metabolism desc bottom-left Thyroid hormones are two hormones produced and released by the thyroid gland, triiodothyronine (T3) and thyroxine (T4). They are tyrosine-based hormones that are primarily responsible for regulation of metabolism. T3 and T4 are partially composed of iodine, derived from food. A deficiency of iodine leads to decreased production of T3 and T4, enlarges the thyroid tissue and will cause the disease known as simple goitre. The major form of thyroid hormone in the blood is thyroxine (T4), whose half-life of arou ...
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Small Molecule
In molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs are small molecules; the terms are equivalent in the literature. Larger structures such as nucleic acids and proteins, and many polysaccharides are not small molecules, although their constituent monomers (ribo- or deoxyribonucleotides, amino acids, and monosaccharides, respectively) are often considered small molecules. Small molecules may be used as research tools to probe biological function as well as leads in the development of new therapeutic agents. Some can inhibit a specific function of a protein or disrupt protein–protein interactions. Pharmacology usually restricts the term "small molecule" to molecules that bind specific biological macromolecules and act as an effector, altering the activity or function of the target. Small molecules can ...
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GIP Receptor
The gastric inhibitory polypeptide receptor (GIP-R), also known as the glucose-dependent insulinotropic polypeptide receptor, is a protein that in humans is encoded by the ''GIPR'' gene. GIP-R is a member of the class B family of G protein coupled receptors. GIP-R is found on beta-cells in the pancreas where it serves as the receptor for the hormone Gastric inhibitory polypeptide (GIP). Function Gastric inhibitory polypeptide, also called glucose-dependent insulinotropic polypeptide, is a 42-amino acid polypeptide synthesized by K cells of the duodenum and small intestine. It was originally identified as an activity in gut extracts that inhibited gastric acid secretion and gastrin release, but subsequently was demonstrated to stimulate insulin release potently in the presence of elevated glucose. The insulinotropic effect on pancreatic islet beta-cells was then recognized to be the principal physiologic action of GIP. Together with glucagon-like peptide-1 Glucagon-l ...
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GLP-1 Receptor Agonist
Glucagon-like peptide-1 (GLP-1) receptor agonists, also known as GLP-1 analogs, GLP-1RAs, or incretin mimetics, are a class of anorectic drugs that reduce blood sugar and energy intake by activating the GLP-1 receptor. They mimic the actions of the endogenous incretin hormone GLP-1, which is released by the gut after eating. GLP-1 agonists were initially developed for type 2 diabetes. The 2022 American Diabetes Association standards of medical care recommend GLP-1 agonists as a first-line therapy for type 2 diabetes, specifically in patients with atherosclerotic cardiovascular disease or obesity. The drugs were also noted to reduce food intake and body weight significantly, and some have been approved to treat obesity and other components of the metabolic syndrome in the absence of diabetes. They are also in development for other indications, such as non-alcoholic fatty liver disease, polycystic ovary syndrome, and diseases of the reward system such as addictions. Mechanism of ...
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Weight Loss Drug
Anti-obesity medication or weight loss medications are pharmacological agents that reduce or control excess body fat. These medications alter one of the fundamental processes of the human body, weight regulation, by: reducing appetite and consequently energy intake, increasing energy expenditure, redirecting nutrients from adipose to lean tissue, or interfering with the absorption of calories. Weight loss drugs have been developed since the early twentieth century, and many have been banned or withdrawn from the market due to adverse effects, including deaths; other drugs proved ineffective. Although many earlier drugs were stimulants such as amphetamines, in the early 2020s, GLP-1 receptor agonists became popular for weight loss. The medications liraglutide, naltrexone/bupropion, orlistat, semaglutide, and tirzepatide are approved by the US Food and Drug Administration (FDA) for weight management in combination with reduced-calorie diet and increased physical activity. As ...
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Rescue Glucagon
Rescue comprises responsive operations that usually involve the saving of life, removal from danger, liberation from restraint, or the urgent treatment of injuries after an incident. It may be facilitated by a range of tools and equipment necessary to deal with the specific circumstances. Rescues may be necessary in a wide range of circumstances and environments, and specialised procedures have been developed for many of these. A rescue may also be performed on an ad hoc basis by the people who are available on site, using equipment available on site or assembled from available materials, particularly when the rescue is urgent or it is unlikely that specialist assistance will be available within a reasonable time. First aid medical attention is often closely associated with rescue, and may be a necessary part of a rescue. Equipment Equipment most commonly refers to a set of tool A tool is an Physical object, object that can extend an individual's ability to modify featur ...
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Glucagon Receptor Antagonists
Glucagon is a peptide hormone, produced by alpha cells of the pancreas. It raises the concentration of glucose and fatty acids in the bloodstream and is considered to be the main catabolic hormone of the body. It is also used as a medication to treat a number of health conditions. Its effect is opposite to that of insulin, which lowers extracellular glucose. It is produced from proglucagon, encoded by the ''GCG'' gene. The pancreas releases glucagon when the amount of glucose in the bloodstream is too low. Glucagon causes the liver to engage in glycogenolysis: converting stored glycogen into glucose, which is released into the bloodstream. High blood-glucose levels, on the other hand, stimulate the release of insulin. Insulin allows glucose to be taken up and used by insulin-dependent tissues. Thus, glucagon and insulin are part of a feedback system that keeps blood glucose levels stable. Glucagon increases energy expenditure and is elevated under conditions of stress. Glucagon be ...
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Hyperglycemia
Hyperglycemia is a condition where unusually high amount of glucose is present in blood. It is defined as blood glucose level exceeding 6.9 mmol/L (125 mg/dL) after fasting for 8 hours or 10 mmol/L (180 mg/dL) 2 hours after eating. Blood glucose level indication Patients with diabetes are oriented to avoid exceeding the recommended postprandial threshold of 160 mg/dL (8.89 mmol/L) for optimal glycemic control. Values of blood glucose higher than 160 mg/dL are classified as 'very high' hyperglycemia, a condition in which an excessive amount of glucose (glucotoxicity) circulates in the blood plasma. These values are higher than the renal threshold of 10 mmol/L (180 mg/dL) up to which glucose reabsorption is preserved at physiological rates and insulin therapy is not necessary. Blood glucose values higher than the cutoff level of 11.1 mmol/L (200 mg/dL) are used to diagnose T2DM and strongly associated with metabolic disturbances, although symp ...
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Congenital Hyperinsulinism
Congenital hyperinsulinism (HI or CHI) is a condition causing severe Neonatal hypoglycemia, hypoglycemia (low blood sugar) in newborns due to the overproduction of insulin. There are various causes of HI, some of which are known to be the result of a Mutation, genetic mutation. Sometimes HI occurs on its own (isolated) and more rarely associated with other medical conditions (as a syndrome). Congenital forms of hyperinsulinism can be transient (short-term) or persistent (long-term) and mild or severe. It can be the result of a defect in the entire pancreas (diffuse HI) or in just part of the pancreas (focal HI). Irrespective of the form, cause, or type, HI is a medical emergency that must be managed from its onset. There is no other hypoglycemic condition in the newborn period as dangerous as HI. Left untreated, hypoglycemia from HI can cause developmental disorders, seizures, permanent brain damage, and even death. For those with focal HI, there is the potential for a cur ...
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