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Modimelanotide
Modimelanotide ( INN) (code names AP-214, ABT-719, ZP-1480) is a melanocortinergic peptide drug derived from α-melanocyte-stimulating hormone (α-MSH) which was under development by, at different times, Action Pharma, Abbott Laboratories, AbbVie, and Zealand for the treatment of acute kidney injury. It acts as a non-selective melanocortin receptor agonist, with IC50 values of 2.9 nM, 1.9 nM, 3.7 nM, and 110 nM at the MC1, MC3, MC4, and MC5 receptors. Modimelanotide failed clinical trials for acute kidney injury despite showing efficacy in animal models, and development was not further pursued. See also * Afamelanotide * BMS-470,539 * Bremelanotide * Melanotan II * PF-00446687 * Setmelanotide Setmelanotide, sold under the brand name Imcivree, is a medication used for the treatment of genetic obesity caused by a rare single-gene mutation. The most common side effects include injection site reactions, skin hyperpigmentation (skin pat ... References Ext ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melanocortin 1 Receptor
The melanocortin 1 receptor (MC1R), also known as melanocyte-stimulating hormone receptor (MSHR), melanin-activating peptide receptor, or melanotropin receptor, is a G protein–coupled receptor that binds to a class of pituitary peptide hormones known as the melanocortins, which include adrenocorticotropic hormone (ACTH) and the different forms of melanocyte-stimulating hormone (MSH). It is coupled to Gαs and upregulates levels of cAMP by activating adenylyl cyclase in cells expressing this receptor. It is normally expressed in skin and melanocytes, and to a lesser degree in periaqueductal gray matter, astrocytes and leukocytes. In skin cancer, MC1R is highly expressed in melanomas but not carcinomas. MC1R is one of the key proteins involved in regulating mammalian skin color and hair color. It is located on the plasma membrane of specialized cells known as melanocytes, which produce the pigment melanin through the process of melanogenesis. It works by controlling the type of m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melanocortin 4 Receptor
Melanocortin 4 receptor (MC4R) is a melanocortin receptor that in humans is encoded by the gene. It encodes the MC4R protein, a G protein-coupled receptor (GPCR) that binds α-melanocyte stimulating hormone (α-MSH). In mouse models, MC4 receptors have been found to be involved in feeding behaviour, the regulation of metabolism, sexual behaviour, and male erectile function. Clinical significance In 2009, two very large genome-wide association studies of body mass index (BMI) confirmed the association of variants about 150 kilobases downstream of the ''MC4R'' gene with insulin resistance, obesity, and other anthropometric traits. ''MC4R'' may also have clinical utility as a biomarker for predicting individual susceptibility to drug-induced adverse effects causing weight gain and related metabolic abnormalities. Another GWAS performed in 2012 identified twenty SNPs located ~190 Kb downstream of ''MC4R'' in association with severe antipsychotic-induced weight gain. This ''locus'' o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BMS-470,539
BMS-470539 is a small-molecule experimental drug which acts as a potent and highly selective full agonist of the MC1 receptor. It was discovered in 2003 as part of an effort to understand the role of the MC1 receptor in immunomodulation, and has since been used in scientific research to determine its role in inflammatory processes. The compound was designed with the intention of mimicking the central His-Phe-Arg-Trp pharmacophore of the melanocortins, and this proved to be successful based on its favorable pharmacodynamic profile. See also * Afamelanotide * Bremelanotide * Melanotan II * Modimelanotide * Setmelanotide Setmelanotide, sold under the brand name Imcivree, is a medication used for the treatment of genetic obesity caused by a rare single-gene mutation. The most common side effects include injection site reactions, skin hyperpigmentation (skin pat ... References Carboxamides Anti-inflammatory agents Imidazoles Immunomodulating drugs Melanoco ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melanocortin Receptor
Melanocortin receptors are members of the rhodopsin family of 7-transmembrane G protein-coupled receptors. There are five known members of the melanocortin receptor system each with differing specificities for melanocortins: * . MC1R is associated with pigmentation genetics. * . MC2R is also known as the ACTH receptor or corticotropin receptor because it is specific for ACTH alone. * . MC3R is associated with childhood growth, accrual of lean mass and onset of puberty. * . Defects in MC4R are a cause of autosomal dominant obesity, accounting for 6% of all cases of early-onset obesity. * . MC5R These receptors are inhibited by endogenous inverse agonists agouti signalling peptide and agouti-related peptide, and activated by synthetic (i.e. afamelanotide) and endogenous agonist melanocyte-stimulating hormones. Selective ligands Several selective ligands for the melanocortin receptors are known, and some synthetic compounds have been investigated as potential tanning, anti-obesity ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melanocortin Receptor Agonists
The melanocortins are a family of neuropeptide hormones which are the ligands of the melanocortin receptorsEricson, M.D., et al., ''Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016.'' Biochim Biophys Acta Mol Basis Dis, 2017. 1863(10 Pt A): p. 2414-2435. The melanocortin system consists of melanocortin receptors, ligands, and accessory proteins. The genes of the melanocortin system are found in chordates. Melanocortins were originally named so because their earliest known function was in melanogenesis. It is now known that the melanocortin system regulates diverse functions throughout the body, including inflammatory response, fibrosis, melanogenesis, steroidogenesis, energy homeostasis, sexual function, and exocrine gland function. There are four endogenous melanocortin agonists which are derived from post-transcriptional processing of the precursor molecule proopiomelanocortin (POMC) (Figure 1). They are Adrenocorticotropic hormone (ACTH), a-mel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Setmelanotide
Setmelanotide, sold under the brand name Imcivree, is a medication used for the treatment of genetic obesity caused by a rare single-gene mutation. The most common side effects include injection site reactions, skin hyperpigmentation (skin patches that are darker than surrounding skin), headache and gastrointestinal side effects (such as nausea, diarrhea, and abdominal pain), among others. Spontaneous penile erections in males and adverse sexual reactions in females have occurred with treatment. Depression and suicidal ideation have also occurred with setmelanotide. Setmelanotide was approved for medical use in the United States in November 2020, and in the European Union in July 2021. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. Medical uses Setmelanotide is indicated for chronic weight management (weight loss and weight maintenance for at least one year) in people six years and older with obesity due to three rare genetic co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PF-00446687
PF-00446687 is a drug developed by Pfizer for the treatment of erectile dysfunction, which is a non-peptide agonist selective for the melanocortin receptor subtype MC4. It was found to be active in preliminary human trials, with the 200mg dose being of similar effectiveness to 100mg sildenafil, though lower doses were ineffective. While it is unclear whether PF-00446687 itself will be potent and effective enough to be developed for medical use, it has demonstrated that selectively targeting the MC4 subtype can produce similar aphrodisiac effects to older non-selective peptide-based melanocortin receptor agonists like melanotan II and bremelanotide, without the side effects caused by action at the other melanocortin receptor subtypes. See also * PL-6983 * PF-219,061 * UK-414,495 UK-414,495 is a drug developed by Pfizer for the treatment of female sexual arousal disorder. UK-414,495 acts as a potent, selective inhibitor of the enzyme neutral endopeptidase, which normal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melanotan II
Melanotan II is a synthetic analogue of the peptide hormone α-melanocyte-stimulating hormone (α-MSH) that stimulates melanogenesis and increases sexual arousal. It was under development as drug candidate for female sexual dysfunction and erectile dysfunction but clinical development ceased by 2003, and as of 2018, no product containing melanotan II was marketed and all commercial development had ceased. Unlicensed, untested, or fraudulent products sold as "melanotan II" are found on the Internet, and purported to be effective as "tanning drugs", though side effects such as uneven pigmentation (it makes already uneven pigmentation more noticeable), new nevi (moles), and darkening or enlargement of existing moles have been reported and have led to medical authorities discouraging its use. There has been no scientific study into the long term and permanent side effects the use of this peptide may cause. Mechanism of action Melanotan II acts as a non-selective agonist of the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bremelanotide
Bremelanotide, sold under the brand name Vyleesi, is a medication used to treat low sexual desire in women. Specifically it is used for low sexual desire which occurs before menopause and is not due to medical problems, psychiatric problems, or problems within the relationship. It is given by an injection just under the skin of the thigh or abdomen. Common side effects include nausea, pain at the site of injection, and headache. It may also cause a temporary increase in blood pressure and decrease in heart rate after each dose, and darkening of the gums, face, and breasts. The medication is a peptide and acts by activating the melanocortin receptors. Bremelanotide was approved for medical use in the United States in 2019. It was developed by Palatin Technologies. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. Medical uses Bremelanotide is used for the treatment of generalized hypoactive sexual desire disorder (HSDD) in premenopa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Afamelanotide
Afamelanotide, sold under the brand name Scenesse, is a synthetic peptide and analogue of α-melanocyte stimulating hormone. It has been used to prevent skin damage from the sun in people with erythropoietic protoporphyria in the European Union since January 2015 and the United States since October 2019. As a medication, it is administered in subcutaneous implant form. Each implant lasts two months. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. Medical use Afamelanotide is used in the European Union to prevent phototoxicity in adults with erythropoietic protoporphyria (EPP). For updates seEMA Index page/ref> Adverse effects Very common (may affect more than 10% of people) adverse effects in people with EPP include headache and nausea. Common (between 1% and 10%) adverse effects include back pain, upper respiratory tract infections, decreased appetite, migraine, dizziness, weakness, fatigue, lethargy, sleepiness, feeling hot, st ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Animal Model
An animal model (short for animal disease model) is a living, non-human, often genetic-engineered animal used during the research and investigation of human disease, for the purpose of better understanding the disease process without the risk of harming a human. Although biological activity in an animal model does not ensure an effect in humans, many drugs, treatments and cures for human diseases are developed in part with the guidance of animal models. Animal models representing specific taxonomic groups in the research and study of developmental processes are also referred to as model organisms. There are three main types of animal models: Homologous, Isomorphic and Predictive. Homologous animals have the same causes, symptoms and treatment options as would humans who have the same disease. Isomorphic animals share the same symptoms and treatments, only. Predictive models are similar to a particular human disease in only a couple of aspects. However, these are useful in isolating ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small pilot studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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