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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-obe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rhodopsin
Rhodopsin, also known as visual purple, is a protein encoded by the RHO gene and a G-protein-coupled receptor (GPCR). It is the opsin of the rod cells in the retina and a light-sensitive receptor protein that triggers visual phototransduction in rods. Rhodopsin mediates dim light vision and thus is extremely sensitive to light. When rhodopsin is exposed to light, it immediately photobleaches. In humans, it is regenerated fully in about 30 minutes, after which the rods are more sensitive. Defects in the rhodopsin gene cause eye diseases such as retinitis pigmentosa and congenital stationary night blindness. Names Rhodopsin was discovered by Franz Christian Boll in 1876. The name rhodospsin derives from Ancient Greek () for "rose", due to its pinkish color, and () for "sight". It was coined in 1878 by the German physiologist Wilhelm Friedrich Kühne (1837-1900). When George Wald discovered that rhodopsin is a holoprotein, consisting of retinal and an apoprotein, ... [...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] |
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 PF-219,061 is a drug that was under development by Pfizer which acts as a potent and highly selective agonist for the dopamine D3 receptor. It was under development as a potential medication for the tre ... [...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 patc ... References Carboxamides Anti-inflammatory agents Imidazoles Immunomodulating drugs Melanocort ... [...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 condi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 patc ... References External lin ... [...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 th ... [...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] |
Gamma-Melanocyte-stimulating Hormone
γ-Melanocyte-stimulating hormone (γ-MSH) is an endogenous peptide hormone and neuropeptide. It is a melanocortin, specifically, one of the three types of melanocyte-stimulating hormone (MSH), and is produced from proopiomelanocortin (POMC). It is an agonist of the MC1, MC3, MC4, and MC5 receptors. It exists in three forms, γ1-MSH, γ2-MSH, and γ3-MSH. Gamma-MSH regulated cardiovascular functions. Gama-MSH effects are measured through the effects it has on the central neural pathway dispersed throughout the kidney. It is not moderated based on tubular sodium transport. Gamma-MSH activates MC3R in renal tubular cells by limiting sodium absorption by inhibiting the central neural pathway.This regulates sodium balance and blood pressure. If MC3R is absent then there is resistance in γ-MSH which results in hypertension on HSD. See also * α-Melanocyte-stimulating hormone * β-Melanocyte-stimulating hormone * Adrenocorticotropic hormone Adrenocorticotropic hormone (A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Beta-Melanocyte-stimulating Hormone
β-Melanocyte-stimulating hormone (β-MSH) is an endogenous peptide hormone and neuropeptide. It is a melanocortin, specifically, one of the three types of melanocyte-stimulating hormone (MSH), and is produced from proopiomelanocortin (POMC). It is an agonist of the MC1, MC3, MC4, and MC5 receptors. B-melanocyte-stimulating hormone is artificially generated because it does not exist in humans naturally. β-MSH is also to decrease food intake in animals such as rats, chicken due to the effect of proopiomelanocortin (POMC). Research was performed to see the effect β-MSH has on chicks, and it has been found that chicks responded with a decrease in food and water intake when treated with β-MSH. The experiment showed that β-MSH causes anorexigenic effects in chicks. See also * α-Melanocyte-stimulating hormone * γ-Melanocyte-stimulating hormone * Adrenocorticotropic hormone Adrenocorticotropic hormone (ACTH; also adrenocorticotropin, corticotropin) is a polypeptide tro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-Melanocyte-stimulating Hormone
α-Melanocyte-stimulating hormone (α-MSH) is an endogenous peptide hormone and neuropeptide of the melanocortin family, with a tridecapeptide structure and the amino acid sequence Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2. It is the most important of the melanocyte-stimulating hormones (MSHs) (also known as melanotropins) in stimulating melanogenesis, a process that in mammals (including humans) is responsible for pigmentation primarily of the hair and skin. It also plays a role in feeding behavior, energy homeostasis, sexual activity, and protection against ischemia and reperfusion injury. α-MSH is a non-selective full agonist of the melanocortin receptors MC1 (Ki = 0.230 nM), MC3 (Ki = 31.5 nM), MC4 (Ki = 900 nM), and MC5 (Ki = 7160 nM), but not MC2 (which is exclusive for adrenocorticotropic hormone (ACTH)). Activation of the MC1 receptor is responsible for its effect on pigmentation, whereas its regulation of appetite, metabolism, and sexual beha ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
