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Nemifitide
Nemifitide (INN-00835) is a novel antidepressant drug with a pentapeptide structure similar to that of melanocyte-inhibiting factor (MIF-1) and the amino acid sequence 4-F-Phe-4-OH-Pro-Arg-Gly-Trp-NH2. It is under development by Tetragenex (previously Innapharma, Inc.) for the treatment of major depressive disorder. It has been given to over 430 people over the course of 12 clinical trials throughout a little over the past decade and has reached Phase III studies, but has not yet been approved for marketing in any country. Nemifitide has shown mixed efficacy in alleviating depressive symptoms, but in the cases in which it has worked it has proven to have a rapid onset of action (~5–7 days), few to no side effects, and an excellent safety profile. However, it is inactive orally and must be administered via subcutaneous injection. Remarkably, despite having a very short half-life of only 15–30 minutes, in most or all studies assessing its efficacy nemifitide has been admin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melanocyte-inhibiting Factor
Melanocyte-inhibiting factor (also known as Pro- Leu-Gly-NH2, Melanostatin, MSH release–inhibiting hormone or MIF-1) is an endogenous peptide fragment derived from cleavage of the hormone oxytocin, but having generally different actions in the body. MIF-1 produces multiple effects, both blocking the effects of opioid receptor activation, while at the same time acting as a positive allosteric modulator of the D2 and D4 dopamine receptor subtypes, as well as inhibiting release of other neuropeptides such as alpha-MSH, and potentiating melatonin activity. This complex mix of actions produces a profile of antidepressant, nootropic, and anti-Parkinsonian effects when MIF-1 is administered, and it has been investigated for various medical uses. MIF-1 is unusually resistant to metabolism in the bloodstream, and crosses the blood–brain barrier easily, though it is poorly active orally and is usually injected. Several other closely related peptides with important actions in the body ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Subcutaneous Injection
Subcutaneous administration is the insertion of medications beneath the skin either by injection or infusion. A subcutaneous injection is administered as a bolus into the subcutis, the layer of skin directly below the dermis and epidermis, collectively referred to as the cutis. The instruments are usually a hypodermic needle and a syringe. Subcutaneous injections are highly effective in administering medications such as insulin, morphine, diacetylmorphine and goserelin. Subcutaneous administration may be abbreviated as SC, SQ, subcu, sub-Q, SubQ, or subcut. Subcut is the preferred abbreviation to reduce the risk of misunderstanding and potential errors. Subcutaneous tissue has few blood vessels and so drugs injected here are for slow, sustained rates of absorption, often with some amount of depot effect. Compared with other routes of administration, it is slower than intramuscular injections but still faster than intradermal injections. Subcutaneous infusion (as opp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressants
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting. There is a slight increased risk of suicidal thinking and behavior when taken by children, adolescents, and young adults. Discontinuation syndrome may occur after stopping any antidepressant which resembles recurrent depression. Some research regarding the effectiveness of antidepressants for depression in adults has found benefits, whilst other research has not. Evidence of benefit in children and adolescents is unclear. The twenty-one most commonly prescribed antidepressant medications are more effective than placebo for the short-term (acute) treatments of adults with major depressive disorder. There is debate in the medical community about how much of the observed effects of antidepre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Molar Concentration
Molar concentration (also called molarity, amount concentration or substance concentration) 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 in SI unit. A solution with a concentration of 1 mol/L is said to be 1 molar, commonly designated as 1 M. 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 per unit volume available to the species, represented by lowercase c: :c = \frac = \frac = \frac. Here, n is the amount of the solute in moles, N is the number of constituent particles present in volume V (in litres) of the solution, and N_\text is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melanocortin 5 Receptor
Melanocortin 5 receptor (MC5R) is a protein that in humans is encoded by the gene. It is located on the chromosome 18 in the human genome. When the MC5R was disrupted in transgenic mice, it induced disruption of their exocrine glands and resulted in decreased production of sebum. Physiology MC5R is necessary for normal sebum production. Stimulation of MC5R promotes fatty acid oxidation in skeletal muscle and lypolysis in adipocytes. MC5R is essential for erythrocyte differentiation. MC5R is involved in inflammation. MC5R helps maintain thermal homeostasis. MC5R is expressed in the brain at different levels depending on physical activity. Pheromones MC5R is heavily expressed in the preputial gland in mice (a modified sebaceous gland involved in pheromone production). MC5R deficiency in male mice decreases aggressive behavior, promotes defensive behavior and encourages other male mice to attack MC5R-deficient males through pheromonal signals. MRAP Melanocortin 2 receptor a ... [...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'' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bombesin Receptor
The bombesin receptors are a group of G-protein coupled receptors which bind bombesin. Three bombesin receptors are currently known: BB1, previously known as Neuromedin B receptor BB2, previously known as Gastrin-releasing peptide receptor BB3, previously known as Bombesin-like receptor 3 External links * G protein-coupled receptors {{transmembranereceptor-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropeptide Y Receptor
Neuropeptide Y receptors are a family of receptors belonging to class A G-protein coupled receptors and they are activated by the closely related peptide hormones neuropeptide Y, peptide YY and pancreatic polypeptide. These receptors are involved in the control of a diverse set of behavioral processes including appetite, circadian rhythm, and anxiety. Activated neuropeptide receptors release the Gi subunit from the heterotrimeric G protein complex. The Gi subunit in turn inhibits the production of the second messenger cAMP from ATP. Only the crystal structure of Y1 in complex with two antagonist is available. Types There are five known mammalian neuropeptide Y receptors designated Y1 through Y5. Four neuropeptide Y receptors each encoded by a different gene have been identified in humans, all of which may represent therapeutic targets for obesity and other disorders. * Y1 - * Y2 - * Y4 - * Y5 - Antagonists *BIBP-3226 *Lu AA-33810 *BIIE-0246 *UR-AK49 UR-AK49 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves " '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, |
5-HT2A Receptor
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
