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Monlunabant
Monlunabant (INV-202, MRI-1891, or S-MRI-1891) is a peripherally selective cannabinoid receptor 1 inverse agonist, discovered as a β-arrestin-2-biased cannabinoid receptor 1 antagonist by Dr George Kunos, Dr Resat Cinar, and Dr Malliga Iyer at the National Institutes of Health. It was developed as a weight loss drug by Inversago Pharma. Novo Nordisk’s obesity drug monlunabant showed only modest weight loss in a Phase 2a trial. The drug was associated with higher rates of mild to moderate neuropsychiatric side effects like anxiety and sleep disturbances. Suicidal ideations were not reported. See also * Zevaquenabant Zevaquenabant (S-MRI-1867, INV-101, or MRI-1867) is an investigational small-molecule drug, discovered by Dr George Kunos, Dr Resat Cinar, and Dr Malliga iyer at the National Institutes of Health. Zevaquenabant was described as a third generation ... References {{Cannabinoid receptor modulators CB1 receptor antagonists Experimental anti-obesity drugs Peri ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peripherally Selective Drug
Peripherally selective drugs have their primary mechanism of action outside of the central nervous system (CNS), usually because they are excluded from the CNS by the blood–brain barrier. By being excluded from the CNS, drugs may act on the rest of the body without producing side-effects related to their effects on the brain or spinal cord. For example, most opioids cause sedation when given at a sufficiently high dose, but peripherally selective opioids can act on the rest of the body without entering the brain and are less likely to cause sedation. These peripherally selective opioids can be used as antidiarrheals, for instance loperamide (Imodium). Mechanisms of peripheral selectivity include physicochemical hydrophilicity and large molecular size, which prevent drug permeation through the lipid bilayer cell membranes of the blood–brain barrier, and efflux out of the brain by blood–brain barrier transporters such as P-glycoprotein among many others. Transport out of the b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoid Receptor 1
Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the ''CNR1'' gene. And discovered, by determination and characterization in 1988, and cloned in 1990 for the first time. The human CB1 receptor is expressed in the peripheral nervous system and central nervous system. It is activated by endogenous cannabinoids called endocannabinoids, a group of retrograde neurotransmitters that include lipids, such as anandamide and 2-arachidonoylglycerol; plant phytocannabinoids, such as docosatetraenoylethanolamide found in wild dagga, the compound tetrahydrocannabinol which is an active constituent of the psychoactive drug cannabis; and synthetic analogs of tetrahydrocannabinol. CB1 is antagonized by the phytocannabinoid tetrahydrocannabivarin at low doses and at higher doses, it activates the CB1 receptor as an agonist, but with less potency than tetrahydrocannabinol. The primary endogenous agonist of the human CB1 receptor is ana ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zevaquenabant
Zevaquenabant (S-MRI-1867, INV-101, or MRI-1867) is an investigational small-molecule drug, discovered by Dr George Kunos, Dr Resat Cinar, and Dr Malliga iyer at the National Institutes of Health. Zevaquenabant was described as a third generation cannabinoid receptor 1 (CB1R) antagonist due to its peripheral selectivity and polypharmacology. It acts as a peripherally selective inverse agonist of the cannabinoid receptor 1 and an inducible nitric oxide synthase (iNOS) inhibitor. It has been studied in the experimental models of fibrotic disorders such as liver fibrosis /sup>, chronic kidney disease, idiopathic pulmonary fibrosis, Hermansky-Pudlak syndrome pulmonary fibrosis, skin fibrosis, and metabolic disorders such as obesity /sup> and dyslipidemia Dyslipidemia is a metabolic disorder characterized by abnormally high or low amounts of any or all lipids (e.g. fats, triglycerides, cholesterol, phospholipids) or lipoproteins in the blood. Dyslipidemia is a risk factor for th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Inverse Agonist
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either; they are in fact sometimes called ''blockers'' (examples include alpha blockers, beta blockers, and calcium channel blockers). Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists. A prerequisite for an inverse agonist response is that the receptor must have a constitutive (also known as intrinsic or basal) level of activity in the absence of any ligand. An agonist increases the activity of a receptor above its basal level, whereas an inverse agonist decreases the activity below the basal level. The efficacy of a full agonist is by definition 100%, a neutral antagonist has 0% efficacy, and an inverse agonist has < 0% (i.e., n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
National Institutes Of Health
The National Institutes of Health (NIH) is the primary agency of the United States government responsible for biomedical and public health research. It was founded in 1887 and is part of the United States Department of Health and Human Services (HHS). Many NIH facilities are located in Bethesda, Maryland, and other nearby suburbs of the Washington metropolitan area, with other primary facilities in the Research Triangle Park in North Carolina and smaller satellite facilities located around the United States. The NIH conducts its scientific research through the NIH Intramural Research Program (IRP) and provides significant biomedical research funding to non-NIH research facilities through its Extramural Research Program. , the IRP had 1,200 principal investigators and more than 4,000 postdoctoral fellows in basic, translational, and clinical research, being the largest biomedical research institution in the world, while, as of 2003, the extramural arm provided 28% of biomedical ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CB1 Receptor Antagonists
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CB1 may refer to: * CB1, a postcode district in the CB postcode area * Cannabinoid receptor 1, a receptor for cannabinoids in the brain * ''Crash Bandicoot'' (video game), the first game in the ''Crash Bandicoot'' series * Manhattan Community Board 1 The Manhattan Community Board 1 is a New York City community board encompassing the neighborhoods of Battery Park City, the Financial District, the South Street Seaport, and TriBeCa in Lower Manhattan in the borough of Manhattan as well as Liber ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Anti-obesity Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons (e ... [...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] |
Trifluoromethyl Compounds
The trifluoromethyl group is a functional group that has the formula In science, a formula is a concise way of expressing information symbolically, as in a mathematical formula or a ''chemical formula''. The informal use of the term ''formula'' in science refers to the general construct of a relationship betwe ... . The naming of is group is derived from the methyl group (which has the formula ), by replacing each hydrogen atom by a fluorine atom. Some common examples are trifluoromethane , 1,1,1-trifluoroethane , and hexafluoroacetone . Compounds with this group are a subclass of the organofluorines. Properties The trifluoromethyl group has a significant electronegativity that is often described as being intermediate between the electronegativities of fluorine and chlorine. For this reason, trifluoromethyl-substituted compounds are often strong acids, such as trifluoromethanesulfonic acid and trifluoroacetic acid. Conversely, the trifluoromethyl group lowers the basicity of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
