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List Of Investigational Anxiolytics
This is a list of investigational anxiolytics, or anxiolytics that are currently under development for clinical use but are not yet approved. Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses. Generalized anxiety disorder * Agomelatine (AGO-178; Valdoxan) – melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist* Riluzole sublingual (BHV-0223) – undefined mechanism of action * TGFK08AA – 5-HT ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Partial Agonist
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist , competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, nalmefene and norclozapine. Examples of ligands acti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Brexpiprazole
Brexpiprazole, sold under the brand name Rexulti among others, is an atypical antipsychotic. It is a dopamine D2 receptor partial agonist and has been described as a "serotonin–dopamine activity modulator" (SDAM). The drug was approved by the U.S. Food and Drug Administration (FDA) on 10 July 2015, for the treatment of schizophrenia, and as an adjunctive treatment for depression. It has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD). The drug was developed by Otsuka and Lundbeck, and is considered to be a successor of Otsuka's top-selling atypical antipsychotic aripiprazole (Abilify). It is available as a generic medication. Medical uses Brexpiprazole is approved for the indication of schizophrenia in Canada, United States, Australia, Japan and Europe. In 2019, it was also approved in Canada as adjunctive treatment in Major Dep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BNC-210
BNC210 (also known as IW-2143 during its time licensed to Ironwood Pharmaceuticals) is an anxiolytic drug that acts via negative allosteric modulation of the α7-nicotinic acetylcholine receptor, by Bionomics Limited. It is currently being investigated for the treatment of post traumatic stress disorder. The drug has demonstrated clinically significant anxiety reduction in both animal models and in Phase I trials. It appears to be devoid of significant sedation or memory-impairing side effects, as well as lacking addictive potential in rat discriminatory models. Phase I trials have shown no serious side effects. Bionomics previously licensed it to Ironwood Pharmaceuticals in January 2012, where it was known as IW-2143. In December 2012, IW-2143 begun undergoing phase I clinical trials in the United States, but in November 2014, was released back to Bionomics in a mutual agreement. Bionomics will now continue development and clinical testing, with Ironwood receiving a royalt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acamprosate
Acamprosate, sold under the brand name Campral, is a medication used along with counselling to treat alcohol use disorder. For label updates seFDA index page for NDA 021431/ref> Acamprosate is thought to stabilize chemical signaling in the brain that would otherwise be disrupted by alcohol withdrawal. When used alone, acamprosate is not an effective therapy for alcohol use disorder in most individuals; studies have found that acamprosate works best when used in combination with psychosocial support since the drug facilitates a reduction in alcohol consumption as well as full abstinence. Serious side effects include allergic reactions, abnormal heart rhythms, and low or high blood pressure, while less serious side effects include headaches, insomnia, and impotence. Diarrhea is the most common side-effect. Acamprosate should not be taken by people with kidney problems or allergies to the drug. Until it became generic in the United States, Campral was manufactured and marketed ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Immunomodulator
Immunotherapy or biological therapy is the treatment of disease by activating or suppressing the immune system. Immunotherapies designed to elicit or amplify an immune response are classified as ''activation immunotherapies,'' while immunotherapies that reduce or suppress are classified as '' suppression immunotherapies''. Immunotherapy is under preliminary research for its potential to treat various forms of cancer. Cell-based immunotherapies are effective for some cancers. Immune effector cells such as lymphocytes, macrophages, dendritic cells, natural killer cells, and cytotoxic T lymphocytes work together to defend the body against cancer by targeting abnormal antigens expressed on the surface of tumor cells. Vaccine-induced immunity to COVID-19 relies mostly on an immunomodulatory T cell response. Therapies such as granulocyte colony-stimulating factor (G-CSF), interferons, imiquimod and cellular membrane fractions from bacteria are licensed for medical use. Others includin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
7-Oxoprasterone
7-Ketodehydroepiandrosterone (7-keto-DHEA,7-oxo-DHEA), also known as 7-oxoprasterone, is a prohormone produced by metabolism of the prohormone dehydroepiandrosterone (DHEA). 7-oxo-DHEA is even more effective than DHEA for inducing heat production (thermogenesis). Because dieting is usually accompanied by reduced resting metabolic rate, obese persons may benefit from using 7-oxo-DHEA when dieting due to increased metabolic rate. 7-Keto-DHEA is not directly converted to testosterone or estrogen, and has thus been investigated as a potentially more useful relative of DHEA. Researchers have raised concern that supplements may trigger positive tests for performance-enhancing drugs. The World Anti-Doping Agency lists 7-keto-DHEA as a prohibited anabolic agent. The FDA has proposed that it be banned from use in compounded drugs. Chemistry 7-Keto-DHEA has a number of chemical names, including: * 7-Ketodehydroepiandrosterone (7-keto-DHEA) * 7-Oxodehydroepiandrosterone (7-oxo-DHEA) * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NMDA Receptor
The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other two being AMPA receptor, AMPA and kainate receptors. Depending on its subunit composition, its Ligand (biochemistry), ligands are glutamate and glycine (or D-Serine, D-serine). However, the binding of the ligands is typically not sufficient to open the channel as it may be blocked by Magnesium, Mg2+ ions which are only removed when the neuron is sufficiently depolarized. Thus, the channel acts as a “coincidence detector” and only once both of these conditions are met, the channel opens and it allows cation, positively charged ions (cations) to flow through the cell membrane. The NMDA receptor is thought to be very important for controlling synaptic plasticity and mediating learning and memory functions. The NMDA receptor is ionotropic, meaning it is a pr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
OX1 Receptor
Orexin receptor type 1 (Ox1R or OX1), also known as hypocretin receptor type 1 (HcrtR1), is a protein that in humans is encoded by the HCRTR1 gene. Function The orexin 1 receptor (OX1), is a G-protein coupled receptor that is heavily expressed in projections from the lateral hypothalamus and is involved in the regulation of feeding behaviour. OX1 selectively binds the orexin-A neuropeptide. It shares 64% identity with OX2. Ligands Agonists * Orexin-A Antagonists * RTIOX-276 - Selective OX1 antagonist * ACT-335827 - Selective OX1 antagonist * Almorexant - Dual OX1 and OX2 antagonist * Lemborexant - Dual OX1 and OX2 antagonist * Nemorexant - Dual OX1 and OX2 antagonist * SB-334,867 - Selective OX1 antagonist * SB-408,124 - Selective OX1 antagonist * SB-649,868 - Dual OX1 and OX2 antagonist * Suvorexant - Dual OX1 and OX2 antagonist See also * Orexin receptor The orexin receptor (also referred to as the hypocretin receptor) is a G-protein-coupled receptor that b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Orexin
Orexin (), also known as hypocretin, is a neuropeptide that regulates arousal, wakefulness, and appetite. The most common form of narcolepsy, type 1, in which the individual experiences brief losses of muscle tone ("drop attacks" or cataplexy), is caused by a lack of orexin in the brain due to destruction of the cells that produce it.Stanford Center for NarcolepsFAQ(retrieved 27-Mar-2012) It exists in the forms of Orexin-A and Orexin-B. There are 50,000–80,000 orexin-producing neurons in the human brain, located predominantly in the perifornical area and lateral hypothalamus. They project widely throughout the central nervous system, regulating wakefulness, feeding, and other behaviours. There are two types of orexin peptide and two types of orexin receptor. Orexin was discovered in 1998 almost simultaneously by two independent groups of researchers working on the rat brain. One group named it orexin, from ''orexis,'' meaning "appetite" in Greek; the other group named it hypo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JNJ-61393215
JNJ-61393215 is an orexin antagonist medication which is under development for the treatment of depression and anxiety disorders. It is an orally active compound and acts as a selective antagonist of the orexin OX1 receptor (1-SORA). Preliminary clinical findings suggest that JNJ-61393215 may have anti-panic effects in humans. As of November 2021, JNJ-61393215 is in phase 2 clinical trials for the treatment of major depressive disorder and is in the preclinical stage of development for treatment of panic disorder, while no further development has been reported for treatment of other anxiety disorders. The drug was originated and developed by Janssen Pharmaceuticals. See also * List of investigational antidepressants § Orexin receptor antagonists * List of investigational anxiolytics This is a list of investigational anxiolytics, or anxiolytics that are currently under development for clinical use but are not yet approved. Chemical/generic names are listed first, with devel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
