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SRX-246
SRX246, also known as API-246, is a small-molecule, centrally-active, highly-selective vasopressin V1A receptor antagonist which is under investigation by Azevan Pharmaceuticals for the treatment of affective and anger disorders. It is an azetidinone derivative, and was developed from LY-307174 as a lead compound. A phase II activity trial of the drug in the treatment of adults with intermittent explosive disorder is ongoing. It is also being studied for the treatment of post-traumatic stress disorder. See also * List of investigational anxiolytics * ABT-436 * Balovaptan * Nelivaptan Nelivaptan (INN) (developmental codename SSR-149,415) is a selective, orally active, non-peptide vasopressin receptor antagonist selective for the V1B subtype. The drug had entered clinical trials for treatment of anxiety and depression. In J ... * TS-121 References External links Azevan Pharmaceuticals, Inc. - Clinical CandidatesSRX-246 - AdisInsight Lactams Oxazolidines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
TS-121
TS-121 (THY1773) is an orally active, selective vasopressin V1B receptor antagonist which is under development by Taisho Pharmaceutical for the adjunctive treatment of major depressive disorder. As of May 2017, it is in phase II clinical trials for this indication. See also * ABT-436 * Balovaptan * List of investigational antidepressants * Nelivaptan * SRX-246 SRX246, also known as API-246, is a small-molecule, centrally-active, highly-selective vasopressin V1A receptor antagonist which is under investigation by Azevan Pharmaceuticals for the treatment of affective and anger disorders. It is an az ... References External links * Antidepressants Drugs with undisclosed chemical structures Experimental drugs Vasopressin receptor antagonists {{systemic-hormonal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nelivaptan
Nelivaptan ( INN) (developmental codename SSR-149,415) is a selective, orally active, non-peptide vasopressin receptor antagonist selective for the V1B subtype. The drug had entered clinical trials for treatment of anxiety and depression. In July 2008, Sanofi-Aventis announced that further development of this drug had been halted. See also * ABT-436 * Balovaptan * SRX-246 * TS-121 TS-121 (THY1773) is an orally active, selective vasopressin V1B receptor antagonist which is under development by Taisho Pharmaceutical for the adjunctive treatment of major depressive disorder. As of May 2017, it is in phase II clinical tri ... References External links * Sanofi Vasopressin receptor antagonists {{systemic-hormonal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Balovaptan
Balovaptan (; developmental code name RG7314), is a selective small molecule antagonist of the vasopressin V1A receptor which is under development by Roche for the treatment of autism. As of August 2019, it is in a phase III clinical trial for adults and a phase II clinical trial for children for this indication. On 29 January 2018, Roche announced that the US Food and Drug Administration (FDA) had granted Breakthrough Therapy Designation for balovaptan in individuals with autism spectrum disorder (ASD). The FDA granted this based on the results of the adult phase II clinical trial called VANILLA (Vasopressin ANtagonist to Improve sociaL communication in Autism) study. The currently-recruiting (Until March 2020) phase III adult study is called V1aduct and the currently-closed (August 2019) phase II child study is called Av1ation. See also * ABT-436 * Nelivaptan Nelivaptan (INN) (developmental codename SSR-149,415) is a selective, orally active, non-peptide vasopressi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ABT-436
ABT-436 is an orally active, highly selective vasopressin V1B receptor antagonist which was under development by Abbott Laboratories and AbbVie for the treatment of major depressive disorder, anxiety disorders, and alcoholism but was discontinued. It reached phase II clinical trials prior to the discontinuation of its development. See also * Balovaptan * Nelivaptan Nelivaptan (INN) (developmental codename SSR-149,415) is a selective, orally active, non-peptide vasopressin receptor antagonist selective for the V1B subtype. The drug had entered clinical trials for treatment of anxiety and depression. In J ... * SRX-246 * TS-121 References Abandoned drugs Antidepressants Anxiolytics AbbVie brands Drugs with undisclosed chemical structures Vasopressin receptor antagonists {{Systemic-hormonal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Small-molecule
Within the fields of molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs are small molecules; the terms are equivalent in the literature. Larger structures such as nucleic acids and proteins, and many polysaccharides are not small molecules, although their constituent monomers (ribo- or deoxyribonucleotides, amino acids, and monosaccharides, respectively) are often considered small molecules. Small molecules may be used as research tools to probe biological function as well as leads in the development of new therapeutic agents. Some can inhibit a specific function of a protein or disrupt protein–protein interactions. Pharmacology usually restricts the term "small molecule" to molecules that bind specific biological macromolecules and act as an effector, altering the activity or function of the target ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lactams
A lactam is a cyclic amide, formally derived from an amino alkanoic acid. The term is a portmanteau of the words ''lactone'' + ''amide''. Nomenclature Greek prefixes in alphabetical order indicate ring size: * α-Lactam (3-atom rings) * β-Lactam (4-atom rings) * γ-Lactam (5-atom rings) * δ-Lactam (6-atom rings) * ε-Lactam (7-atom rings) This ring-size nomenclature stems from the fact that a hydrolyzed α-Lactam leads to an α-amino acid and a β-Lactam to a β-amino acid, ''etc''. Synthesis General synthetic methods exist for the organic synthesis of lactams. Beckmann rearrangement Lactams form by the acid-catalyzed rearrangement of oximes in the Beckmann rearrangement. Schmidt reaction Lactams form from cyclic ketones and hydrazoic acid in the Schmidt reaction. Cyclization of amino acids Lactams can be formed from cyclisation of amino acids via the coupling between an amine and a carboxylic acid within the same molecule. Lactamization is most efficient in this wa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Post-traumatic Stress Disorder
Post-traumatic stress disorder (PTSD) is a mental and behavioral disorder that can develop because of exposure to a traumatic event, such as sexual assault, warfare, traffic collisions, child abuse, domestic violence, or other threats on a person's life. Symptoms may include disturbing thoughts, feelings, or dreams related to the events, mental or physical distress to trauma-related cues, attempts to avoid trauma-related cues, alterations in the way a person thinks and feels, and an increase in the fight-or-flight response. These symptoms last for more than a month after the event. Young children are less likely to show distress but instead may express their memories through play. A person with PTSD is at a higher risk of suicide and intentional self-harm. Most people who experience traumatic events do not develop PTSD. People who experience interpersonal violence such as rape, other sexual assaults, being kidnapped, stalking, physical abuse by an intimate partner, an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Central Nervous System
The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain and spinal cord. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all parts of the bodies of bilaterally symmetric and triploblastic animals—that is, all multicellular animals except sponges and diploblasts. It is a structure composed of nervous tissue positioned along the rostral (nose end) to caudal (tail end) axis of the body and may have an enlarged section at the rostral end which is a brain. Only arthropods, cephalopods and vertebrates have a true brain (precursor structures exist in onychophorans, gastropods and lancelets). The rest of this article exclusively discusses the vertebrate central nervous system, which is radically distinct from all other animals. Overview In vertebrates, the brain and spinal cord are both enclosed in the meninges. The meninges provide a barrier to chemicals dissolv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phases Of Clinical Research
The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phases start with testing for safety in a few human subjects, then expand to many study participants (potentially tens of thousands) to determine if the treatment is effective. Clinical research is conducted on drug candidates, vaccine candidates, new medical devices, and new diagnostic assays. Summary Clinical trials testing potential medical products are commonly classified into four phases. The drug development process will normally proceed through all four phases over many years. If the drug successfully passes through Phases I, II, and III, it will usually be approved by the national regulatory authority for use in the general population. Phase IV trials are 'post-marketing' or 'surveillance' studies conducted to monitor safety over sever ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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