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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 Sanofi S.A. is a French multinational pharmaceutical and healthcare company headquartered in Paris, France. Originally, the corporation was established in 1973 and merged with Synthélabo in 1999 to form Sanofi-Synthélabo. In 2004, Sanofi-Syn ... announced that further development of this drug had been halted. See also * ABT-436 * Balovaptan * SRX-246 * TS-121 References External links * Sanofi Vasopressin receptor antagonists {{systemic-hormonal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Arginine Vasopressin Receptor 1B
Vasopressin V1b receptor (V1BR) also known as vasopressin 3 receptor (VPR3) or antidiuretic hormone receptor 1B is a protein that in humans is encoded by the ''AVPR1B'' (arginine vasopressin receptor 1B) gene. V1BR acts as a receptor for vasopressin. AVPR1B belongs to the subfamily of G-protein coupled receptors. Its activity is mediated by G proteins which stimulate a phosphatidylinositol-calcium second messenger system. It is a major contributor to homeostasis and the control of water, glucose, and salts in the blood. Arginine vasopressin has four receptors, each of which are located in different tissues and have specific functions. AVPR1b is a g-protein coupled pituitary receptor that has only recently been characterized because of its rarity. It has been found that the 420-amino-acid sequence of the AVPR1B receptor shared the most overall similarities with the AVP1A, AVP2 and oxytocin receptors. AVPR1B maps to chromosome region 1q32 and is a member of the vasopressin/oxytocin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vasopressin Receptor Antagonist
A vasopressin receptor antagonist (VRA) is an agent that interferes with action at the vasopressin receptors. Most commonly VRAs are used in the treatment of hyponatremia, especially in patients with congestive heart failure, liver cirrhosis or SIADH. Types Vaptans The "vaptan" drugs act by directly blocking the action of vasopressin at its receptors ( V1A, V1B and V2). These receptors have a variety of functions, with the V1A and V2 receptors are expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V1A and V1B receptors are expressed in the central nervous system. V1A is expressed in many regions of the brain, and has been linked to a variety of social behaviors in humans and animals. The vaptan class of drugs contains a number of compounds with varying selectivity, several of which are either already in clinical use or in clinical trials as of 2009. ;Unselective (mixed V1A/V2) * Conivaptan ;V1A selective (V1RA ... [...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] |
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] |
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] |
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] |
Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
Binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand may bind more preferentially to one receptor than another. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate. Binding selectivity is of major importance in biochemistry and in chemical separation processes. Selectivity coefficient The concept of selectivity is used to quantify the extent to which one chemical substance, A, binds each of two other chemical substances, B and C. The simplest case is where the complexes formed have 1:1 stoichiometry. Then, the two interactions may be characterized by equilibrium constants ''K''AB and ''K''AC.The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. : + B AB; \mathit K_ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Orally Active
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Non-peptide
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. Small mole ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small pilot studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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