|
ENX-105
ENX-105 is an investigational new drug being developed by Engrail Therapeutics for the treatment of post-traumatic stress disorder (PTSD). It is currently in the preclinical stage, trailing behind a closely related Engrail compound, ENX-104, which is focused on depression and anhedonia. The drug is described as a dopamine D2 and D3 receptor antagonist and serotonin 5-HT1A and 5-HT2A receptor agonist. Its antagonistic potencies () are 0.08nM at the dopamine D2L receptor, 0.8nM at the dopamine D2S receptor, and 3.8nM at the dopamine D3 receptor, whereas its activational potencies () are 5nM at the serotonin 5-HT2A receptor and 16nM at the serotonin 5-HT1A receptor. ENX-105 does not produce the head-twitch response, a behavioral proxy of psychedelic effects, in rodents, and hence is putatively non-hallucinogenic. The drug has shown anxiolytic-, antipsychotic-, anti-anhedonic-, and pro-cognitive-like effects in rodents. It has also been found to increase dopamine levels in t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ENX-104
ENX-104, also known as deuterated nemonapride enantiomer, is a selective dopamine D2 and D3 receptor antagonist which is under development for the treatment of major depressive disorder. It is specifically under development for the treatment of major depressive disorder characterized by anhedonia. The drug is being developed for use at low doses to preferentially block presynaptic dopamine D2 and D3 autoreceptors and hence to enhance rather than inhibit dopaminergic neurotransmission. It is taken by mouth. Pharmacology Pharmacodynamics ENX-104 is intended for use at low doses to produce preferential presynaptic dopamine D2 and D3 autoreceptor antagonism and consequent enhancement of dopaminergic neurotransmission. The target occupancy of the dopamine D2 and D3 receptors is approximately 40 to 70%. For comparison, dopamine D2 receptor occupancy of 65 to 80% is associated with antipsychotic-like effects and hence with substantial postsynaptic dopamine D2 receptor antagonism in a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Investigational New Drug
The United States Food and Drug Administration's Investigational New Drug (IND) program is the means by which a pharmaceutical industry, pharmaceutical company obtains permission to start human clinical trials and to ship an experimental drug interstate commerce, across state lines (usually to clinical investigators) before a marketing application for the drug has been approved. Regulations are primarily at . Similar procedures are followed in the European Union, Japan, and Canada due to regulatory harmonization efforts by the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use, International Council for Harmonisation. Types * Research or investigator INDs are non-commercial INDs filed by researchers to study an unapproved drug or to study an approved drug for a new indication or in a new patient population. * Expanded access, Emergency Use INDs, also called compassionate use or single-patient INDs, are filed for emergency use of a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytic
An anxiolytic (; also antipanic or anti-anxiety 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 response. 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. Those with anxiety disorders may have concurrent psychological disorders, such as depression. Anxiety disorders are classified using six possible clinical assessments: Different types of anxiety disorders will share some general symptoms while having their own distinctive symptoms. This explains why people with different types of anxiety disorders will respond differently to diffe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D3 Antagonists
D3, D03, D.III, D III or D-3 may refer to: Transportation Roads * London Buses route D3, a Transport for London contracted bus route * D3 motorway (Czech Republic), a motorway in the Czech Republic * D3 road (Croatia), a state road in Croatia * D3 motorway (Slovakia), a motorway in northern Slovakia Aircraft * Albatros D.III, a 1916 German biplane fighter aircraft * Dewoitine D.3, a Dewoitine aircraft * Dunne D.3, a British Dunne aircraft * Fokker D.III, a 1916 German single-seat fighter aircraft * Mercedes D.III, a 1914 German 6-cylinder, liquid-cooled inline aircraft engine * Phönix D.III, a variant of the Austro-Hungarian First World War Phönix D.I biplane fighter * Pfalz D.III, a 1917 German fighter aircraft * Schütte-Lanz D.III, a 1918 German fighter aircraft prototype * Siemens-Schuckert D.III, a 1917 German prototype single-seat fighter aircraft Automobiles * Ford D3 platform, a full-size car automobile platform * Peugeot D3, a panel van manufactured from 1950 t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D2 Antagonists
D, or d, is the fourth letter of the Latin alphabet, used in the modern English alphabet, the alphabets of other western European languages and others worldwide. Its name in English is ''dee'' (pronounced ), plural ''dees''. History The Semitic letter Dāleth may have developed from the logogram for a fish or a door. There are many different Egyptian hieroglyphs that might have inspired this. In Semitic, Ancient Greek and Latin, the letter represented ; in the Etruscan alphabet the letter was archaic but still retained. The equivalent Greek letter is delta, Δ. The minuscule (lower-case) form of 'd' consists of a lower-story left bowl and a stem ascender. It most likely developed by gradual variations on the majuscule (capital) form 'D', and is now composed as a stem with a full lobe to the right. In handwriting, it was common to start the arc to the left of the vertical stroke, resulting in a serif at the top of the arc. This serif was extended while the rest of t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chlorobenzene Derivatives
Chlorobenzene (abbreviated PhCl) is an aryl chloride and the simplest of the chlorobenzenes, consisting of a benzene ring substituted with one chlorine atom. Its chemical formula is C6H5Cl. This colorless, flammable liquid is a common solvent and a widely used intermediate in the manufacture of other chemicals. Uses The major use of chlorobenzene is as a precursor for further intermediates such as nitrophenols, nitroanisole, chloroaniline, and phenylenediamines, which are used in the production of herbicides, dyestuffs, chemicals for rubber, and pharmaceuticals. It is also used as a high-boiling solvent in industrial and laboratory applications, for materials such as oils, waxes, resins, and rubber. Chlorobenzene is nitrated on a large scale to give a mixture of 2-nitrochlorobenzene and 4-nitrochlorobenzene, which are separated and used as intermediates in production of other chemicals. These mononitrochlorobenzenes are converted to related 2-nitrophenol, 2-nitroanisole, b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzyl Compounds
In organic chemistry, benzyl is the substituent or molecular fragment possessing the structure . Benzyl features a benzene ring () attached to a methylene group (). Nomenclature In IUPAC nomenclature, the prefix benzyl refers to a substituent, for example benzyl chloride or benzyl benzoate. Benzyl is not to be confused with phenyl with the formula . The term benzylic is used to describe the position of the first carbon bonded to a benzene or other aromatic ring. For example, is referred to as a "benzylic" carbocation. The benzyl free radical has the formula . The benzyl cation or phenylcarbenium ion is the carbocation with formula ; the benzyl anion or phenylmethanide ion is the carbanion with the formula . None of these species can be formed in significant amounts in the solution phase under normal conditions, but they are useful referents for discussion of reaction mechanisms and may exist as reactive intermediates. Abbreviations Benzyl is most commonly abbreviated Bn. For ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzamides
Benzamide is an organic compound with the chemical formula of C7H7NO. It is the simplest amide derivative of benzoic acid. In powdered form, it appears as a white solid, while in crystalline form, it appears as colourless crystals. It is slightly soluble in water, and soluble in many organic solvents. It is a natural alkaloid Alkaloids are a broad class of natural product, naturally occurring organic compounds that contain at least one nitrogen atom. Some synthetic compounds of similar structure may also be termed alkaloids. Alkaloids are produced by a large varie ... found in the herbs of '' Berberis pruinosa''. Chemical derivatives A number of substituted benzamides are commercial drugs, including: See also * References External links Physical characteristics {{Authority control Phenyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Secondary Amines
In chemistry, amines (, ) are organic compounds that contain carbon-nitrogen bonds. Amines are formed when one or more hydrogen atoms in ammonia are replaced by alkyl or aryl groups. The nitrogen atom in an amine possesses a lone pair of electrons. Amines can also exist as hetero cyclic compounds. Aniline is the simplest aromatic amine, consisting of a benzene ring bonded to an amino group. Amines are classified into three types: primary (1°), secondary (2°), and tertiary (3°) amines. Primary amines (1°) contain one alkyl or aryl substituent and have the general formula RNH2. Secondary amines (2°) have two alkyl or aryl groups attached to the nitrogen atom, with the general formula R2NH. Tertiary amines (3°) contain three substituent groups bonded to the nitrogen atom, and are represented by the formula R3N. The functional group present in primary amines is called the amino group. Classification of amines Amines can be classified according to the nature and number o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nemonapride
Nemonapride, also previously known as emonapride and sold under the brand name Emilace, is an atypical antipsychotic which is used in the treatment of schizophrenia. It is taken by mouth. Side effects of nemonapride include akathisia, dystonia, hypokinesia, tremor, hypersalivation, and hyperprolactinemia, among others. The drug acts as a dopamine D2, D3, and D4 receptor antagonist. To a lesser extent, it is also a serotonin 5-HT1A receptor partial agonist. Structurally, nemonapride is a benzamide derivative and is related to sulpiride and other benzamides. Nemonapride was introduced for medical use in either 1991 or 1997. It was developed and marketed by Yamanouchi Pharmaceuticals. The drug is approved only in Japan and China. Medical uses Nemonapride is used in the treatment of schizophrenia. It is described as being effective in treating the positive symptoms of schizophrenia. It is also said to have some antidepressant and anxiolytic effects. However, clinical data ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enantiomer
In chemistry, an enantiomer (Help:IPA/English, /ɪˈnænti.əmər, ɛ-, -oʊ-/ Help:Pronunciation respelling key, ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities which are mirror images of each other and non-superposable. Enantiomer molecules are like right and left hands: one cannot be superposed onto the other without first being converted to its mirror image. It is solely a relationship of chirality (chemistry), chirality and the permanent three-dimensional relationships among molecules or other chemical structures: no amount of re-orientation of a molecule as a whole or conformational isomerism, conformational change converts one chemical into its enantiomer. Chemical structures with chirality rotate plane-polarized light. A mixture of equal amounts of each enantiomer, a ''racemic mixture'' or a ''racemate'', does not rotate light. Stereoisomers include both enantiomers and diastereomers. Diaste ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Deuteration
Deuterium (hydrogen-2, symbol H or D, also known as heavy hydrogen) is one of two Stable isotope ratio, stable isotopes of hydrogen; the other is protium, or hydrogen-1, H. The deuterium atomic nucleus, nucleus (deuteron) contains one proton and one neutron, whereas the far more common H has no neutrons. The name ''deuterium'' comes from Greek ''Wikt:δεύτερος, deuteros'', meaning "second". American chemist Harold Urey discovered deuterium in 1931. Urey and others produced samples of heavy water in which the H had been highly concentrated. The discovery of deuterium won Urey a List of Nobel laureates in Chemistry, Nobel Prize in 1934. Nearly all deuterium found in nature was Big Bang nucleosynthesis, synthesized in the Big Bang 13.8 billion years ago, forming the primordial ratio of H to H (~26 deuterium nuclei per 10 hydrogen nuclei). Deuterium is subsequently produced by the slow stellar proton–proton chain, but rapidly destroyed by exothermic Nuclear fusio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
