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Blixeprodil
Blixeprodil,https://iris.who.int/bitstream/handle/10665/380497/9789240107038-eng.pdf "blixeprodilum blixeprodil (2R)-2-(4-fluorophenyl)-2-(methylamino)cyclohexan-1-one N-methyl-D-aspartate (NMDA) receptor antagonist" also known by its developmental code name GM-1020 or as (''R'')-4-fluorodeschloroketamine ((''R'')-4-FDCK), is an NMDA receptor antagonist related to ketamine which is under development for the treatment of major depressive disorder, bipolar depression, and other depressive disorders. It is taken oral administration, by mouth. The drug is oral administration, orally active, in contrast to the poor oral bioavailability of ketamine. Its oral bioavailability is >60%. The Tmax (pharmacology), time to peak levels of blixeprodil is 1.5hours and its elimination half-life is 4.3hours. Blixeprodil shows antidepressant-like effects in rodents. It appears to have a greater separation between antidepressant-like and ataxia-inducing doses than ketamine in rodents and hence might ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gilgamesh Pharmaceuticals
Gilgamesh Pharmaceuticals is a pharmaceutical company that is developing psychedelic and related drugs as medicines. It is a "discovery stage" company and is focused on developing new chemical entities. Its drug candidates include the ketamine-related NMDA receptor antagonist blixeprodil (GM-1020; (''R'')-4-fluorodeschloroketamine or (''R'')-4-FDCK), the dimethyltryptamine (DMT)-related serotonergic psychedelic bretisilocin (GM-2505; 5-fluoro-''N''-methyl-''N''-ethyltryptamine or 5F-MET), the noribogaine-related κ-opioid receptor agonist GM-3009, and the non-hallucinogenic psychoplastogen GM-5022. Another potential candidate is GM-2040, a putatively non-hallucinogenic serotonin 5-HT2A receptor agonist. The company was co-founded by Jonathan Sporn, Jeff Witkin, Dalibor Sames, Andrew Kruegel, and Mike Cunningham. Cunningham is a research scientist at Gilgamesh. Sames, Kruegel, and Cunningham have worked together at Sames's lab at Columbia University. In May 2024, AbbVie mad ... [...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] |
Functional Group
In organic chemistry, a functional group is a substituent or moiety in a molecule that causes the molecule's characteristic chemical reactions. The same functional group will undergo the same or similar chemical reactions regardless of the rest of the molecule's composition. This enables systematic prediction of chemical reactions and behavior of chemical compounds and the design of chemical synthesis. The reactivity of a functional group can be modified by other functional groups nearby. Functional group interconversion can be used in retrosynthetic analysis to plan organic synthesis. A functional group is a group of atoms in a molecule with distinctive chemical properties, regardless of the other atoms in the molecule. The atoms in a functional group are linked to each other and to the rest of the molecule by covalent bonds. For repeating units of polymers, functional groups attach to their nonpolar core of carbon atoms and thus add chemical character to carbon chains. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluorexetamine
Fluorexetamine (3'-Fluoro-2-oxo-PCE, FXE) is a recreational designer drug from the arylcyclohexylamine family, with dissociative effects. Effects are slightly more stimulating than regular ketamine. Still produces analgesic effects with stimulating dissociative effects. Has reportedly been sold over the internet since around 2017, though has remained relatively uncommon. See also * 3-Fluoro-PCP * 2-Fluorodeschloroketamine * 3-Fluorodeschloroketamine * Deoxymethoxetamine * Hydroxetamine * Methoxetamine * MXiPr MXiPr (Methoxisopropamine, Isopropyloxetamine, Isopropyxetamine') is a recreational designer drug with dissociative effects. It is an arylcyclohexylamine derivative, related to drugs such as ketamine and methoxetamine. It was first identified ... References Arylcyclohexylamines Designer drugs Dissociative drugs Fluoroarenes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3-Fluorodeschloroketamine
3-Fluorodeschloroketamine (3F-DCK, 3-FDCK, FXM) is a recreational designer drug related to ketamine. It is from the arylcyclohexylamine family and has dissociative effects. It was made illegal in Finland in August 2019. See also * 2-Fluorodeschloroketamine * 3-Fluoro-PCP * Deschloroketamine * Fluorexetamine * Methoxmetamine Methoxmetamine (also known as 3-MeO-2'-Oxo-PCM, MXM and MMXE) is a dissociative anesthetic of the arylcyclohexylamine class that is closely related to methoxetamine and methoxyketamine, and has been sold online as a designer drug. Reference ... References Arylcyclohexylamines Designer drugs Dissociative drugs Fluoroarenes Secondary amines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2-Fluorodeschloroketamine
2-Fluorodeschloroketamine (also known as 2'-Fl-2-Oxo-PCM, Fluoroketamine and 2-FDCK) is a dissociative anesthetic related to ketamine. Its sale and use as a designer drug has been reported in various countries. It is an analogue of ketamine where the chlorine group has been replaced by fluorine. Due to its recent emergence, the pharmacological specifics of the compound are mostly unclear. Effects are still ketamine like but with more euphoria and analgesic properties. History The synthesis of 2-FDCK was first described in a 2013 paper as part of a larger effort to synthesize and evaluate new anesthetic drugs based on ketamine and its analogues. Ketamine itself was first introduced in 1964 and was approved for clinical use in 1970. Since then it has become one of the most important and applicable general anesthetics as well as a popular recreational drug. The use of 2-FDCK as a research chemical has been reported in various countries.European Monitoring Centre for Drugs and D ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Investigational Hallucinogens And Entactogens
This is a list of investigational hallucinogens and entactogens, or hallucinogens and entactogens that are currently under formal development for clinical use but are not yet approved. Many of the indications are not for continuous medication therapy but rather for medication-assisted psychotherapy or short-term use only. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.'' Hallucinogens Psychedelics * Dimethyltryptamine (DMT) – addiction, substance-related disorders – Entheon Biomedica* Lysergic acid diethylamide (LSD; "Lucy") – anxiety disorders, attention-deficit hyperactivity disorder – MAPS, MindMedbr> * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Investigational Antidepressants
This is a list of investigational antidepressants, or antidepressants that are currently under development for clinical use in the treatment of mood disorders but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.'' All drugs listed are specifically under development for major depressive disorder (MDD) and/or treatment-resistant depression (TRD) unless noted otherwise. Other forms of depression may include bipolar depression and postpartum depression. Glutamatergics NMDA receptor modulators * 4-Chlorokynurenine (AV-101) – NMDA receptor glycine site antagonist * Apimostinel (GATE-202, NRX-1074) – NMDA receptor modulator * Arketamine (PCN-101, HR-071603) – unknown mechanism of action, indirect AMPA receptor activator * Esketamine (Esketamine DPI, Falkieri, PG061) – non-competitive NMDA receptor antagonist – approved for TRD, specifically under development for bipolar depressio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, pharmaceutical drug, drugs, medical nutrition therapy, 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 institutional review board, 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 experiment, pi ... [...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] |
Dissociation (psychology)
Dissociation, as a concept that has been developed over time, is a wide array of experiences, ranging from a mild emotional detachment from the immediate surroundings, to a more severe disconnection from physical and emotional experiences. The major characteristic of all dissociative phenomena involves a detachment from reality, rather than a loss of reality as in psychosis. The phenomena are diagnosable under the ''DSM-5'' as a group of disorders as well as a symptom of other disorders through various diagnostic tools. Its cause is believed to be related to neurobiological mechanisms, trauma, anxiety, and psychoactive drugs. Research has further related it to suggestibility and hypnosis, and it is inversely related to mindfulness, which is a potential treatment. History French philosopher and psychologist Pierre Janet (1859–1947) is considered to be the author of the concept of dissociation. Contrary to some conceptions of dissociation, Janet did not believe that dissocia ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Arketamine
Arketamine (developmental code names PCN-101, HR-071603), also known as (''R'')-ketamine or (''R'')-(−)-ketamine, is the (''R'')-(−) enantiomer of ketamine. Similarly to racemic ketamine and esketamine, the ''S''(+) enantiomer of ketamine, arketamine is biologically active; however, it is less potent as an NMDA receptor antagonist and anesthetic and thus has never been approved or marketed for clinical use as an enantiopure drug. Arketamine is currently in clinical development as a novel antidepressant. Relative to esketamine, arketamine possesses 4 to 5 times lower affinity for the PCP site of the NMDA receptor. In accordance, arketamine is significantly less potent than racemic ketamine and especially esketamine in terms of anesthetic, analgesic, and sedative-hypnotic effects. Racemic ketamine has weak affinity for the sigma receptor, where it acts as an agonist, whereas esketamine binds negligibly to this receptor, and so the sigma receptor activity of racemic k ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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