Ketamine Temsirolimus
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Ketamine Temsirolimus
Ketamine is a cyclohexanone-derived general anesthetic and NMDA receptor antagonist with analgesic and hallucinogenic properties, used medically for anesthesia, depression, and pain management. Ketamine exists as its S- (esketamine) and R- (arketamine) two enantiomers and has antidepressant action likely involving additional mechanisms than NMDA antagonism. At anesthetic doses, ketamine induces a state of dissociative anesthesia, a trance-like state providing pain relief, sedation, and amnesia. Its distinguishing features as an anesthestic are preserved breathing and airway reflexes, stimulated heart function with increased blood pressure, and moderate bronchodilation. As an anesthetic, it is used especially in trauma, emergency, and pediatric cases. At lower, sub-anesthetic doses, it is used as a treatment for pain and treatment-resistant depression. Ketamine is legally used in medicine but is also tightly controlled due to its potential for recreational use and dissoci ...
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Drug Enforcement Administration
The Drug Enforcement Administration (DEA) is a Federal law enforcement in the United States, United States federal law enforcement agency under the U.S. Department of Justice tasked with combating illicit Illegal drug trade, drug trafficking and distribution within the U.S. It is the lead agency for domestic enforcement of the Controlled Substances Act, sharing concurrent jurisdiction with the Federal Bureau of Investigation and U.S. Customs and Border Protection. The DEA is responsible for coordinating and pursuing U.S. drug investigations both domestically and internationally. It was established in 1973 as part of the U.S. government's War on Drugs, war on drugs. The DEA has an DEA Office of National Security Intelligence, intelligence unit that is also a member of the U.S. Intelligence Community. While the unit is part of the DEA chain-of-command, it also reports to the Director of National Intelligence, director of national intelligence. The DEA has been criticized for sche ...
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Norketamine
Norketamine, or ''N''-desmethylketamine, is the major active metabolite of ketamine, which is formed mainly by CYP3A4. Similarly to ketamine, norketamine acts as a noncompetitive NMDA receptor antagonist, but is about 3–5 times less potent as an anesthetic in comparison. Pharmacology Pharmacodynamics Similarly to ketamine, norketamine acts as a noncompetitive NMDA receptor antagonist (Ki = 1.7μM and 13μM for (''S'')-(+)-norketamine and (''R'')-(–)-norketamine, respectively). Also, similarly again to ketamine, norketamine binds to the μ- and κ-opioid receptors. Relative to ketamine, norketamine is much more potent as an antagonist of the α7-nicotinic acetylcholine receptor, and produces rapid antidepressant effects in animal models which have been reported to correlate with its activity at this receptor. However, norketamine is about 1/5 as potent as ketamine as an antidepressant in mice as per the forced swim test, and this seems also to be in accordance with i ...
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Anesthesia
Anesthesia (American English) or anaesthesia (British English) is a state of controlled, temporary loss of sensation or awareness that is induced for medical or veterinary purposes. It may include some or all of analgesia (relief from or prevention of pain), paralysis (muscle relaxation), amnesia (loss of memory), and unconsciousness. An individual under the effects of anesthetic drugs is referred to as being anesthetized. Anesthesia enables the painless performance of procedures that would otherwise require physical restraint in a non-anesthetized individual, or would otherwise be technically unfeasible. Three broad categories of anesthesia exist: * ''General anesthesia'' suppresses central nervous system activity and results in unconsciousness and total lack of Sensation (psychology), sensation, using either injected or inhaled drugs. * ''Sedation'' suppresses the central nervous system to a lesser degree, inhibiting both anxiolysis, anxiety and creation of long-term memory, ...
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Hallucinogen
Hallucinogens, also known as psychedelics, entheogens, or historically as psychotomimetics, are a large and diverse class of psychoactive drugs that can produce altered states of consciousness characterized by major alterations in thought, mood, and perception as well as other changes. Hallucinogens are often categorized as either being psychedelics, dissociatives, or deliriants, but not all hallucinogens fall into these three classes. Examples of hallucinogens include psychedelics or serotonin 5-HT2A receptor agonists like LSD, psilocybin, mescaline, and DMT; dissociatives or NMDA receptor antagonists like ketamine, PCP, DXM, and nitrous oxide; deliriants or antimuscarinics like scopolamine and diphenhydramine; cannabinoids or cannabinoid CB1 receptor agonists like THC, nabilone, and JWH-018; κ-opioid receptor agonists like salvinorin A and pentazocine; GABAA receptor agonists like muscimol and gaboxadol; and oneirogens like ibogaine and harmaline, a ...
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General Anaesthetic
General anaesthetics (or anesthetics) are often defined as compounds that induce a loss of consciousness in humans or loss of righting reflex in animals. Clinical definitions are also extended to include an induced coma that causes lack of awareness to painful stimuli, sufficient to facilitate surgical applications in clinical and veterinary practice. General anaesthetics do not act as analgesics and should also not be confused with sedatives. General anaesthetics are a structurally diverse group of compounds whose mechanisms encompass multiple biological targets involved in the control of neuronal pathways. The precise workings are the subject of some debate and ongoing research. General anesthetics elicit a state of General anaesthesia, general anesthesia. It remains somewhat controversial regarding how this state should be defined. General anesthetics, however, typically elicit several key reversible effects: immobility, analgesia, amnesia, unconsciousness, and reduced autonomi ...
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Cyclohexanone
Cyclohexanone is the organic compound with the formula (CH2)5CO. The molecule consists of six-carbon cyclic molecule with a ketone functional group. This colorless oily liquid has a sweet odor reminiscent of benzaldehyde. Over time, samples of cyclohexanone assume a pale yellow color. Cyclohexanone is slightly soluble in water and miscible with common organic solvents. Millions of tonnes are produced annually, mainly as a precursor to nylon. History and synthesis The compound was discovered by in 1888 among the products of AC electrolysis of slightly acidified water solutions of phenol. He named it hydrophenoketone and correctly suggested that phenol was first hydrogenated by electrolytic hydrogen to cyclohexanol, which he wasn't able to isolate, and then oxidized by electrolytic oxygen. Laboratory synthesis Cyclohexanone can be prepared from cyclohexanol by oxidation with chromium trioxide ( Jones oxidation). An alternative method utilizes the safer and more readily avai ...
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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 ...
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Esketamine
Esketamine, sold under the brand names Spravato (for depression (mood), depression) and Ketanest (for anesthesia) among others, is the ''S''(+) enantiomer of ketamine. It is a dissociative hallucinogen drug used as a general anesthetic and as an antidepressant for treatment of depression (mood), depression. Esketamine is the biological activity, active enantiomer of ketamine in terms of NMDA receptor antagonist, NMDA receptor antagonism and is more potency (pharmacology), potent than racemic ketamine. It is specifically used as a therapy for treatment-resistant depression (TRD) and for major depressive disorder (MDD) with co-occurring suicidal ideation or Suicide, behavior. Its efficacy for depression is modest and similar to that of other antidepressants. Esketamine is not used by Intravenous therapy, infusion into a vein for depression as it is only Food and Drug Administration, FDA-approved in the form of a nasal spray under direct medical supervision for this indication (th ...
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Racemic Mixture
In chemistry, a racemic mixture or racemate () is a mixture that has equal amounts (50:50) of left- and right-handed enantiomers of a chiral molecule or salt. Racemic mixtures are rare in nature, but many compounds are produced industrially as racemates. History The first known racemic mixture was racemic acid, which Louis Pasteur found to be a mixture of the two enantiomeric isomers of tartaric acid. He manually separated the crystals of a mixture, starting from an aqueous solution of the sodium ammonium salt of racemate tartaric acid. Pasteur benefited from the fact that ammonium tartrate salt gives enantiomeric crystals with distinct crystal forms (at 77 °F). Reasoning from the macroscopic scale down to the molecular, he reckoned that the molecules had to have non-superimposable mirror images. A sample with only a single enantiomer is an ''enantiomerically pure'' or ''enantiopure'' compound. Etymology The word ''racemic'' derives from Latin , meaning pertaining to a ...
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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 ...
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Esketamine
Esketamine, sold under the brand names Spravato (for depression (mood), depression) and Ketanest (for anesthesia) among others, is the ''S''(+) enantiomer of ketamine. It is a dissociative hallucinogen drug used as a general anesthetic and as an antidepressant for treatment of depression (mood), depression. Esketamine is the biological activity, active enantiomer of ketamine in terms of NMDA receptor antagonist, NMDA receptor antagonism and is more potency (pharmacology), potent than racemic ketamine. It is specifically used as a therapy for treatment-resistant depression (TRD) and for major depressive disorder (MDD) with co-occurring suicidal ideation or Suicide, behavior. Its efficacy for depression is modest and similar to that of other antidepressants. Esketamine is not used by Intravenous therapy, infusion into a vein for depression as it is only Food and Drug Administration, FDA-approved in the form of a nasal spray under direct medical supervision for this indication (th ...
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Feces
Feces (also known as faeces American and British English spelling differences#ae and oe, or fæces; : faex) are the solid or semi-solid remains of food that was not digested in the small intestine, and has been broken down by bacteria in the large intestine. Feces contain a relatively small amount of metabolic waste products such as bacterially-altered bilirubin and dead epithelial cells from the lining of the gut. Feces are discharged through the anus or cloaca during defecation. Feces can be used as fertilizer or soil conditioner in agriculture. They can also be burned as dry animal dung fuel, fuel or dried and used for wattle and daub, construction. Some medicinal uses have been found. In the case of human feces, fecal transplants or fecal bacteriotherapy are in use. Urine and feces together are called excretion, excreta. Characteristics The distinctive odor of feces is due to skatole, and thiols (sulfur-containing compounds), as well as amines and carboxylic acids. Sk ...
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