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Caleicine
Caleicine is a unique sesquiterpene compound found exclusively in ''Calea ternifolia'', a Mexican flowering plant known for its potential psychoactive properties. This compound has garnered interest in the field of ethnopharmacology and natural product chemistry due to its putative role as a prodrug of eugenol, a potent GABAA receptor positive allosteric modulator, GABA positive modulator. Caleicine is the P-Coumaric acid, ''p''-Coumaric ester of junenol and has no lactone moiety making it distinctly unique from the other sesquiterpene lactones in Calea ternifolia. Chemistry Caleicine is a sesquiterpene that has a phenylpropanoid moiety bonded to junenol In an investigation, Laboratory mouse, lab mice were administered with an aqueous solution of Calea ternifolia, ''Calea ternifolia'' in doses of 200, 400 and 800 mg and made to undergo a Behavioural despair test, forced swim test. Under dosages of 400 and 800 mg, the mice showed Sedative, depressive like effects. ...
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Calea Ternifolia
''Calea ternifolia'' ( syn. ''Calea zacatechichi'') is a species of flowering plant in the aster family, Asteraceae. It is native to Mexico and Central America. Its English language common names include bitter-grass, Mexican calea, and dream herb.Simonienko, K., et al. (2013)Psychoactive plant species – actual list of plants prohibited in Poland. ''Psychiatria Polska'' XLVII(3), 499–508. It is used in traditional medicine and ritual in its native range.Ferraz, A., et al. (2009)Pharmacological and genotoxic evaluation of ''Calea clematidea'' and ''Calea uniflora''.''Latin American Journal of Pharmacy'' 28(6), 858-6/ref> Uses In Mexico the plant is used as a herbalism, herbal remedy for dysentery and fever. The Zoque Popoluca people call the plant ''tam huñi'' ("bitter gum") and use it to treat diarrhea and asthma, and the Mixe people know it as ''poop taam ujts'' ("white bitter herb") and use it for stomachache and fever. The Chontal people of Oaxaca reportedly use th ...
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Eugenol
Eugenol is an allyl chain-substituted guaiacol, a member of the allylbenzene class of chemical compounds. It is a colorless to pale yellow, aromatic oily liquid extracted from certain essential oils especially from clove, nutmeg, cinnamon, basil and bay leaf. It is present in concentrations of 80–90% in clove bud oil and at 82–88% in clove leaf oil. Eugenol has a pleasant, spicy, clove-like scent. The name is derived from ''Eugenia caryophyllata'', the former Linnean nomenclature term for cloves. The currently accepted name is ''Syzygium aromaticum''. Biosynthesis The biosynthesis of eugenol begins with the amino acid tyrosine. L-tyrosine is converted to ''p''-coumaric acid by the enzyme tyrosine ammonia lyase (TAL). From here, ''p''-coumaric acid is converted to caffeic acid by ''p''-coumarate 3-hydroxylase using oxygen and NADPH. ''S''-Adenosyl methionine (SAM) is then used to methylate caffeic acid, forming ferulic acid, which is in turn converted to feruloyl- ...
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Eugenol Biosynthesis
Eugenol is an allyl chain-substituted guaiacol, a member of the allylbenzene class of chemical compounds. It is a colorless to pale yellow, aromatic oily liquid extracted from certain essential oils especially from clove, nutmeg, cinnamon, basil and bay leaf. It is present in concentrations of 80–90% in clove bud oil and at 82–88% in clove leaf oil. Eugenol has a pleasant, spicy, clove-like scent. The name is derived from ''Eugenia caryophyllata'', the former Linnean nomenclature term for cloves. The currently accepted name is ''Syzygium aromaticum''. Biosynthesis The biosynthesis of eugenol begins with the amino acid tyrosine. L-tyrosine is converted to ''p''-coumaric acid by the enzyme tyrosine ammonia lyase (TAL). From here, ''p''-coumaric acid is converted to caffeic acid by ''p''-coumarate 3-hydroxylase using oxygen and NADPH. ''S''-Adenosyl methionine (SAM) is then used to methylate caffeic acid, forming ferulic acid, which is in turn converted to feruloyl- CoA by t ...
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Sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or Psychomotor agitation, excitement. They are central nervous system (CNS) Depressant, depressants and interact with brain activity, causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter Gamma-Aminobutyric acid, gamma-aminobutyric acid (GABA). Most sedatives produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or Anxiolytic, relieve anxiety, whereas the term ''hypnotic'' describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness), they are often referred to collectively as ''sedative–hypnotic'' drugs. Terminology There is some overlap ...
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GABAA Receptor Positive Allosteric Modulator
In pharmacology, GABAA receptor positive allosteric modulators, also known as GABAkines or GABAA receptor potentiators, are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it triggers the GABAA receptor to open its chloride channel to allow chloride ions into the neuron, making the cell hyperpolarized and less likely to fire. GABAA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present. Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-aminobutyric acid (GABA) neurotransmitter molecule: they affect the receptor by binding at a different site on the protein. This is called allosteric modulation. In psychopharmacology, GABAA receptor PAMs u ...
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Propofol
Propofol is the active component of an intravenous anesthetic formulation used for induction and maintenance of general anesthesia. It is chemically termed 2,6-diisopropylphenol. The formulation was approved under the brand name Diprivan. Numerous generic versions have since been released. Intravenous administration is used to induce unconsciousness after which anesthesia may be maintained using a combination of medications. It is manufactured as part of a sterile injectable emulsion formulation using soybean oil and lecithin, giving it a white milky coloration. Recovery from propofol-induced anesthesia is generally rapid and associated with less frequent side effects (e.g., drowsiness, nausea, vomiting) compared to other anesthetic agents. Propofol may be used prior to diagnostic procedures requiring anesthesia, in the management of refractory status epilepticus, and for induction or maintenance of anesthesia prior to and during surgeries. It may be administered as a bolus ...
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Alcohol (drug)
Alcohol, sometimes referred to by the chemical name ethanol, is the active ingredient in alcoholic drinks such as beer, wine, and distilled spirits (hard liquor). Alcohol is a central nervous system (CNS) depressant, decreasing Action potential, electrical activity of neurons in the brain, which causes the characteristic effects of alcohol intoxication ("drunkenness"). Among other effects, alcohol produces euphoria, anxiolytic, decreased anxiety, increased sociability, sedation, and impairment of cognitive, memory, motor control, motor, and sense, sensory function. Alcohol has a variety of adverse effects. Short-term effects of alcohol consumption, Short-term adverse effects include generalized impairment of neurocognitive function, dizziness, nausea, vomiting, and symptoms of hangover. Alcohol is addiction, addictive and can result in alcohol use disorder, Substance dependence, dependence, and Alcohol withdrawal syndrome, withdrawal upon cessation. The long-term effects of ...
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Methaqualone
Methaqualone is a hypnotic sedative. It was sold under the brand names Quaalude ( ) and Sopor among others, which contained 300 mg of methaqualone, and sold as a combination drug under the brand name Mandrax, which contained 250 mg methaqualone and 25 mg diphenhydramine within the same tablet, mostly in Europe. Commercial production of methaqualone was halted in the mid-1980s due to widespread abuse and addictiveness. It is a member of the quinazolinone class. Medical use The sedative–hypnotic activity of methaqualone was recognized in 1955. Its use peaked in the early 1970s for the treatment of insomnia, and as a sedative and muscle relaxant. Methaqualone was not recommended for use while pregnant and is in pregnancy category D. Similar to other GABAergic agents, methaqualone will produce tolerance and physical dependence with extended periods of use. Overdose An overdose of methaqualone can lead to coma and death. Additional effects are delirium, con ...
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Deliriant
Deliriants are a subclass of hallucinogen. The term was coined in the early 1980s to distinguish these drugs from psychedelics such as LSD and dissociatives such as ketamine, due to their primary effect of causing delirium, as opposed to the more lucid and less disturbed states produced by other types of hallucinogens, where rational thought is better preserved (including the ability to distinguish hallucinations from reality). Duncan, D. F., and Gold, R. S. (1982). Drugs and the Whole Person. New York: John Wiley & Sons The term generally refers to anticholinergic drugs, which are substances that inhibit the function of the neurotransmitter acetylcholine. Common examples of deliriants include plants of the genera ''Datura'' and '' Brugmansia'', both containing scopolamine, as well as higher than recommended dosages of diphenhydramine (Benadryl). A number of plant deliriants such as that of the Solanaceae family, particularly in the Americas, have been used by some indi ...
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Oneirogen
An oneirogen, from the Greek ὄνειρος ''óneiros'' meaning "dream" and ''gen'' "to create", is a substance that induces a dream-like state of consciousness. Oneirogens function by altering neural processing in a way that shifts the brain from bottom-up sensory input to top-down generative activity, resembling the mechanisms involved in dreaming. This neural shift is associated with increased internal imagery and reduced responsiveness to external stimuli. Psychedelics—particularly those acting on the 5-HT2A receptor—produce oneirogenic effects by promoting this altered balance of neural signaling. List of oneirogens * '' Calea zacatechichi'' ("''Calea ternifolia''") has been traditionally used in Central America as a believed way to potentiate lucid dreams and perform dream divination. It can promote dreams vivid to the senses, sight, scent, hearing, touch, and taste. May be taken as a tea or smoked. * '' Entada rheedii'' ("African dream bean") * Mugwort, see Ar ...
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Nausea
Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. It can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the throat. Over 30 definitions of nausea were proposed in a 2011 book on the topic. Nausea is a non-specific symptom, which means that it has many possible causes. Some common causes of nausea are gastroenteritis and other gastrointestinal disorders, food poisoning, motion sickness, dizziness, migraine, fainting, low blood sugar, anxiety, hyperthermia, dehydration and lack of sleep. Nausea is a side effect of many medications including chemotherapy, or morning sickness in early pregnancy. Nausea may also be caused by disgust and depression. Medications taken to prevent and treat nausea and vomiting are called antiemetics. The most commonly prescribed antiemetics in the US are promethazine, metoclopramide, and the newer ondansetron. The word na ...
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GABAergic
In molecular biology and physiology, something is GABAergic or GABAnergic if it pertains to or affects the neurotransmitter gamma-aminobutyric acid (GABA). For example, a synapse is GABAergic if it uses GABA as its neurotransmitter, and a GABAergic neuron produces GABA. A substance is GABAergic if it produces its effects via interactions with the GABA system, such as by stimulating or blocking neurotransmission. A GABAergic or GABAnergic agent is any chemical that modifies the effects of GABA in the body or brain. Some different classes of GABAergic drugs include agonists, antagonists, modulators, reuptake inhibitors and enzymes. See also * Adenosinergic * Adrenergic * Cannabinoidergic * Cholinergic * Dopaminergic Dopaminergic means "related to dopamine" (literally, "working on dopamine"), a common neurotransmitter. Dopaminergic substances or actions increase dopamine-related activity in the brain. Dopaminergic pathways, Dopaminergic brain pathways facil ... * Glutamat ...
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