2-Ethyl-5-methoxy-DMT
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2-Ethyl-5-methoxy-DMT
2-Ethyl-5-methoxy-''N'',''N''-dimethyltryptamine (EMDT), also known as 2-ethyl-5-MeO-DMT, is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT6 receptor agonist, with a Ki of 16nM, and was one of the first selective agonists developed for this receptor. Its affinities for many other targets have also been reported. EMDT inhibits both short- and long-term memory formation in animal studies, and this effect can be reversed by the selective 5-HT6 antagonist SB-399,885. Additionally, it is active in the tail suspension test, suggesting that it could be an effective antidepressant. See also * 2-Methyltryptamine 2-Methyltryptamine (2-MT, 2-Me-T, or 2-methyl-T) is a serotonin receptor agonist of the substituted tryptamine, tryptamine family. It shows dramatically reduced activity at serotonin receptors compared to tryptamine and mixed effects in terms of ... * BGC20-761 * EMD-386,088 * ST-1936 References {{DEFAULTSORT:Ethyl-5 ...
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2-Methyltryptamine
2-Methyltryptamine (2-MT, 2-Me-T, or 2-methyl-T) is a serotonin receptor agonist of the substituted tryptamine, tryptamine family. It shows dramatically reduced activity at serotonin receptors compared to tryptamine and mixed effects in terms of head-twitch response, psychedelic-like effects in animals. Pharmacology 2-MT shows affinity (pharmacology), affinity (Ki) for the serotonin 5-HT1A receptor, 5-HT1A and 5-HT2A receptor, 5-HT2A receptors, with Ki values of 1,095nM and 7,774nM, respectively. These affinities were respectively 34-fold and 3.2-fold lower than those of tryptamine in the same study. It also acts as an agonist of the serotonin 5-HT1A and 5-HT2A receptors, with values of 12,534nM and 4,598nM, respectively. These receptor activation, activational potency (pharmacology), potencies were respectively 14-fold and 19-fold lower than those of tryptamine in the same study. It does not produce conditioned place preference (CPP), self-administration, or changes in locomoto ...
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2-Alkyltryptamines
2-Methyltryptamine (2-MT, 2-Me-T, or 2-methyl-T) is a serotonin receptor agonist of the tryptamine family. It shows dramatically reduced activity at serotonin receptors compared to tryptamine and mixed effects in terms of psychedelic-like effects in animals. Pharmacology 2-MT shows affinity (Ki) for the serotonin 5-HT1A and 5-HT2A receptors, with Ki values of 1,095nM and 7,774nM, respectively. These affinities were respectively 34-fold and 3.2-fold lower than those of tryptamine in the same study. It also acts as an agonist of the serotonin 5-HT1A and 5-HT2A receptors, with values of 12,534nM and 4,598nM, respectively. These activational potencies were respectively 14-fold and 19-fold lower than those of tryptamine in the same study. It does not produce conditioned place preference (CPP), self-administration, or changes in locomotor activity in rodents. Findings on whether 2-MT produces the head-twitch response (HTR), a behavioral proxy of psychedelic effects, are mixed. In ...
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Tryptamine
Tryptamine is an indolamine metabolite of the essential amino acid tryptophan. The chemical structure is defined by an indole—a fused benzene and pyrrole ring, and a 2-aminoethyl group at the second carbon (third aromatic atom, with the first one being the heterocyclic nitrogen). The structure of tryptamine is a shared feature of certain aminergic neuromodulators including melatonin, serotonin, bufotenin and psychedelic derivatives such as dimethyltryptamine (DMT), psilocybin, psilocin and others. Tryptamine has been shown to activate serotonin receptors and trace amine-associated receptors expressed in the mammalian brain, and regulates the activity of dopaminergic, serotonergic and glutamatergic systems. In the human gut, bacteria convert dietary tryptophan to tryptamine, which activates 5-HT4 receptors and regulates gastrointestinal motility. Multiple tryptamine-derived drugs have been developed to treat migraines, while trace amine-associated receptors are bei ...
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Tail Suspension Test
The tail suspension test (TST) is an experimental method used in scientific research to measure stress in rodents. It is based on the observation that if a mouse is subjected to short term inescapable stress then the mouse will become immobile. It is used to measure the effectiveness of antidepressant-like agents but there is significant controversy over its interpretation and usefulness. History The TST was introduced in 1985 due to the popularity of a similar test called the forced swim test (FST). However this test only recently became popular in the 2000s where data has shown that animals do show a change in behavior when injected with antidepressants. TST is more reliable when done in conjunction with other depression models such as FST, learned helplessness, anhedonia models and olfactory bulbectomy. Modeling depression Depression is a complex multi-faceted disorder with symptoms that can have multiple causes such as psychological, behavioral, and genetics. Sinc ...
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5-HT6 Agonists
The 5HT6 receptor is a subtype of 5HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5HT). It is a G protein-coupled receptor (GPCR) that is coupled to Gs and mediates excitatory neurotransmission. ''HTR6'' denotes the human gene encoding for the receptor. Distribution The 5HT6 receptor is expressed almost exclusively in the brain. It is distributed in various areas including, but not limited to, the olfactory tubercle, cerebral cortex ( frontal and entorhinal regions), nucleus accumbens, striatum, caudate nucleus, hippocampus, and the molecular layer of the cerebellum. Based on its abundance in extrapyramidal, limbic, and cortical regions it can be suggested that the 5HT6 receptor plays a role in functions like motor control, emotionality, cognition, and memory. Function Blockade of central 5HT6 receptors has been shown to increase glutamatergic and cholinergic neurotransmission in various brain areas, whereas activation enhances GABAe ...
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ST-1936
ST-1936, also known as 2-methyl-5-chloro-''N'',''N''-dimethyltryptamine (2-methyl-5-chloro-DMT), is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT6 receptor agonist, with a Ki of 13 nM, and much weaker action at 5-HT2B and 5-HT7 subtypes. In animal studies it has been found to increase dopamine and noradrenaline mediated signalling but decreases glutamatergic transmission, and has antidepressant effects. See also * 2-Methyltryptamine 2-Methyltryptamine (2-MT, 2-Me-T, or 2-methyl-T) is a serotonin receptor agonist of the substituted tryptamine, tryptamine family. It shows dramatically reduced activity at serotonin receptors compared to tryptamine and mixed effects in terms of ... * EMD-386,088 * EMDT * 5-Bromo-DMT * 5-Chloro-AMT References {{Tryptamines 5-HT6 agonists 2-Alkyltryptamines Chloroarenes N,N-Dialkyltryptamines 5-Halotryptamines ...
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EMD-386,088
EMD-386088 is an indole derivative which is used in scientific research. It acts as a potent 5-HT6 receptor partial agonist, with a Ki of 1 nM, a significantly higher affinity than older 5-HT6 agonists such as EMDT, although it possesses moderate affinity for the 5-HT3 receptor as well. Subsequent research has determined that EMD-386088 is also a dopamine reuptake inhibitor and that this action is involved in the antidepressant-like effects of the drug in rodents. EMD-386088 can be further reacted with a butyrophenone sidechain.Genus Possanza, Kurt Freter, & Sven Luttke, (1976 to Boehringer Ingelheim GmbH). See also * 2-Methyltryptamine * EMDT * RU-24,969 * RU-28253 * ST-1936 ST-1936, also known as 2-methyl-5-chloro-''N'',''N''-dimethyltryptamine (2-methyl-5-chloro-DMT), is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT6 receptor agonist, with a Ki of 13 nM, and much weake ... References 5-HT6 agonists Chloroaren ...
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BGC20-761
BGC20-761 (5-MeO-2-phenyl-DMT, PMDT) is an experimental drug which acts as an antagonist of the 5-HT6, 5-HT2 family, and dopamine D2 receptors, with strongest affinity for 5-HT6. In animal studies it has antipsychotic-like effects, but also memory enhancing action attributed to its 5-HT6 affinity. See also * EMDT * ST-1936 ST-1936, also known as 2-methyl-5-chloro-''N'',''N''-dimethyltryptamine (2-methyl-5-chloro-DMT), is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT6 receptor agonist, with a Ki of 13 nM, and much weake ... References {{Tryptamines 5-Methoxytryptamines N,N-Dialkyltryptamines Experimental drugs Serotonin receptor modulators ...
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Antidepressant
Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathisia, sexual dysfunction, and emotional blunting. There is an increased risk of Suicidal ideation, suicidal thinking and Suicide, behavior when taken by children, adolescents, and young adults. Antidepressant discontinuation syndrome, Discontinuation syndrome, which resembles recurrent Depression (mood), depression in the case of the Selective serotonin reuptake inhibitor, SSRI class, may occur after stopping the intake of any antidepressant. Research regarding the effectiveness of antidepressants for depression in adults is controversial and has found both benefits and drawbacks. Meanwhile, evidence of benefit in children and adolescents is unclear, even though antidepressant use has considerably increased in children and adolescents in th ...
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SB-399,885
SB-399885 is a drug which is used in scientific research. It acts as a potent, selective and orally active 5-HT6 receptor antagonist, with a Ki of 9.0nM. SB-399885 and other 5-HT6 antagonists show nootropic effects in animal studies, as well as antidepressant and anxiolytic effects which are comparable to and synergistic with drugs such as imipramine and diazepam, and have been proposed as potential novel treatments for cognitive disorders such as schizophrenia and Alzheimer's disease Alzheimer's disease (AD) is a neurodegenerative disease and the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in remembering recent events. As the disease advances, symptoms can include problems wit .... References 5-HT6 antagonists Methoxy compounds Sulfonamides Chlorobenzene derivatives 1-Piperazinyl compounds {{nervous-system-drug-stub ...
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Scientific Research
The scientific method is an empirical method for acquiring knowledge that has been referred to while doing science since at least the 17th century. Historically, it was developed through the centuries from the ancient and medieval world. The scientific method involves careful observation coupled with rigorous skepticism, because cognitive assumptions can distort the interpretation of the observation. Scientific inquiry includes creating a testable hypothesis through inductive reasoning, testing it through experiments and statistical analysis, and adjusting or discarding the hypothesis based on the results. Although procedures vary across fields, the underlying process is often similar. In more detail: the scientific method involves making conjectures (hypothetical explanations), predicting the logical consequences of hypothesis, then carrying out experiments or empirical observations based on those predictions. with added notes. Reprinted with previously unpublished part, ...
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