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EMD-386088
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 RU-28253 is a non-selective serotonin receptor agonist of the tryptamine and 5-methoxytryptamine families. It is a tetrahydropyridylindole and a conformationally constrained analogue of 5-MeO-DMT. The drug shows high affinity for the serotonin ... * ST-1936 References 5-HT6 agonists Chloroa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RU-24,969
RU-24,969 is a serotonin receptor modulator related to 5-MeO-DMT which is used in scientific research. It is a selective agonist of the serotonin 5-HT1A and 5-HT1B receptors, with 5-fold preference for the latter receptor over the former. In studies, its affinities (Ki) were 2nM for the serotonin 5-HT1 receptor, 5nM for the serotonin 5-HT1A receptor, 4nM for the serotonin 5-HT1B receptor, 780 to 1,000nM for the serotonin 5-HT2 receptor, and 400nM for the serotonin 5-HT2C receptor. It also has affinity for the serotonin 5-HT5A, 5-HT5B, and 5-HT7 receptors. The drug produces MDMA-like locomotor hyperactivity in animals and this is thought to be mediated by activation of both serotonin 5-HT1A and 5-HT1B receptors. As with other serotonin 5-HT1B receptor agonists such as CP-94,253, RU-24,969 has also been found to increase the reinforcing properties of cocaine in animals, suggesting a role for serotonin 5-HT1B receptors in cocaine addiction as well. RU-24,969 was first de ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RU-28253
RU-28253 is a non-selective serotonin receptor agonist of the tryptamine and 5-methoxytryptamine families. It is a tetrahydropyridylindole and a conformationally constrained analogue of 5-MeO-DMT. The drug shows high affinity for the serotonin 5-HT1A receptor (Ki = 5.7nM) and lower affinity for the serotonin 5-HT2A receptor (Ki = 230nM). Its affinities for these receptors were higher than those of dimethyltryptamine (DMT). RU-28253 is described as a potent agonist of the serotonin 5-HT1 and 5-HT2 receptors, including of the serotonin 5-HT1B receptor, and is also an agonist of the serotonin 5-HT4 receptor. RU-28253 was first described in the scientific literature by 1983. See also * Cyclized tryptamine * VU6067416 * RS134-49 * (''R'')-69 * RU-24,969 * EMD-386088 * SN-22 * MPMI * Pyr-T Pyr-T, also known as ''N'',''N''-tetramethylenetryptamine or as 3-(2-pyrrolidinoethyl)indole, is a lesser-known serotonin receptor modulator of the tryptamine family. It is the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indole
Indole is an organic compound with the formula . Indole is classified as an aromatic heterocycle. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indoles are derivatives of indole where one or more of the hydrogen atoms have been replaced by substituent groups. Indoles are widely distributed in nature, most notably as amino acid tryptophan and neurotransmitter serotonin. General properties and occurrence Indole is a solid at room temperature. It occurs naturally in human feces and has an intense fecal odor. At very low concentrations, however, it has a flowery smell, and is a constituent of many perfumes. It also occurs in coal tar. It has been identified in cannabis. It is the main volatile compound in stinky tofu. When indole is a substituent on a larger molecule, it is called an ''indolyl group'' by systematic nomenclature. Indole undergoes electrophilic substitution, mainly at position 3 (see diagram in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloroarenes
In organic chemistry, an aryl halide (also known as a haloarene) is an aromatic compound in which one or more hydrogen atoms directly bonded to an aromatic ring are replaced by a halide ion (such as fluorine F''−'', chlorine Cl−1,−3,−5, bromine Br−1, or iodine I−). Aryl halides are distinct from haloalkanes (alkyl halides) due to significant differences in their methods of preparation, chemical reactivity, and physical properties. The most common and important members of this class are aryl chlorides, but the group encompasses a wide range of derivatives with diverse applications in organic synthesis, pharmaceuticals, and materials science. Classification according to halide Aryl fluorides Aryl fluorides are used as synthetic intermediates, e.g. for the preparation of pharmaceuticals, pesticides, and liquid crystals. The conversion of diazonium salts is a well established route to aryl fluorides. Thus, anilines are precursors to aryl fluorides. In the classic Schiemann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Reuptake Inhibitor
A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. DRIs are used in the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy for their psychostimulant effects, and in the treatment of obesity and binge eating disorder for their appetite suppressant effects. They are sometimes used as antidepressants in the treatment of mood disorders, but their use as antidepressants is limited given that strong DRIs have a high abuse potential and legal restrictions on their use. Lack of dopamine reuptake and the increase in extracellular levels of dopamine have been l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT3 Receptor
The 5-HT3 receptor belongs to the Cys-loop superfamily of ligand-gated ion channels (LGICs) and therefore differs structurally and functionally from all other 5-HT receptors (5-hydroxytryptamine, or serotonin receptors) which are G-protein-coupled receptor, G protein-coupled receptors. This ion channel is cation-selective and mediates neuronal depolarization and excitation within the Central nervous system, central and Peripheral nervous system, peripheral nervous systems. As with other ligand gated ion channels, the 5-HT3 receptor consists of five subunits arranged around a central ion conducting pore, which is permeable to sodium (Na), potassium (K), and calcium (Ca) ions. Binding of the neurotransmitter 5-hydroxytryptamine (serotonin) to the 5-HT3 receptor opens the channel, which, in turn, leads to an excitatory response in neurons. The rapidly activating, desensitizing, inward current is predominantly carried by sodium and potassium ions. 5-HT3 receptors have a negligible perme ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EMDT
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 * BGC20-761 * EMD-386,088 * 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 {{DEFAULTSORT:Ethyl-5-met ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
