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TFMBOX
TFMBOX is a putative serotonergic psychedelic of the phenethylamine and benzoxepin ("BOX") families. It is the cyclized phenethylamine analogue of DOTFM and 2C-TFM in which the α carbon has been connected to the 2-methoxy group via an ethyl chain to form a benzoxepin ring system. The drug was assessed at and showed affinity for the serotonin 5-HT2A and 5-HT1A receptors, with Ki values of 340nM and 1,300nM, respectively. Its affinity for the serotonin 5-HT2A receptor was about 15-fold lower than that of DOB and DOI, whereas its affinity for the serotonin 5-HT1A receptor was the same as that of DOI and was about half that of DOB. TFMBOX also very weakly inhibited the reuptake of serotonin ( = 9,900nM), but did not affect dopamine or norepinephrine reuptake ( = >50,000–100,000nM). The drug fully substituted for LSD in rodent drug discrimination tests, albeit with about one-third of the potency of DOB and 2C-B. TFMBOX was first described in the scientific literature by N ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Substituted Phenethylamine
Substituted phenethylamines (or simply phenethylamines) are a chemical class of organic compounds that are based upon the phenethylamine structure; the class is composed of all the derivative (chemistry), derivative compounds of phenethylamine which can be formed by replacing, or substitution reaction, substituting, one or more hydrogen atoms in the phenethylamine core structure with substituents. Phenylethylamines are also generally found to be central nervous system stimulants with many also being entactogens/empathogens, and hallucinogens. Structural classification The structural formula of any substituted phenethylamine contains a phenyl group, phenyl ring that is joined to an amino group, amino (NH) group via a two-carbon substituent, sidechain. Hence, any substituted phenethylamine can be classified according to the substitution of hydrogen atom, hydrogen (H) atoms on phenethylamine's phenyl ring, sidechain, or amino group with a moiety (chemistry), specific group of at ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzoxepin
Benzoxepin (BOX) is an oxygen-containing bicyclic molecule consisting of an oxepin ring and a benzene ring. There are three isomers, varying in where the oxygen is positioned in the oxepin heterocycle relative where the benzene is fused to it. Natural occurrence 1-Benzoxepin, with the oxygen closest to the benzene, is found in the skeleton of several fungal metabolites. 2-Benzoxepin skeletons are likewise found in fungal metabolites. 3-Benzoxepin, with the oxygen furthest from the benzene, is the core of natural products such as perilloxin from ''Perilla frutescens'' (variant Acuta) and tenual and tenucarb from '' Asphodeline tenuior''. : Derivatives Certain substituted benzoxepins, like TFMBOX, are serotonergic psychedelic Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary mental states (known as psychedelic experiences or "trips") and a perceived "expansion of consciousness". Also referred to as classic halluc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclized Phenethylamine
Substituted phenethylamines (or simply phenethylamines) are a chemical class of organic compounds that are based upon the phenethylamine structure; the class is composed of all the derivative compounds of phenethylamine which can be formed by replacing, or substituting, one or more hydrogen atoms in the phenethylamine core structure with substituents. Phenylethylamines are also generally found to be central nervous system stimulants with many also being entactogens/empathogens, and hallucinogens. Structural classification The structural formula of any substituted phenethylamine contains a phenyl ring that is joined to an amino (NH) group via a two-carbon sidechain. Hence, any substituted phenethylamine can be classified according to the substitution of hydrogen (H) atoms on phenethylamine's phenyl ring, sidechain, or amino group with a specific group of atoms. Several classes of substances can be considered phenylethylamine derivatives such as Substituted amphetamines, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Modulator
5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in multiple tissues including the central and peripheral nervous systems. They mediate both excitatory and inhibitory neurotransmission. The serotonin (i.e., 5-hydroxytryptamine, hence "5-HT") receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. Serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. They are the target of a variety of pharmaceutical and recreational drugs, includin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Reuptake
Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the pre-synaptic neuron at a synapse) or glial cell after it has performed its function of transmitting a neural impulse. Reuptake is necessary for normal synaptic physiology because it allows for the recycling of neurotransmitters and regulates the level of neurotransmitter present in the synapse, thereby controlling how long a signal resulting from neurotransmitter release lasts. Because neurotransmitters are too large and hydrophilic to diffuse through the membrane, specific transport proteins are necessary for the reabsorption of neurotransmitters. Much research, both biochemical and structural, has been performed to obtain clues about the mechanism of reuptake. Protein structure The first primary sequence of a reuptake protein was published in 1990. The technique for protein sequence determination relied upon the purification, s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOI (drug)
2,5-Dimethoxy-4-iodoamphetamine (DOI) is a psychedelic drug of the amphetamine and 4-substituted-2,5-dimethoxyamphetamine (DOx) families. It is relatively little-used as a recreational drug but is frequently used in scientific research in the study of psychedelics and serotonin receptors. DOI acts as a potent serotonin 5-HT2 receptor agonist, including of the serotonin 5-HT2A and 5-HT2C receptors. The compound has a stereocenter, and ''R''-(−)-DOI is the more active stereoisomer. 125I">sup>125I''R''-(−)-DOI is used as a radioligand and indicator of the presence of serotonin 5-HT2A receptors in studies. DOI's effects have been compared to LSD, although there are differences that experienced users can distinguish. Besides the longer duration of DOI compared to LSD, the trip tends to be more energetic than an LSD trip, with more body load and a different subjective visual experience. The after effects include residual stimulation and difficulty sleeping, which, depen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Reuptake Inhibitor
A serotonin reuptake inhibitor (SRI) is a type of drug which acts as a reuptake inhibitor of the neurotransmitter serotonin (5-hydroxytryptamine, or 5-HT) by blocking the drug action, action of the serotonin transporter (SERT). This in turn leads to increased extracellular concentrations of serotonin and, therefore, an increase in Serotonin, serotonergic neurotransmission. It is a type of monoamine reuptake inhibitor (MRI); other types of MRIs include dopamine reuptake inhibitors and norepinephrine reuptake inhibitors. SRIs are not synonymous with selective serotonin reuptake inhibitors (SSRIs), as the latter term is usually used to describe the chemical class, class of antidepressants of the same name, and because SRIs, unlike SSRIs, can either be binding selectivity, selective or non-selective in their drug action, action. For example, cocaine, which non-selectively inhibits the reuptake of serotonin, norepinephrine, and dopamine, is an SRI but not an SSRI. SRIs are used pred ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine
Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic chemical of the catecholamine and phenethylamine families. It is an amine synthesized by removing a carboxyl group from a molecule of its precursor chemical, L-DOPA, which is synthesized in the brain and kidneys. Dopamine is also synthesized in plants and most animals. In the brain, dopamine functions as a neurotransmitter—a chemical released by neurons (nerve cells) to send signals to other nerve cells. The brain includes several distinct dopamine pathways, one of which plays a major role in the motivational component of reward-motivated behavior. The anticipation of most types of rewards increases the level of dopamine in the brain, and many addictive drugs increase dopamine release or block its reuptake into neurons following release. Other brain dopamine pathways are involved in motor control and in controllin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic compound, organic chemical in the catecholamine family that functions in the brain and human body, body as a hormone, neurotransmitter and neuromodulator. The name "noradrenaline" (from Latin '':wikt:ad-, ad'', "near", and '':wikt:ren, ren'', "kidney") is more commonly used in the United Kingdom and the rest of the world, whereas "norepinephrine" (from Ancient Greek :wikt:ἐπί, ἐπῐ́ (''epí''), "upon", and :wikt:νεφρός, νεφρός (''nephrós''), "kidney") is usually preferred in the United States. "Norepinephrine" is also the international nonproprietary name given to norepinephrine (drug), the drug. Regardless of which name is used for the substance itself, parts of the body that produce or are affected by it are referred to as noradrenergic. The general function of norepinephrine is to mobilize the brain and body for action. Norepinephrine release is lowest during sleep, rise ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2C-B
2C-B, also known as 4-bromo-2,5-dimethoxyphenethylamine or by the slang name Nexus, is a synthetic psychedelic drug of the 2C family, mainly used as a recreational drug. It was first synthesized by Alexander Shulgin in 1974 for use in psychotherapy. To date, there is limited scientific information regarding the drug's pharmacokinetics and pharmacological effects in humans. The existing studies primarily classify 2C-B as a stimulant and hallucinogen, and less commonly an entactogen. 2C-B is also known by a number of slang names and appears on the illicit market in multiple forms: as a powder, in capsules or pills. For recreational use, the substance is generally consumed orally or nasally. Use Recreational 2C-B became briefly popular in the United States as substitute for the street drug ecstasy (MDMA) when the latter became illegal in 1985. Many 2C-B users are young adults who attend raves. Although 2C-B is still used in the rave subculture (commonly mistaken for and/o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug Discrimination
Drug discrimination (DD) is a technique in behavioral neuroscience used to evaluate the discriminative stimulus properties or interoceptive cues of psychoactive drugs. In drug discrimination, a subject is trained on a training drug, and then it is tested with novel drugs to see if the novel drugs are experienced as similar to the training drug. In essence, the drug discrimination paradigm has the subject "tell" the experimenter "I think you gave me the training drug" or "I don't think you gave me anything". The discriminative stimulus properties of drugs are believed to reflect their subjective effects. When partial or full stimulus generalization of a test drug to a training drug occurs, the test drug can be assumed to have effects that are subjectively similar to those of the training drug. Drug discrimination tests are usually performed in animals, but have also been conducted in humans. Drug discrimination assays have been employed to assess whether drugs have stimulant- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Potency (pharmacology)
In pharmacology, potency or biological potency is a measure of a drug's biological activity expressed in terms of the dose required to produce a pharmacological effect of given intensity. A highly potent drug (e.g., fentanyl, clonazepam, risperidone, benperidol, bumetanide) evokes a given response at low concentrations, while a drug of lower potency (e.g. morphine, alprazolam, ziprasidone, haloperidol, furosemide) evokes the same response only at higher concentrations. Higher potency does not necessarily mean greater effectiveness nor more side effects nor less side effects. Types of potency The International Union of Basic and Clinical Pharmacology (IUPHAR) has stated that "potency is an imprecise term that should always be further defined", and lists of types of potency as follows: Miscellaneous Lysergic acid diethylamide (LSD) is one of the most potent psychoactive drug A psychoactive drug, psychopharmaceutical, mind-altering drug, consciousness-altering drug, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
