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XOB
XOB, also known as ASR-6001 or as ''N''- 4-phenylbutoxy)hexyl4-bromo-2,5-dimethoxyphenethylamine, is a serotonin 5-HT2A receptor antagonist and voltage-gated sodium channel (VGSC) blocker of the phenethylamine and 2C families. It is a derivative of 2C-B in which the amine-containing side chain has been extended with the same long group found in salmeterol. The drug is of relatively low potency as a serotonin 5-HT2A receptor antagonist. It shows modest selectivity for the serotonin 5-HT2A receptor over the serotonin 5-HT2B and 5-HT2C receptors. XOB was accidentally found to have local anesthetic properties upon contact with human skin, which led to the elucidation of its sodium channel-blocking activity. XOB was developed in part by researchers at the Alexander Shulgin Research Institute (ASRI). See also * Substituted methoxyphenethylamine * 2C (psychedelics) * Evenamide Evenamide () (developmental code names NW-3509, NW-3509A) is a selective voltage-gated sodium channel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alexander Shulgin Research Institute
Alexander Shulgin Research Institute (ASRI) is an organization developing novel psychedelic and entactogen drugs as potential pharmaceuticals, among other activities. Its goal is to advance the scientific work and legacy of psychedelic chemist Alexander "Sasha" Shulgin and to complete his unfinished projects. The ASRI was informally established by Alexander Shulgin in the 1980s. However, discussions to formally establish the institute began shortly after Shulgin's passing in 2014. The organization was formally incorporated on April 19th, 2021, Bicycle Day, by Ann Shulgin, the late widow of Alexander Shulgin, and by psychedelic chemists and longtime Shulgin research colleagues Paul Daley and Nicholas Cozzi. Cozzi was the organization's first president between 2020 and 2025. He was succeeded by Daley in March 2025. As of April 2025, ASRI has filed and/or been granted several patents covering various entactogenic and psychedelic compounds. Shulgin himself was not averse to intellect ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2C Series
2C (2C-''x'') is a general name for the family of psychedelic phenethylamines containing methoxy groups on the 2 and 5 positions of a benzene ring. Most of these compounds also carry lipophilic substituents at the 4 position, usually resulting in more potent and more metabolically stable and longer acting compounds. Most of the currently known 2C compounds were first synthesized by Alexander Shulgin in the 1970s and 1980s and published in his book ''PiHKAL'' (''Phenethylamines i Have Known And Loved''). Shulgin also coined the term 2C, being an acronym for the 2 carbon atoms between the benzene ring and the amino group. 2C-B is the most popular of the 2C drugs. Use The 2C drugs are orally active, are used at oral doses of 6 to 150mg depending on the drug, and have durations of 3 to 48hours depending on the drug. However, many have doses in the range of 10 to 60mg and durations in the range of 4 to 12hours. The 2C drugs produce psychedelic effects. Some, such as 2C-B, have al ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2C (psychedelics)
2C (2C-''x'') is a general name for the family of psychedelic drug, psychedelic substituted phenethylamine, phenethylamines containing Methoxy, methoxy groups on the 2 and 5 carbon, positions of a benzene ring. Most of these compounds also carry lipophilic substituents at the 4 position, usually resulting in more potent and more metabolism, metabolically stable and longer acting compounds. Most of the currently known 2C compounds were first synthesized by Alexander Shulgin in the 1970s and 1980s and published in his book ''PiHKAL'' (''Phenethylamines i Have Known And Loved''). Shulgin also coined the term 2C, being an acronym for the 2 carbon atoms between the benzene ring and the amino group. 2C-B is the most popular of the 2C drugs. Use The 2C drugs are oral administration, orally active, are used at oral doses of 6 to 150mg depending on the drug, and have duration of action, durations of 3 to 48hours depending on the drug. However, many have doses in the range of 10 to 60mg an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, memory, and physiological processes such as vomiting and vasoconstriction. In the CNS, serotonin regulates mood, appetite, and sleep. Most of the body's serotonin—about 90%—is synthesized in the gastrointestinal tract by enterochromaffin cells, where it regulates intestinal movements. It is also produced in smaller amounts in the brainstem's raphe nuclei, the skin's Merkel cells, pulmonary neuroendocrine cells, and taste receptor cells of the tongue. Once secreted, serotonin is taken up by platelets in the blood, which release it during clotting to promote vasoconstriction and platelet aggregation. Around 8% of the body's serotonin is stored in platelets, and 1–2% is found in the CNS. Serotonin acts as both a vasoconstrictor and vas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
In chemistry, binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand may bind more preferentially to one receptor than another. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate. Binding selectivity is of major importance in biochemistry and in chemical separation processes. Selectivity coefficient The concept of selectivity is used to quantify the extent to which one chemical substance, A, binds each of two other chemical substances, B and C. The simplest case is where the complexes formed have 1:1 stoichiometry. Then, the two interactions may be characterized by equilibrium constants and .The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. \begin \ce;& \quad ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Local Anesthetics
A local anesthetic (LA) is a medication that causes absence of all sense, sensation (including pain) in a specific body part without loss of consciousness, providing local anesthesia, as opposed to a general anesthetic, which eliminates all sensation in the entire body and causes unconsciousness. Local anesthetics are most commonly used to eliminate pain during or after surgery. When it is used on specific nerve pathways (local anesthetic nerve block), paralysis (loss of muscle function) also can be induced. Classification LAs are of 2 types: *Clinical LAs: **amino amide LAs **amino ester LAs *Synthetic LAs **Cocaine derivatives Synthetic cocaine-derived LAs differ from cocaine because they have a much lower abuse potential and do not cause hypertension vasoconstriction (with few exceptions). The suffix "-caine" at the ends of these medication names is derived from the word "cocaine", because cocaine was formerly used as a local anesthetic. Examples Short Duration of Actio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bromobenzene Derivatives
Bromobenzene is an aryl bromide and the simplest of the bromobenzenes, consisting of a benzene ring substituted with one bromine atom. Its chemical formula is . It is a colourless liquid although older samples can appear yellow. It is a reagent in organic synthesis. Synthesis and reactions Bromobenzene is prepared by the action of bromine on benzene in the presence of Lewis acid catalysts such as aluminium chloride or ferric bromide. Bromobenzene is used to introduce a phenyl group into other compounds. One method involves its conversion to the Grignard reagent, phenylmagnesium bromide. This reagent can be used, e.g. in the reaction with carbon dioxide to prepare benzoic acid. Other methods involve palladium-catalyzed coupling reactions, such as the Suzuki reaction. Bromobenzene is used as a precursor in the manufacture of phencyclidine Phencyclidine or phenylcyclohexyl piperidine (PCP), also known in its use as a street drug as angel dust among other names, is a dis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Antagonists
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and functions as a G protein-coupled receptor (GPCR). It is a cell surface receptor that activates multiple intracellular signalling cascades. Like all 5-HT2 receptors, the 5-HT2A receptor is coupled to the Gq/G11 signaling pathway. It is the primary excitatory receptor subtype among the serotonin-responsive GPCRs. The 5-HT2A receptor was initially noted for its central role as the primary target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. It later regained research prominence when found to mediate, at least in part, the effects of many antipsychotic drugs, particularly atypical antipsychotics. Downregulation of post-synaptic 5-HT2A receptors is an adaptive response triggered by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Elevated 5-HT2A receptor density has been observed in suicidal and ot ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Evenamide
Evenamide () (developmental code names NW-3509, NW-3509A) is a selective voltage-gated sodium channel blocker, including (and not limited to) subtypes Nav1.3, Nav1.7, and Nav1.8, which is described as an antipsychotic and is under development by Newron Pharmaceuticals as an add-on therapy for the treatment of schizophrenia. The drug has shown efficacy in animal models of psychosis, mania, depression, and aggression. It has completed phase I clinical trials, and phase II clinical trials will be commenced in the third quarter of 2015. The drug was discovered by Newron Pharmaceuticals SpA, a pharmaceutical company located in Italy and according to the company, it shows benefit to the management of schizophrenia to poorly responded treatment with antipsychotics. It acts exclusively through glutamatergic inhibition. Clinical studies In a randomized study with treatment-resistant schizophrenia patients, evenamide was added to the treatment regimen, with the psychological a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Substituted Methoxyphenethylamine
Methoxyphenethylamines (MPEAs), as well as methoxyamphetamines (MAs) in the case of the amphetamine (α-methylphenethylamine) homologues, are substituted phenethylamines with one or more methoxy groups. In some cases, one or more of the methoxy groups may also be extended to form other alkoxy and related groups such as ethoxy or propoxy. Methoxyphenethylamines may have additional substitutions as well. Many methoxyphenethylamines that have multiple methoxy groups in the 2- through 5-positions of the phenyl ring, for instance mescaline, 2C-B, TMA, DOM, and 25I-NBOMe, are serotonin 5-HT2A receptor agonists and serotonergic psychedelics. Other methoxyphenethylamines, particularly monomethoxyamphetamines like ''para''-methoxyamphetamine (PMA), are monoamine releasing agents of serotonin, norepinephrine, and/or dopamine, with stimulant and/or entactogen-related effects. Compounds closely related to methoxyphenethylamines include methylenedioxyphenethylamines (MDxx) like M ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Local Anesthetic
A local anesthetic (LA) is a medication that causes absence of all sensation (including pain) in a specific body part without loss of consciousness, providing local anesthesia, as opposed to a general anesthetic, which eliminates all sensation in the entire body and causes unconsciousness. Local anesthetics are most commonly used to eliminate pain during or after surgery. When it is used on specific nerve pathways ( local anesthetic nerve block), paralysis (loss of muscle function) also can be induced. Classification LAs are of 2 types: *Clinical LAs: ** amino amide LAs ** amino ester LAs *Synthetic LAs **Cocaine derivatives Synthetic cocaine-derived LAs differ from cocaine because they have a much lower abuse potential and do not cause hypertension vasoconstriction (with few exceptions). The suffix "-caine" at the ends of these medication names is derived from the word "cocaine", because cocaine was formerly used as a local anesthetic. Examples Short Duration of Act ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2C Receptor
The 5-HT2C receptor is a subtype of the 5-HT2 receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). Like all 5-HT2 receptors, it is a G protein-coupled receptor (GPCR) that is coupled to Gq/G11 and mediates excitatory neurotransmission. ''HTR2C'' denotes the human gene encoding for the receptor, that in humans is located on the X chromosome. As males have one copy of the gene and females have one of the two copies of the gene repressed, polymorphisms at this receptor can affect the two sexes to differing extent. Structure At the cell surface the receptor exists as a homodimer. The crystal structure has been known since 2018. Distribution 5-HT2C receptors are located mainly in the choroid plexus, and in rats is also found in many other brain regions in high concentrations, including parts of the hippocampus, anterior olfactory nucleus, substantia nigra, several brainstem nuclei, amygdala, subthalamic nucleus and lateral habenula. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
