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DOI-NBOMe
DOI-NBOMe, or NBOMe-DOI, also known as ''N''-(2-methoxybenzyl)-4-iodo-2,5-dimethoxyamphetamine, is a serotonin 5-HT2A receptor agonist and possible psychedelic drug of the phenetylamine, DOx, and 25-NB (NBOMe) families. It is the ''N''-(2-methoxybenzyl) derivative of DOI and the amphetamine (i.e., α-methyl) analogue of 25I-NBOMe. Pharmacology The drug is a potent serotonin 5-HT2A receptor partial agonist, with an affinity (Ki) of 0.78 to 1.08nM, an of 36.1nM, and an of 43% in the employed assay. As an agonist of the serotonin 5-HT2A receptor, DOI-NBOMe had about half the affinity and potency of DOI and a little more than half the efficacy in comparison ''in vitro'' (with DOI having a Ki of 0.58–0.64nM, an of 19.2nM, and an of 77%). Compared to 25I-NBOMe, the corresponding NBOMe analogue of 2C-I, DOI-NBOMe had about 14.4-fold lower potency as a serotonin 5-HT2A receptor agonist and slightly more than half the activational efficacy. Whereas the potency of 2Cs can be dr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOx (psychedelics)
4-Substituted-2,5-dimethoxyamphetamines (DO''x'') is a chemical class of substituted amphetamine derivatives featuring methoxy groups at the 2- and 5- positions of the phenyl ring, and a substituent such as alkyl or halogen at the 4- position of the phenyl ring. They are 4-substituted derivatives of 2,5-dimethoxyamphetamine (2,5-DMA, DOH) and are structurally related to the naturally occurring phenethylamine psychedelic mescaline. The most well-known DOx drugs are DOM, DOI, DOB, DOET, and DOC. DOI is widely used in scientific research. DOM has been used as a recreational drug, while DOET was an experimental pharmaceutical drug. Most compounds of this class are potent and long-lasting psychedelic drugs, and act as selective 5-HT2A, 5-HT2B, and 5-HT2C receptor agonists. A few bulkier derivatives such as DOAM have similarly high affinity for 5-HT2 receptors but have reduced activational efficacy and do not produce psychedelic effects. DOI has been found to have ext ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOM-NBOMe
DOM-NBOMe, or NBOMe-DOM, also known as ''N''-(2-methoxybenzyl)-4-methyl-2,5-dimethoxyamphetamine, is a serotonin 5-HT2 receptor agonist and putative psychedelic drug of the phenethylamine, DOx, and 25-NB (NBOMe) families. Table 1. 5-HT2A receptor binding affinities of disclosed compounds. Table 3. Functional activity at 5-HT receptor subtypes. ..Table 4. Activity in the HTR assay in mice. .. It is the ''N''-(2-methoxybenzyl) derivative of DOM and the amphetamine (i.e., α-methyl) analogue of 25D-NBOMe. Pharmacology Pharmacodynamics DOM-NBOMe is a potent agonist of the serotonin 5-HT2 receptors, including the serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptors. Its affinity (Ki) for the serotonin 5-HT2A receptor was reported to be 45.8nM. In terms of functional activity, DOM-NBOMe showed an of 4.25nM and of 88.8% at the serotonin 5-HT2A receptor, an of 54.6nM and of 20.1% at the serotonin 5-HT2B receptor, and an of 9.96nM and of 87.6% at the serotonin 5-HT2C receptor. It ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOB-NBOMe
DOB-NBOMe, or NBOMe-DOB, also known as ''N''-(2-methoxybenzyl)-4-bromo-2,5-dimethoxyamphetamine, is a serotonin 5-HT2A receptor agonist and possible psychedelic drug of the phenethylamine, DOx, and 25-NB (NBOMe) families. It is the ''N''-(2-methoxybenzyl) derivative of DOB and the amphetamine (i.e., α-methyl) analogue of 25B-NBOMe. Pharmacology The drug is a potent serotonin 5-HT2A receptor partial agonist, with an of 7.94nM and an of 20% in the employed assay. As an agonist of the serotonin 5-HT2A receptor, DOB-NBOMe had about the same potency as DOB but had greatly reduced efficacy in comparison ''in vitro'' (with DOB having an of 10.2nM and an of 71%). Compared to 25B-NBOMe, the corresponding NBOMe analogue of 2C-B, DOB-NBOMe had about 30-fold lower potency as a serotonin 5-HT2A receptor agonist and about half the activational efficacy. Whereas the potency of 2Cs can be dramatically increased by ''N''-(2-methoxybenzyl) substitution, this has not been the case with the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
25-NB
The 25-NB (25''x''-NB''x'') series, or NBOMe series, also known as the ''N''-benzylphenethylamines, is a family of serotonergic psychedelics. They are substituted phenethylamines and were derived from the 2C family. The most commonly encountered NBOMe drugs are 25I-NBOMe, 25B-NBOMe, and 25C-NBOMe. The NBOMe drugs act as selective agonists of the serotonin 5-HT2 receptors. The 25-NB family is unique relative to other classes of psychedelics in that they are, generally speaking, extremely potent and quite selective for the 5-HT2 receptors. Use of NBOMe series drugs has caused many deaths and hospitalisations since the drugs popularisation in the 2010s. This is primarily due to their high potency, unpredictable pharmacokinetics, and sellers passing off the compounds in the series as LSD. Use The 25-NB drugs are inactive orally and instead are typically used sublingually, buccally, by insufflation, or sometimes via inhalation. They are typically employed at doses in the ra ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
25I-NBOMe
25I-NBOMe, also known as 2C-I-NBOMe, Cimbi-5, and shortened to "25I", is a psychedelic drug of the phenethylamine, 2C, and NBOMe (25-NB) families. Since 2010, it has circulated in the recreational drug scene, often misrepresented as LSD. It is the most well-known member of the 25-NB family and the earliest member to be encountered as a novel recreational drug. The carbon-11 labelled version of 25I-NBOMe, 11C">sup>11Cimbi-5, was synthesized and validated as a radiotracer for positron emission tomography (PET) in Copenhagen. Being the first 5-HT2A receptor full agonist PET radioligand, 11C">sup>11CIMBI-5 shows promise as a more functional marker of these receptors, particularly in their high affinity states. Street and media nicknames for this drug include "N-Bomb", "Solaris", "Smiles", and "Wizard", although the drug is frequently fraudulently sold as LSD.Mackin, Teresa (October 9, 2012)Dangerous synthetic drug making its way across the country. WISH-TV Due to its physica ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2C-I
2C-I, also known as 2,5-dimethoxy-4-iodophenethylamine, is a phenethylamine of the 2C family with psychedelic effects. It was first synthesized by Alexander Shulgin, and is described in Shulgin's book ''PiHKAL'' (1991). The substance is consumed as a recreational drug, and is circulated in the drug market in a powder form. 2C-I is sometimes confused with other related chemical substances such as 25I-NBOMe (2C-I-NBOMe), nicknamed "Smiles" and "N-bomb" in the media.Weiss, Piper (September 20, 2012)2C-I or 'Smiles': The New Killer Drug Every Parent Should Know About.'' Yahoo! News'' WISH-TV Use In the early 2000s, 2C-I was sold in Dutch smart shops as a recreational drug after the drug 2C-B was banned. According to the US Drug Enforcement Administration, 2C-I is taken orally or snorted in a powder form.Reuters (March 20, 2011)Synthetic drug, subject of proposed bans, kill teen./ref> Interactions 2C-I is metabolized by the monoamine oxidase (MAO) enzymes MAO-A and MA ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Affinity (pharmacology)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bioassay
A bioassay is an analytical method to determine the potency or effect of a substance by its effect on animal testing, living animals or plants (''in vivo''), or on living cells or tissues (''in vitro''). A bioassay can be either quantal or quantitative, direct or indirect. If the measured response is binary, the assay is mwod:quantal, quantal; if not, it is Quantitative research, quantitative. A bioassay may be used to detect biological hazards or to give an assessment of the quality of a mixture. A bioassay is often used to monitor water quality as well as wastewater discharges and its impact on the surroundings. It is also used to assess the environmental impact and safety of new technologies and facilities. Bioassays are essential in pharmaceutical, medical and agricultural sciences for development and launching of new drugs, vitamins, etc. Principle A bioassay is a biochemical test to estimate the potency of a sample compound. Usually this potency can only be measured rela ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
In Vitro
''In vitro'' (meaning ''in glass'', or ''in the glass'') Research, studies are performed with Cell (biology), cells or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in biology and its subdisciplines are traditionally done in labware such as test tubes, flasks, Petri dishes, and microtiter plates. Studies conducted using components of an organism that have been isolated from their usual biological surroundings permit a more detailed or more convenient analysis than can be done with whole organisms; however, results obtained from ''in vitro'' experiments may not fully or accurately predict the effects on a whole organism. In contrast to ''in vitro'' experiments, ''in vivo'' studies are those conducted in living organisms, including humans, known as clinical trials, and whole plants. Definition ''In vitro'' (Latin language, Latin for "in glass"; often not italicized in English usage) studies are conducted ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemical Substituent
In organic chemistry, a substituent is one or a group of atoms that replaces (one or more) atoms, thereby becoming a moiety in the resultant (new) molecule. The suffix ''-yl'' is used when naming organic compounds that contain a single bond replacing one hydrogen; ''-ylidene'' and ''-ylidyne'' are used with double bonds and triple bonds, respectively. In addition, when naming hydrocarbons that contain a substituent, positional numbers are used to indicate which carbon atom the substituent attaches to when such information is needed to distinguish between isomers. Substituents can be a combination of the inductive effect and the mesomeric effect. Such effects are also described as electron-rich and electron withdrawing. Additional steric effects result from the volume occupied by a substituent. The phrases ''most-substituted'' and ''least-substituted'' are frequently used to describe or compare molecules that are products of a chemical reaction. In this terminology, methane is ... [...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] |
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] |
