DEMPDHPCA
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DEMPDHPCA
DEMPDHPCA is a serotonin 5-HT2 receptor agonist and a cyclized phenethylamine and simplified or partial ergoline that is structurally related to the serotonergic psychedelic lysergic acid diethylamide (LSD). It is the analogue of LSD in which the carbon and nitrogen atoms at positions 1 through 4 of the ergoline ring system have been removed. Pharmacology DEMPDHPCA produces gross behavioral effects very similar to those of psychedelics like LSD in rodents and has been assumed to act as a hallucinogen likewise. However, the drug has not been tested in humans. DEMPDHPCA is much less potent than LSD in rodents, which was active at a dose of 0.16μmol/kg by intraperitoneal injection, whereas DEMPDHPCA was active at doses of 10 to 35μmol/kg. On the other hand, DEMPDHPCA was more potent than dimethyltryptamine (DMT) and is more potent than mescaline. Like LSD, the drug has been found to act as a potent serotonin 5-HT2A and 5-HT2C receptor agonist ''in vitro''. The affinitie ...
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Simplified/partial LSD Analogue
Partial or simplified ergolines and lysergamides are structural analog, analogues of ergolines and substituted lysergamide, lysergamides like LSD in which one or more atoms or covalent bond, bonds, for instance within the ergoline ring system (chemistry), ring system, have been removed. Additional chemical substituent, substitutions may also be added, for instance on the A ring of the ergoline nucleus. It is notable that the ergoline ring system contains embedded substituted tryptamine, tryptamine and substituted phenethylamine, phenethylamine moiety (chemistry), moieties within its chemical structure, structure, and so some partial ergolines are simple tryptamines, cyclized tryptamines, simple phenethylamines, and/or cyclized phenethylamines. In terms of pharmacology, partial lysergamides include serotonin receptor agonist, serotonin and dopamine receptor agonists. Some, like NDTDI, DEMPDHPCA, DEIMDHPCA, and LPH-5 (drug), LPH-5, are serotonin 5-HT2A receptor, 5-HT2A receptor agon ...
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Simplified Or Partial Ergoline
Partial or simplified ergolines and lysergamides are analogues of ergolines and lysergamides like LSD in which one or more atoms or bonds, for instance within the ergoline ring system, have been removed. Additional substitutions may also be added, for instance on the A ring of the ergoline nucleus. It is notable that the ergoline ring system contains embedded tryptamine and phenethylamine moieties within its structure, and so some partial ergolines are simple tryptamines, cyclized tryptamines, simple phenethylamines, and/or cyclized phenethylamines. In terms of pharmacology, partial lysergamides include serotonin and dopamine receptor agonists. Some, like NDTDI, DEMPDHPCA, DEIMDHPCA, and LPH-5, are serotonin 5-HT2A receptor agonists and have psychedelic-like and/or psychoplastogenic effects. Some, like 8-OH-DPAT and LY-178210, are selective serotonin 5-HT1A receptor agonists. Others, like rotigotine, nolomirole, and RU-28251, are dopamine D2-like receptor agonists. Part ...
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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 ...
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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 hallucinogens or serotonergic hallucinogens, the term ''psychedelic'' is sometimes used more broadly to include various other types of hallucinogens as well, such as those which are atypical or adjacent to psychedelia like salvia and MDMA, respectively. Classic psychedelics generally cause specific psychological, visual, and auditory changes, and oftentimes a substantially altered state of consciousness. They have had the largest influence on science and culture, and include mescaline, LSD, psilocybin, and DMT. There are a large number of both naturally occurring and synthetic serotonergic psychedelics. Most psychedelic drugs fall into one of the three families of chemical compounds: tryptamines, phenethylamines, or lysergamides. They pro ...
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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 ...
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Mescaline
Mescaline, also known as mescalin or mezcalin, and in chemical terms 3,4,5-trimethoxyphenethylamine, is a natural product, naturally occurring psychedelic drug, psychedelic alkaloid, protoalkaloid of the substituted phenethylamine class, found in Cactus, cacti like peyote (''Lophophora williamsii'') and San Pedro cactus, San Pedro (certain species of the Echinopsis genus) and known for its Serotonin, serotonergic Hallucinogen, hallucinogenic effects. Mescaline is typically taken orally and used recreationally, spiritually, and medically, with psychedelic effects occurring at doses from 100 to 1,000 mg, including microdosing below 75 mg, and it can be consumed in pure form or via mescaline-containing cacti. Mescaline induces a psychedelic experience characterized by vivid visual patterns, altered perception of time and self, synesthesia, and spiritual effects, with an onset of 0.5–0.9 hours and a duration that increases with dose, ranging from about 6 to 14 hours. Mescaline h ...
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5-HT2A Receptor
The 5-HT2A receptor is a subtype of the 5-HT2 receptor, 5-HT2 receptor that belongs to the serotonin receptor family and functions as a GPCR, 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 protein, 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 antipsychotic, 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 ...
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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. ...
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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 ...
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Receptor Activation
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and produce physiological responses, such as a change in the electrical activity of a cell. For example, GABA, an inhibitory neurotransmitter, inhibits electrical activity of neurons by binding to GABA receptors. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Cell surface receptors, also known as transmembrane receptors, include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. Intracellular rece ...
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Enantiomer
In chemistry, an enantiomer (Help:IPA/English, /ɪˈnænti.əmər, ɛ-, -oʊ-/ Help:Pronunciation respelling key, ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities which are mirror images of each other and non-superposable. Enantiomer molecules are like right and left hands: one cannot be superposed onto the other without first being converted to its mirror image. It is solely a relationship of chirality (chemistry), chirality and the permanent three-dimensional relationships among molecules or other chemical structures: no amount of re-orientation of a molecule as a whole or conformational isomerism, conformational change converts one chemical into its enantiomer. Chemical structures with chirality rotate plane-polarized light. A mixture of equal amounts of each enantiomer, a ''racemic mixture'' or a ''racemate'', does not rotate light. Stereoisomers include both enantiomers and diastereomers. Diaste ...
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