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Simplified LSD Analogue
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. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmacology
Pharmacology is the science of drugs and medications, including a substance's origin, composition, pharmacokinetics, pharmacodynamics, therapeutic use, and toxicology. More specifically, it is the study of the interactions that occur between a living organism and chemicals that affect normal or abnormal biochemical function. If substances have medicinal properties, they are considered pharmaceuticals. The field encompasses drug composition and properties, functions, sources, synthesis and drug design, molecular and cellular mechanisms, organ/systems mechanisms, signal transduction/cellular communication, molecular diagnostics, interactions, chemical biology, therapy, and medical applications and antipathogenic capabilities. The two main areas of pharmacology are pharmacodynamics and pharmacokinetics. Pharmacodynamics studies the effects of a drug on biological systems, and pharmacokinetics studies the effects of biological systems on a drug. In broad terms, pharmacod ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY-178210
LY-178210 is a selective and highly potent serotonin 5-HT1A receptor partial agonist. It has an affinity (Ki) of 0.67nM for the serotonin 5-HT1A receptor. The drug has high selectivity for this receptor over 12other assessed targets, including the serotonin 5-HT1D, 5-HT2A, 5-HT2C, and 5-HT3 receptors among others (Ki = ≥380–4,000nM). LY-178210 is a tricyclic simplified or partial ergoline and is structurally related to LSD. It was described as a potential clinical development candidate but was not further developed and was never marketed. The drug was first reported in the scientific literature by 1990. See also * Partial lysergamide * RU-27849 * RU-28306 * Bay R 1531 (LY-197206) * LY-293284 * NDTDI * 8-OH-DPAT 8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor, 5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonis ... ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
8-OH-DPAT
8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor, 5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonists to have been discovered. Originally believed to be binding selectivity, selective for the 5-HT1A receptor, 8-OH-DPAT was later found to act as a 5-HT7 receptor, 5-HT7 receptor agonist and serotonin reuptake inhibitor/serotonin releasing agent, releasing agent as well. In animal studies, 8-OH-DPAT has been shown to possess antidepressant, anxiolytic, serenic, anorectic, antiemetic, hypothermia, hypothermic, hypotension, hypotensive, bradycardia, bradycardic, hyperventilation, hyperventilative, and analgesic effects. See also * 5-OH-DPAT * 7-OH-DPAT * Bay R 1531 * MDAT * RDS-127 * UH-301 References External links * Yves Aubert, Thesis, Leiden University. (Dec 11, 2012Sex, aggression and pair-bond: a study on the serotonergic r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Psychoplastogen
Psychoplastogens, also known as neuroplastogens, are a group of Small molecule#Drugs, small molecule drugs that produce rapid and sustained effects on neuronal structure and function, intended to manifest therapeutic benefit after a single administration. Several existing psychoplastogens have been identified and their therapeutic effects demonstrated; several are presently at various stages of development as medications including ketamine, MDMA, scopolamine, and the serotonergic psychedelics, including Lysergic acid diethylamide, LSD, psilocin (the active metabolite of psilocybin), N,N-Dimethyltryptamine, DMT, and 5-MeO-DMT. Compounds of this sort are being explored as therapeutics for a variety of brain disorders including Depression (mood), depression, addiction, and Post-traumatic stress disorder, PTSD. The ability to rapidly promote neuronal changes via mechanisms of neuroplasticity was recently discovered as the common therapeutic activity and mechanism of action. Etymol ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Psychedelic Drug
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. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an Receptor antagonist, antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Ancient Greek, Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive." Types of agonists Receptor (biochemistry), Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as medication, drugs), resulting in a biological response. A physiological agonism an ...[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...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] |
LPH-5 (drug)
LPH-5 is a psychedelic discovered by Emil Marcher-Rørsted, Jesper L. Kristensen and Anders A. Jensen at Danish biopharmaceutical company Lophora. It is a conformationally-restricted derivative of the phenethylamine 2C-TFM, also a hallucinogen, and acts as a potent agonist of the 5-HT2A receptor (EC50 = 3.2 nM, Emax = 78%). It shows 10- to 100-fold selectivity for the 5-HT2A receptor over the 5-HT2B and 5-HT2C receptors and, along with related compounds like 25CN-NBOH, is said to be one of the few truly selective 5-HT2A receptor agonists. LPH-5 is expected to avoid the cardiac risks of 5-HT2B receptor activation. LPH-48, an analogue of LPH-5 that likewise acts as a selective serotonin 5-HT2A receptor agonist and psychedelic hallucinogen and shows similar characteristics but has a shorter duration of action, is also under development by Lophora. See also * 2C-B-PP * 2C-TFM * CYB-210010 * DEMPDHPCA * DEMPDHPCA-2C-D * DMBMPP * LPH-48 * OSU-6162 * TCB-2 TCB-2 is a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DEIMDHPCA
DEIMDHPCA, also known as 3,5-seco-LSD, is an indole chemical derivative, derivative and a "partial" or simplified ergoline which is closely related to the highly potency (pharmacology), potent serotonergic psychedelic lysergic acid diethylamide (LSD). It is specifically the structural analogue, analogue of LSD in which one of LSD's carbon atoms in the ergoline ring system (chemistry), ring system, the carbon at position 4, has been removed. This in turn renders the DEIMDHPCA molecule more flexible and makes it a partially rigid structure, rigid indole, indolic substituted phenethylamine, phenethylamine-containing chemical compound, compound rather than an ergoline. DEIMDHPCA is known to be a highly potent serotonin 5-HT2 receptor, 5-HT2 receptor agonist similarly to LSD and to produce psychoplastogenic effects. Pharmacology Like LSD, the drug is known to be a highly potent serotonin 5-HT2A receptor, 5-HT2A and 5-HT2C receptor, 5-HT2C receptor agonist ''in vitro''. Its affinity ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
