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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 ...
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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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Structural Analog
A structural analog, also known as a chemical analog or simply an analog, is a chemical compound, compound having a chemical structure, structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronicity, isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analog (chemistry), functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is virtual screening, screened for structural analogs of a ...
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Experimental Antidepressants
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons (e ...
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ZC-B
ZC-B (3-(4-bromo-2,5-dimethoxyphenyl)azetidine) is a phenethylamine derivative which acts as a serotonin receptor agonist selective for the 5-HT2 subtypes, with an EC50 of 1.6nM at 5-HT2A, vs 5.8nM at 5-HT2C. It is structurally related to the psychedelic phenethylamines 2C-B and DOB, but with the amine side chain conformationally restricted as an azetidine ring. See also * DOB * β-Methyl-2C-B * 4C-B * TCB-2 TCB-2 is a hallucinogen discovered in 2006 by Thomas McLean working in the lab of David Nichols at Purdue University. It is a conformationally-restricted derivative of the phenethylamine 2C-B, also a hallucinogen, and acts as a potent agonis ... * LPH-5 * LSZ References {{Phenethylamines 2,5-Dimethoxyphenethylamines Designer drugs Serotonin receptor agonists Azetidines Bromoarenes ...
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Z3517967757
Z3517967757, or simply Z7757, is a piperidine chemical derivative, derivative which acts as an agonist at the 5-HT2 receptor, 5-HT2 family of serotonin Receptor (biochemistry), receptors, first reported in 2024. It can also be viewed as a ring (chemistry), ring-restrained substituted phenethylamine, phenethylamine. It has strongest pharmacological activity, activity at the 5-HT2A receptor, 5-HT2A receptor and lower affinity (pharmacology), affinity at the 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C receptors. However, it has been reported to have excellent binding selectivity, selectivity for the 5-HT2A receptor, with no agonistic activity at the 5-HT2B and 5-HT2C receptors. The drug was developed using ''in silico'' modelling to docking (molecular), dock a large chemical library, library of compounds against a 5-HT2A receptor model generated by the artificial intelligence program AlphaFold, and then chemical synthesis, synthesised and tested in the laboratory to confirm a ...
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TCB-2
TCB-2 is a hallucinogen discovered in 2006 by Thomas McLean working in the lab of David Nichols at Purdue University. It is a conformationally-restricted derivative of the phenethylamine 2C-B, also a hallucinogen, and acts as a potent agonist for the 5-HT2A and 5-HT2C receptors with a Ki of 0.26nM at the human 5-HT2A receptor. In drug-substitution experiments in rats, TCB-2 was found to be of similar potency to both LSD and Bromo-DragonFLY, ranking it among the most potent phenethylamine hallucinogens yet discovered. This high potency and selectivity has made TCB-2 useful for distinguishing 5-HT2A receptor-mediated responses from those produced by other similar receptors. TCB-2 has similar but not identical effects in animals to related phenethylamine hallucinogens such as DOI, and has been used for studying how the function of the 5-HT2A receptor differs from that of other serotonin receptors in a number of animal models, such as studies of cocaine addiction and ne ...
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OSU-6162
OSU-6162 (PNU-96391) is a compound which acts as a partial agonist at both dopamine D2 receptors and 5-HT2A receptors. It acts as a dopamine stabilizer in a similar manner to the closely related drug pridopidine, and has antipsychotic, anti- addictive and anti-Parkinsonian effects in animal studies. Both enantiomers show similar activity but with different ratios of effects, with the (S) enantiomer (–)-OSU-6162 that is more commonly used in research, having higher binding affinity to D2 but is a weaker partial agonist at 5-HT2A, while the (R) enantiomer (+)-OSU-6162 has higher efficacy at 5-HT2A but lower D2 affinity. See also * Flumexadol * LPH-5 * PF-219,061 PF-219,061 is a drug that was under development by Pfizer which acts as a potent and highly selective agonist for the dopamine D3 receptor. It was under development as a potential medication for the treatment of female sexual dysfunction. It d ... References {{Serotonergics Benzosulfones Dopamine agon ...
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DMBMPP
DMBMPP, also known as juncosamine or as 2-(2,5-dimethoxy-4-bromobenzyl)-6-(2-methoxyphenyl)piperidine, is a highly selective serotonin 5-HT2A receptor agonist and 2-benzylpiperidine analogue of the serotonergic psychedelic 25B-NBOMe which is used in scientific research. Use Research Despite its uniquely high selectivity for the serotonin 5-HT2A receptor, it has been said that DMBMPP is not widely used as a pharmacological tool in scientific research, presumably due to its chemical synthesis being relatively inaccessible. Consequently, 25CN-NBOH, another highly selective serotonin 5-HT2A receptor agonist, has been proposed as an alternative to DMBMPP for use in scientific research. DMBMPP and 25CN-NBOH are the two most selective serotonin 5-HT2A receptor agonists known as of 2020. Pharmacology The (''S'',''S'')-isomer ((2''S'',6''S'')-DMBMPP) is the most selective agonist for the human serotonin 5-HT2A receptor yet discovered, with a affinity ( Ki) of 2.5nM at the human se ...
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DEMPDHPCA-2C-D
DEMPDHPCA-2C-D is a possible serotonergic psychedelic of the phenethylamine and 2C families. It is a cyclized phenethylamine and a partial or simplified lysergamide. More specifically, the compound is a derivative of 2C-D in which the β position has been cyclized with the amine to form a pyridine ring, an LSD-like ''N'',''N''-diethylcarboxamide moiety has been added to the pyridine ring, and an ''N''-methyl group has been added to the amine. Alternatively, it may be viewed as an analogue of LSD in which the atoms at positions 1 through 4 of the ergoline ring system have been removed and 4-methyl and 2,5- dimethoxy substitutions have been added to the phenyl ring (i.e., the A ring of LSD). DEMPDHPCA-2C-D was synthesized and described by David E. Nichols in his thesis in 1973. Its pharmacology was not reported. However, several close analogues of DEMPDHPCA-2C-D, such as DEMPDHPCA and a few of its derivatives, have been reported to be potent serotonin 5-HT2A receptor agonis ...
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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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