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LSM-775
LSM-775, also known as ''N''-morpholinyllysergamide or as lysergic acid morpholide, is a chemical derivative, derivative of ergine (lysergamide). It is less potent than lysergic acid diethylamide (LSD) but is reported to have some LSD-like effects at doses ranging from 75 to 700 micrograms and a shorter duration of action, duration. LSM-775 may only produce weak or threshold serotonergic psychedelic, psychedelic effects in humans. The drug is a potency (pharmacology), potent full agonist of the serotonin 5-HT1A receptor, 5-HT1A receptor and a potent partial agonist of the serotonin 5-HT2A receptor, 5-HT2A, 5-HT2B receptor, 5-HT2B, and 5-HT2C receptor, 5-HT2C receptors. It does not produce the head-twitch response, a behavioral proxy of psychedelic effects, in rodents. However, LSM-775 can robustly increase head twitches if it is coadministered with the serotonin 5-HT1A receptor receptor antagonist, antagonist WAY-100635. These findings indicate that serotonin 5-HT1A receptor acti ...
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Substituted Lysergamide
Lysergamides, also known as ergoamides or as lysergic acid amides, are amides of lysergic acid (LA). They are ergolines, with some lysergamides being found naturally in ergot as well as other fungi. Lysergamides are notable in containing embedded phenethylamine and tryptamine moieties within their ergoline ring system. The simplest lysergamides are ergine (lysergic acid amide; LSA) and isoergine (iso-lysergic acid amide; iso-LSA). In terms of pharmacology, the lysergamides include numerous serotonin and dopamine receptor agonists, most notably the psychedelic drug lysergic acid diethylamide (LSD) but also a number of pharmaceutical drugs like ergometrine, methylergometrine, methysergide, and cabergoline. Various analogues of LSD, such as the psychedelics ALD-52 (1A-LSD), ETH-LAD, LSZ, and 1P-LSD and the non-hallucinogenic 2-bromo-LSD (BOL-148), have also been developed. Ergopeptines like ergotamine, dihydroergotamine, and bromocriptine are also lysergamides, but with a ...
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Lysergic Acid Piperidide
Lysergic acid piperidide (LA-Pip or LSD-Pip), also known as ''N''-piperidinyllysergamide, is a serotonin receptor modulator of the lysergamide family related to lysergic acid diethylamide (LSD). It is the analogue of LSD in which the ''N'',''N''-di ethyl substitution has been replaced with an ''N''- piperidide ring. The drug has fairly similar affinity and efficacy as a serotonin 5-HT2A receptor agonist compared to LSD, though is variably less potent in terms of depending on the assay. It also has high affinity for the serotonin 5-HT1A and 5-HT2C receptors. LA-Pip has about 8.5% of the antiserotonergic activity of LSD (relative to 2.0% for LSM-775 and 4.7% for LPD-824) in the isolated rat uterus ''in vitro''. LA-Pip has been said to be non-hallucinogenic or much less psychedelic than LSD in humans. However, this does not appear to have actually been stated anywhere in the originally cited source. Other sources imply that LA-Pip has not been assessed in humans. Corresp ...
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5-HT2B Receptor
5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the ''HTR2B'' gene. 5-HT2B is a member of the 5-HT2 receptor, 5-HT2 receptor family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). Like all 5-HT2 receptors, the 5-HT2B receptor is Gq protein, Gq/G11-protein coupled, leading to downstream activation of phospholipase C. Tissue distribution and function First discovered in the stomach of rats, 5-HT2B was challenging to characterize initially because of its structural similarity to the other 5-HT2 receptors, particularly 5-HT2C. The 5-HT2 receptors (of which the 5-HT2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system (CNS) effects include neuronal sensitization to tactile stimuli and mediation of some of the effects of halluci ...
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Head-twitch Response
The head-twitch response (HTR), also sometimes known as wet dog shakes (WDS) in rats, is a rapid side-to-side head movement that occurs in mice and rats in association with serotonin 5-HT2A receptor activation. Serotonergic psychedelics like lysergic acid diethylamide (LSD) and psilocybin consistently induce the HTR in rodents. Because of this, the HTR is widely employed in scientific research as an animal behavioral model of hallucinogen effects and in the discovery of new psychedelic drugs. The HTR is one of the only behavioral paradigms for assessment of psychedelic-like effects in animals, with the other most notable test being drug discrimination. However, the HTR is far less costly and time-consuming than drug discrimination and hence has become much more popular in recent years. Limitations of the HTR include the fact that various other drugs besides serotonin 5-HT2A receptor agonists, such as NMDA receptor antagonists and muscarinic acetylcholine receptor antagonists, ...
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Lysergic Acid 2,4-dimethylazetidide
Lysergic acid 2,4-dimethylazetidide, also known as LSZ, LA-SS-Az, or LA-Azetidide, is an analog of LSD developed by the team led by David E. Nichols at Purdue University. It was developed as a rigid analog of LSD with the diethylamide group constrained into an azetidine ring in order to map the binding site at the 5-HT2A receptor. There are three possible stereoisomers around the azetidine ring, with the (''S'',''S'')-(+) isomer being the most active, slightly more potent than LSD itself in drug discrimination tests using trained rats. There have been several unconfirmed reports of lysergic acid 2,4-dimethylazetidide being synthesized in illicit laboratories and distributed on blotter paper or in liquid solution under names such as "diazedine" and " λ". Dosage and effects The dosage of LSZ in humans is said to be 100 to 300μg orally, which is higher than the listed dosage of LSD (60–200μg). According to David E. Nichols, LSZ is about equipotent with LSD in humans. ...
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Lysergic Acid Pyrrolidide
''N''-Pyrrolidyllysergamide (LPD-824), also known as lysergic acid pyrrolidide (LA-Pyr), is a psychedelic drug of the lysergamide family related to lysergic acid diethylamide (LSD). It is the analogue of LSD in which the ''N'',''N''-diethylamide moiety has been cyclized into an ''N'',''N''- pyrrolidide ring. Use and effects The drug has been reported to have mild and relatively short-lasting LSD-like effects in humans at an oral dose of 800μg equivalent to one-tenth this amount of LSD (i.e., 80μg). Based on different clinical studies, it is estimated to be 5 to 10% as potent as LSD in humans. Its duration was shorter than that of LSD, lasting around 5hours as opposed to 7hours in the case of LSD. The drug produced nausea at small doses in humans, which was dose-limiting in terms of evaluating its effects. Pharmacology LPD-824 is known to be a serotonin receptor modulator, including of the serotonin 5-HT2A receptor, where it acted as a partial agonist with about 17-fold ...
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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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5-HT1A Agonists
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarization and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene. Distribution The 5-HT1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus. The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors. Function Neuromodulation 5-HT1A ...
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WAY-100635
WAY-100635 is a piperazine drug and research chemical widely used in scientific studies. It was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor. It is sometimes referred to as a silent antagonist at the former receptor. It is closely related to WAY-100135. In light of its dopaminergic activity, conclusions drawn from studies that employ WAY-100635 as a selective 5-HT1A antagonist may need to be re-evaluated. Human PET studies In human PET studies WAY-100635 shows high binding in the cerebral cortex, hippocampus, raphe nucleus and amygdaloid nucleus, while lower in thalamus and basal ganglia. One study described a single case with relatively high binding in the cerebellum. In relating its binding to subject variables one Swedish study found WAY-100635 binding in raphe brain region correlating with self-transcendence and spiritual acceptance personality traits. ...
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Albert Hofmann
Albert Hofmann (11 January 1906 – 29 April 2008) was a Swiss chemist known for being the first to synthesize, ingest, and learn of the psychedelic effects of lysergic acid diethylamide (LSD). Hofmann's team also isolated, named and synthesized the principal psychedelic mushroom compounds psilocybin and psilocin. He authored more than 100 scientific articles and numerous books, including ''LSD: Mein Sorgenkind'' (''LSD: My Problem Child''). In 2007, he shared first place with Tim Berners-Lee on a list of the 100 greatest living geniuses published by ''The Daily Telegraph'' newspaper. Early life and education Albert Hofmann was born in Baden, Switzerland, on 11 January 1906. He was the first of four children to factory toolmaker Adolf Hofmann and Elisabeth ( Schenk) and was baptized Protestant. When his father became ill, Hofmann obtained a position as a commercial apprentice in concurrence with his studies. Owing to his father's low income, Albert's godfather paid for his e ...
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Scientific Literature
Scientific literature encompasses a vast body of academic papers that spans various disciplines within the natural and social sciences. It primarily consists of academic papers that present original empirical research and theoretical contributions. These papers serve as essential sources of knowledge and are commonly referred to simply as "the literature" within specific research fields. The process of academic publishing involves disseminating research findings to a wider audience. Researchers submit their work to reputable journals or conferences, where it undergoes rigorous evaluation by experts in the field. This evaluation, known as peer review, ensures the quality, validity, and reliability of the research before it becomes part of the scientific literature. Peer-reviewed publications contribute significantly to advancing our understanding of the world and shaping future research endeavors. Original scientific research first published in scientific journals co ...
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