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ITI-333
ITI-333 is a drug which has a mixed mechanism of action, acting as an antagonist at the 5-HT2A, D1 and α1A receptors, and also as a partial agonist at the μ-opioid receptor. In animal studies it blocked the head-twitch response produced by DOI and also reduced responses to morphine, while also reducing the symptoms produced by naloxone-precipitated withdrawal in opioid habituated mice. It has been developed for potential uses in treatment of opioid withdrawal and opioid use disorder. See also * IHCH-7086 * IHCH-7079 * IHCH-7113 IHCH-7113 is a putative psychedelic drug which acts as an agonist at the 5-HT2A serotonin receptor. It was derived by structural simplification of the 5-HT2A receptor antagonist atypical antipsychotic drug lumateperone along with several relate ... * Lumateperone References Experimental drugs Serotonin receptor agonists Nitrogen heterocycles Heterocyclic compounds with 4 rings 4-Fluorophenyl compounds Lactams {{nervous-s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IHCH-7079
IHCH-7079 is a drug which acts as an agonist at the 5-HT2A serotonin receptor. It was derived by structural simplification of the 5-HT2A antagonist atypical antipsychotic drug lumateperone along with several related compounds such as IHCH-7086, which was found to be a non-hallucinogenic biased 5-HT2A agonist that was active in antidepressant assays but did not produce psychedelic-like responding in mice. The related structure IHCH-7113 was found to produce a positive head-twitch response in mice, suggesting likely hallucinogenic activity in humans. See also * AAZ-A-154 * Efavirenz * IHCH-7086 * IHCH-7113 * ITI-333 * Lisuride * Mefloquine Mefloquine, sold under the brand name Lariam among others, is a medication used to prevent or treat malaria. When used for prevention it is typically started before potential exposure and continued for several weeks after potential exposure. It ... * NDTDI * RH-34 * SCHEMBL5334361 * WAY-163909 References 2-Methoxyphenyl co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antagonist (pharmacology)
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves ." '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include s, |
Opioid Use Disorder
Opioid use disorder (OUD) is a substance use disorder characterized by cravings for opioids, continued use despite physical and/or psychological deterioration, increased tolerance with use, and withdrawal symptoms after discontinuing opioids. Opioid withdrawal symptoms include nausea, muscle aches, diarrhea, trouble sleeping, agitation, and a low mood. Addiction and dependence are important components of opioid use disorder. Risk factors include a history of opioid misuse, current opioid misuse, young age, socioeconomic status, race, untreated psychiatric disorders, and environments that promote misuse (social, family, professional, etc.). Complications may include opioid overdose, suicide, HIV/AIDS, hepatitis C, and problems meeting social or professional responsibilities. Diagnosis may be based on criteria by the American Psychiatric Association in the DSM-5. Opioids include substances such as heroin, morphine, fentanyl, codeine, dihydrocodeine, oxycodone, and hydrocodon ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Heterocyclic Compounds With 4 Rings
A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s). Heterocyclic organic chemistry is the branch of organic chemistry dealing with the synthesis, properties, and applications of organic heterocycles. Examples of heterocyclic compounds include all of the nucleic acids, the majority of drugs, most biomass (cellulose and related materials), and many natural and synthetic dyes. More than half of known compounds are heterocycles. 59% of US FDA-approved drugs contain nitrogen heterocycles. Classification The study of organic heterocyclic chemistry focuses especially on organic unsaturated derivatives, and the preponderance of work and applications involves unstrained organic 5- and 6-membered rings. Included are pyridine, thiophene, pyrrole, and furan. Another large class of organic heterocycles refers to those fused to benzene rings. For example, the fused benzene derivatives of pyridin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitrogen Heterocycles
Nitrogen is a chemical element; it has symbol N and atomic number 7. Nitrogen is a nonmetal and the lightest member of group 15 of the periodic table, often called the pnictogens. It is a common element in the universe, estimated at seventh in total abundance in the Milky Way and the Solar System. At standard temperature and pressure, two atoms of the element bond to form N2, a colourless and odourless diatomic gas. N2 forms about 78% of Earth's atmosphere, making it the most abundant chemical species in air. Because of the volatility of nitrogen compounds, nitrogen is relatively rare in the solid parts of the Earth. It was first discovered and isolated by Scottish physician Daniel Rutherford in 1772 and independently by Carl Wilhelm Scheele and Henry Cavendish at about the same time. The name was suggested by French chemist Jean-Antoine-Claude Chaptal in 1790 when it was found that nitrogen was present in nitric acid and nitrates. Antoine Lavoisier suggested instead the nam ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Agonists
A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin (5-hydroxytryptamine; 5-HT), a neurotransmitter and hormone and the endogenous ligand of the serotonin receptors. Non-selective agonists Serotonergic psychedelics such as tryptamines (e.g., psilocybin, psilocin, , 5-MeO-DMT, bufotenin), lysergamides (e.g., , ergine ()), phenethylamines (e.g., mescaline, 2C-B, 25I-NBOMe), and amphetamines (e.g., , ) are non-selective agonists of serotonin receptors. Their hallucinogenic effects are specifically mediated by activation of the 5-HT2A receptor. Drugs that increase extracellular serotonin levels such as serotonin reuptake inhibitors (e.g., fluoxetine, venlafaxine), serotonin releasing agents (e.g., fenfluramine, ), and monoamine oxidase inhibitors (e.g., phenelzine, moclobemide) are indirect non-selective serotonin receptor agonists. They are used variously as an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Drugs
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 ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lumateperone
Lumateperone, sold under the brand name Caplyta, is an atypical antipsychotic medication of the butyrophenone class. It is approved for the treatment of schizophrenia as well as bipolar depression, as either monotherapy or adjunctive therapy (with lithium or valproate). It is developed by Intra-Cellular Therapies, licensed from Bristol-Myers Squibb. Lumateperone was approved for medical use in the United States in December 2019 with an initial indication for schizophrenia, and became available in February 2020. It has since demonstrated efficacy in bipolar depression and received FDA approval in December 2021 for depressive episodes associated with both bipolar I and II disorders. Part of the drug shows structural similarity to Pirlindole. Medical uses Schizophrenia On December 20, 2019, the United States Food and Drug Administration (FDA) approved lumateperone for the treatment of schizophrenia in adults. Bipolar depression In December 2021, the FDA approved lumatep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IHCH-7113
IHCH-7113 is a putative psychedelic drug which acts as an agonist at the 5-HT2A serotonin receptor. It was derived by structural simplification of the 5-HT2A receptor antagonist atypical antipsychotic drug lumateperone along with several related compounds such as IHCH-7079 and IHCH-7086, which were found to be non-hallucinogenic biased 5-HT2A agonists that were active in antidepressant assays but did not produce psychedelic-like responding in mice. IHCH-7113 however produced a head-twitch response comparable to that of DOI or LSD, which was blocked by the 5-HT2A antagonist MDL100907. See also * Efavirenz * IHCH-7079 * IHCH-7086 * Lisuride * Mefloquine * NDTDI * RH-34 * SCHEMBL5334361 * WAY-163909 * Z3517967757 * Zalsupindole Zalsupindole,https://iris.who.int/bitstream/handle/10665/380497/9789240107038-eng.pdf "zalsupindolum zalsupindole (2R)-1-(5-methoxy-1H-indol-1-yl)-N,N-dimethylpropan-2-amine antidepressant" also known by its developmental code names DLX-001 an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IHCH-7086
IHCH-7086 is a drug which acts as an agonist at the 5-HT2A serotonin receptor. It was derived by structural simplification of the 5-HT2A antagonist atypical antipsychotic drug lumateperone along with several related compounds such as IHCH-7079, which was found to be a non-hallucinogenic biased 5-HT2A agonist that was active in antidepressant assays but did not produce psychedelic-like responding in mice. The related structure IHCH-7113 was found to produce a positive head-twitch response in mice, suggesting likely hallucinogenic activity in humans. See also * Efavirenz * IHCH-7079 * IHCH-7113 * Lisuride * Mefloquine Mefloquine, sold under the brand name Lariam among others, is a medication used to prevent or treat malaria. When used for prevention it is typically started before potential exposure and continued for several weeks after potential exposure. It ... * NDTDI * RH-34 * SCHEMBL5334361 * WAY-163909 * Z3517967757 * Zalsupindole References 2-Methoxy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opioid Withdrawal
Opioid withdrawal is a set of symptoms arising from the sudden cessation or reduction of opioids where previous usage has been heavy and prolonged. Signs and symptoms of withdrawal can include drug craving, anxiety, restless legs syndrome, nausea, vomiting, diarrhea, sweating, and an elevated heart rate. Opioid use triggers a rapid adaptation in cellular signaling pathways that, when reduced or stopped, can cause adverse physiological effects. All opioids, both recreational drugs and medications, when reduced or stopped, can lead to opioid withdrawal symptoms. When withdrawal symptoms are due to recreational opioid use, the term opioid use disorder is used, whereas when due to prescribed medications, the term ''prescription opioid use disorder'' is used. Opioid withdrawal can be managed by the use of opioid replacement therapy, while symptoms may be relieved by the use of medications such as lofexidine and clonidine. Signs and symptoms Withdrawal from any opioid produces s ... [...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] |
