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(R)-69
(''R'')-69 (3IQ) is a tetrahydropyridine derivative which acts as a 5-HT2A receptor agonist, with 4.6x selectivity over 5-HT2B and 49x selectivity over 5-HT2C. It has a 5-HT2A Ki of 680nM and an EC50 of 41nM. (''R'')-69 is a biased agonist selective for activation of the Gq coupled signalling pathway, with much weaker activation of the β-arrestin 2 coupled pathway. In animal studies it produces antidepressant-like activity but without producing the head-twitch response associated with psychedelic effects. See also * AAZ-A-154 * RU-24969 * SN-22 SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19nM at 5HT2 subtypes vs 514 nM at 5-HT1A receptors. Many related derivatives are known, most of which are ligand ... References Designer drugs Pyrrolopyridines Tetrahydropyridines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Receptor
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and otherwis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AAZ-A-154
AAZ-A-154 is a novel isotryptamine derivative which acts as a 5-HT2A receptor, 5-HT2A receptor agonist discovered and synthesized by the lab of Professor David E. Olson at University of California, Davis, UCDavis. Animal studies suggest that it produces antidepressant effects without the psychedelic action typical of drugs from this class. In tests, AAZ-A-154 had antidepressant effects in mice without causing the head-twitch response linked to hallucinogenic effects. Due to the rapidly-induced and enduring neuroplasticity, AAZ-A-154 is a member of the class of compounds known as non-hallucinogenic psychoplastogens. This compound, as well as related compounds, are licensed by Delix Therapeutics and are being developed as potential medicines for Mental disorder, neuropsychiatric disorders. See also * α,N,N-Trimethyltryptamine * 5-MeO-DMT * 6-Fluoro-DET * AL-34662 * IHCH-7113 * (R)-69 * Neuroplasticity * Psychoplastogen * Delix Therapeutics * David E. Olson References Desi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). 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 hallucinogenic substituted amphetamines. The 5-HT2B receptor is expressed in several areas of the CNS, including the dorsal hypothalamus, frontal cortex, medial ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2C Receptor
The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). 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 at the X chromosome. As males have one copy of the gene and in females one of the two copies of the gene is 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 is 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. 5-HT2C receptors are also found on epithel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biased Agonist
Functional selectivity (or “agonist trafficking”, “biased agonism”, “biased signaling”, "ligand bias" and “differential engagement”) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor. Functional selectivity can be present when a receptor has several possible signal transduction pathways. To which degree each pathway is activated thus depends on which ligand binds to the receptor. Functional selectivity, or biased signaling, is most extensively characterized at G protein coupled receptors (GPCRs). A number of biased agonists, such as those at muscarinic M2 receptors tested as analgesics or antiproliferative drugs, or those at opioid receptors that mediate pain, show potential at various receptor families to increase beneficial properties while reducing side effects. For example, pre-clinical studies with G protein biased agonists at the μ-opioid re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gq Alpha Subunit
Gq protein alpha subunit is a family of heterotrimeric G protein alpha subunits. This family is also commonly called the Gq/11 (Gq/G11) family or Gq/11/14/15 family to include closely related family members. G alpha subunits may be referred to as Gq alpha, Gαq, or Gqα. Gq proteins couple to G protein-coupled receptors to activate beta-type phospholipase C (PLC-β) enzymes. PLC-β in turn hydrolyzes phosphatidylinositol 4,5-bisphosphate (PIP2) to diacyl glycerol (DAG) and inositol trisphosphate (IP3). IP3 acts as a second messenger to release stored calcium into the cytoplasm, while DAG acts as a second messenger that activates protein kinase C (PKC). Family members In humans, there are four distinct proteins in the Gq alpha subunit family: * Gαq is encoded by the gene GNAQ. * Gα11 is encoded by the gene GNA11. * Gα14 is encoded by the gene GNA14. * Gα15 is encoded by the gene GNA15. Function The general function of Gq is to activate intracellular signaling p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Arrestin Beta 2
Beta-arrestin-2, also known as arrestin beta-2, is an intracellular protein that in humans is encoded by the ''ARRB2'' gene. Members of arrestin/beta-arrestin protein family are thought to participate in agonist-mediated desensitization of G protein-coupled receptors and cause specific dampening of cellular responses to stimuli such as hormones, neurotransmitters, or sensory signals, as well as having signalling roles in their own right. Arrestin beta 2, like arrestin beta 1, was shown to inhibit beta-adrenergic receptor function in vitro. It is expressed at high levels in the central nervous system and may play a role in the regulation of synaptic receptors. Besides the brain, a cDNA for arrestin beta 2 was isolated from thyroid gland, and thus it may also be involved in hormone-specific desensitization of TSH receptors. Multiple alternatively spliced transcript variants have been found for this gene, but the full-length nature of some variants has not been defined. The protein ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting. There is a slight increased risk of suicidal thinking and behavior when taken by children, adolescents, and young adults. Discontinuation syndrome may occur after stopping any antidepressant which resembles recurrent depression. Some research regarding the effectiveness of antidepressants for depression in adults has found benefits, whilst other research has not. Evidence of benefit in children and adolescents is unclear. The twenty-one most commonly prescribed antidepressant medications are more effective than placebo for the short-term (acute) treatments of adults with major depressive disorder. There is debate in the medical community about how much of the observed effects of antidep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Head-twitch Response
The head-twitch response (HTR) is a rapid side-to-side head movement that occurs in mice and rats after the serotonin 5-HT2A receptor is activated. The prefrontal cortex may be the neuroanatomical locus mediating the HTR. Many serotonergic hallucinogens, including lysergic acid diethylamide (LSD), induce the head-twitch response, and so the HTR is used as a behavioral model of hallucinogen effects. However while there is generally a good correlation between compounds that induce head twitch in mice and compounds that are hallucinogenic in humans, it is unclear whether the head twitch response is primarily caused by 5-HT2A receptors, 5-HT2C receptors or both, though recent evidence shows that the HTR is mediated by the 5-HT2A receptor and modulated by the 5-HT2C receptor. Also, the effect can be non-specific, with head twitch responses also produced by some drugs that do not act through 5-HT2 receptors, such as phencyclidine, yohimbine, atropine and cannabinoid receptor antagonists. As ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Psychedelic
Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary states of consciousness (known as psychedelic experiences or "trips").Pollan, Michael (2018). ''How to Change Your Mind: What the New Science of Psychedelics Teaches Us About Consciousness, Dying, Addiction, Depression, and Transcendence'' Sometimes, they are called classic hallucinogens, serotonergic hallucinogens, or serotonergic psychedelics, and the term ''psychedelics'' is used more broadly to include all hallucinogens; this article uses the narrower definition of ''psychedelics''. Psychedelics cause specific psychological, visual, and auditory changes, and often a substantially altered state of consciousness.Leary, Timothy; Metzner, Ralph (1964). ''The Psychedelic Experience: A Manual Based on The Tibetan Book of the Dead'' Psychedelic states are often compared to meditative, psychodynamic or transcendental types of alterations of mind. The "classical" psychedelics, the psyc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RU-24969
RU-24,969 is a drug and research chemical widely used in scientific studies. It is a selective agonist at the 5-HT1A and 5-HT1B receptors, with preference for the latter. As with other 5-HT1B agonists such as CP-94,253, RU-24,969 has been found to increase the reinforcing properties of cocaine, suggesting a role for 5-HT1B receptors in cocaine addiction. See also * RU-28306 * SN-22 SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19nM at 5HT2 subtypes vs 514 nM at 5-HT1A receptors. Many related derivatives are known, most of which are ligand ... References 5-HT1A agonists 5-HT1B agonists 5-HT7 agonists Phenol ethers Tetrahydropyridines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SN-22
SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19nM at 5HT2 subtypes vs 514 nM at 5-HT1A receptors. Many related derivatives are known, most of which are ligands for 5-HT1A, 5-HT6 or dopamine D2 receptors or show SSRI activity. See also * BRL-54443 * LY-334370 * LY-367,265 * MPMI * MPTP * Naratriptan * N,N-Dimethyltryptamine * RU-24969 * Sertindole Sertindole, sold under the brand name Serdolect among others, is an antipsychotic medication. Sertindole was developed by the Danish pharmaceutical company Lundbeck and marketed under license by Abbott Labs. Like other atypical antipsychotics, i ... References Serotonin receptor agonists {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
