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ABT-239
ABT-239 is an H3-receptor inverse agonist developed by Abbott. It has stimulant and nootropic effects, and has been investigated as a treatment for ADHD, Alzheimer's disease, and schizophrenia Schizophrenia () is a mental disorder characterized variously by hallucinations (typically, Auditory hallucination#Schizophrenia, hearing voices), delusions, thought disorder, disorganized thinking and behavior, and Reduced affect display, f .... ABT-239 is more active at the human H3 receptor than comparable agents such as thioperamide, ciproxifan, and cipralisant. It was ultimately dropped from human trials after showing the dangerous cardiac side effect of QT prolongation, but is still widely used in animal research into H3 antagonists / inverse agonists. References External links * Nootropics H3 receptor antagonists Benzonitriles Benzofuranethanamines Pyrrolidines Biphenyls Nitriles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Histamine H3 Receptor
Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act as autoreceptors in presynaptic histaminergic neurons and control histamine turnover by feedback inhibition of histamine synthesis and release. The H3 receptor has also been shown to presynaptically inhibit the release of a number of other neurotransmitters (i.e. it acts as an inhibitory heteroreceptor) including, but probably not limited to dopamine, GABA, acetylcholine, noradrenaline, histamine and serotonin. The gene sequence for H3 receptors expresses only about 22% and 20% homology with both H1 and H2 receptors respectively. There is much interest in the histamine H3 receptor as a potential therapeutic target because of its involvement in the neuronal mechanism behind many cognitive disorders and especially its location in the central nervous system.Rapanelli, Maximiliano. “The Magnificent Two: Histamine and the H3 Receptor as Key Mod ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cipralisant
Cipralisant (GT-2331, tentative trade name Perceptin) is an extremely potent histamine H3 receptor ligand originally developed by Gliatech. Cipralisant was initially classified as a selective H3 antagonist, but newer research (2005) suggests also agonist properties, i.e., functional selectivity. The relatively recent cloning of human H3 receptor, as well as the discovery of its constitutive activity provided the ability to better assess the activity of H3 receptor ligands. Consequently, cipralisant was reassessed as an H3 receptor agonist in human and rat recombinant systems, showing functional selectivity 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 end ... and stimulating one type of G-protein coupled pathway while failing to activate other intracellular pathways. Gliatech file ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyrrolidines
Pyrrolidine, also known as tetrahydropyrrole, is an organic compound with the molecular formula (CH2)4NH. It is a cyclic secondary amine, also classified as a saturated heterocycle. It is a colourless liquid that is miscible with water and most organic solvents. It has a characteristic odor that has been described as "ammoniacal, fishy, shellfish-like". In addition to pyrrolidine itself, many substituted pyrrolidines are known. Production and synthesis Industrial production Pyrrolidine is prepared industrially by the reaction of 1,4-butanediol and ammonia at a temperature of 165–200 °C and a pressure of 17–21 MPa in the presence of a cobalt- and nickel oxide catalyst, which is supported on alumina. : The reaction is carried out in the liquid phase in a continuous tube- or tube bundle reactor, which is operated in the cycle gas method. The catalyst is arranged as a fixed-bed and the conversion is carried out in the downflow mode. The product is obtained after m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
H3 Receptor Antagonists
H3, H03 or H-3 may refer to: Entertainment * ''H3'' (film), a 2001 film about the 1981 Irish hunger strike * '' H3 – Halloween Horror Hostel'', a 2008 German horror-parody television film * '' Happy Hustle High'', a manga series by Rie Takada, originally titled "H3 School!" * h3h3Productions, styled " 3, a satirical YouTube channel Science * Triatomic hydrogen (H3), an unstable molecule * Trihydrogen cation (), one of the most abundant ions in the universe * Tritium (3H), or hydrogen-3, an isotope of hydrogen * ATC code H03 ''Thyroid therapy'', a subgroup of the Anatomical Therapeutic Chemical Classification System * British NVC community H3, a heath community of the British National Vegetation Classification system * Histamine H3 receptor, a human gene * Histone H3, a component of DNA higher structure in eukaryotic cells * Hekla 3 eruption, a huge volcanic eruption around 1000 BC Computing * HTTP/3, the third major version of the Hypertext Transfer Protocol * So ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nootropics
Nootropics ( or ) (colloquially brain supplements, smart drugs, cognitive enhancers, memory enhancers, or brain boosters) are chemical substances which purportedly improve cognitive functions, such as attention, memory, wakefulness, and self-control. In the United States, nootropics can be over-the-counter drugs and commonly advertised with unproven claims of effectiveness for improving cognition. The Federal Trade Commission and FDA have warned manufacturers and consumers about possible advertising fraud and marketing scams concerning nootropic supplements. Nootropics include both prescription drugs and dietary supplements marketed to enhance brain function, but while FDA-approved drugs have proven benefits and oversight, many dietary supplements lack evidence, may contain unapproved or hidden drugs, and pose safety and regulatory risks.Nootropics: Drugs vs Dietary Supplements for Brain Health. Operation Supplement Safety. https://www.opss.org/article/nootropics-drugs-vs-di ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biochemical Pharmacology (journal)
''Biochemical Pharmacology'' is a peer-reviewed medical journal published by Elsevier. It covers research on the pharmacodynamics and pharmacokinetics of drugs and non-therapeutic xenobiotics. The editor-in-chief is Jacques Piette, University of Liege. , accessed on February 11th, 2013 Abstracting and indexing The journal is abstracted and indexed in: According to the '''', the journal received a 2019impact factor
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QT Prolongation
QT or Qt may refer to: Businesses * The Qt Company, a Finnish software developer * QT Hotels & Resorts, an Australasian hospitality provider * QT Inc., an American bracelet manufacturer * QuikTrip, an American convenience store chain People * QT (musician) (born 1988), American pop singer * QTCinderella (born 1994), American Twitch streamer and YouTuber * Q-Tee, British rapper (active in the 1990s) * Quentin Tarantino (born 1963), American filmmaker Science and technology Computer software * Qt (software), a cross-platform application framework * QuickTime, a multimedia technology from Apple Inc. Heart medicine * QT interval, on an electrocardiogram ** Long QT syndrome, a rare condition ** Short QT syndrome, a very rare disease Units of measure * Quart (qt), an imperial unit of volume Television shows * '' QT: QueerTelevision'', a 1990s Canadian LGBT newsmagazine * ''Question Time'' (TV programme), a British panel debate (first aired 1979) Transport * QT (New York City ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ciproxifan
Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist. The histamine H3 receptor is an inhibitory autoreceptor located on histaminergic nerve terminals, and is believed to be involved in modulating the release of histamine in the brain. Histamine has an excitatory effect in the brain via H1 receptors in the cerebral cortex, and so drugs such as ciproxifan which block the H3 receptor and consequently allow more histamine to be released have an alertness-promoting effect. Ciproxifan produces wakefulness and attentiveness in animal studies, and produced cognitive enhancing effects without prominent stimulant effects at relatively low levels of receptor occupancy, and pronounced wakefulness at higher doses. It has therefore been proposed as a potential treatment for sleep disorders such as narcolepsy and to improve vigilance in old age, particularly in the treatment of conditions such as Alzheimer's disease Alzheimer's disease (AD) is a neurodegener ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Inverse Agonist
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either; they are in fact sometimes called ''blockers'' (examples include alpha blockers, beta blockers, and calcium channel blockers). Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists. A prerequisite for an inverse agonist response is that the receptor must have a constitutive (also known as intrinsic or basal) level of activity in the absence of any ligand. An agonist increases the activity of a receptor above its basal level, whereas an inverse agonist decreases the activity below the basal level. The efficacy of a full agonist is by definition 100%, a neutral antagonist has 0% efficacy, and an inverse agonist has < 0% (i.e., n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thioperamide
Thioperamide is a potent HRH4 antagonist and selective HRH3 antagonist capable of crossing the blood–brain barrier. It was used by Jean-Charles Schwartz in his early experiments regarding the H3 receptor. Thioperamide was found to be an antagonist of histamine autoreceptor An autoreceptor is a type of Receptor (biochemistry), receptor located in the cell membrane, membranes of neuron, nerve cells. It serves as part of a negative feedback loop in signal transduction. It is only sensitive to the neurotransmitters or ...s, which negatively regulate the release of histamine. The drug enhances the activity of histaminergic neurons by blocking autoreceptors, leading to greater release of histamine. Its action on H3 receptors is thought to promote wakefulness and improve memory consolidation. See also * H3 receptor antagonist References H3 receptor antagonists Thioureas Piperidines Imidazoles Cyclohexyl compounds {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
