|
F-11,461
F-11,461 is a drug that acts as an agonist of the 5-HT1A receptor (Ki = 1.36 nM) that has been used as a radioligand in PET studies. It possesses modest affinity for the 5-HT7 (Ki = 9.1 nM) and D4 (Ki = 8.5 nM) receptors, although the interaction of F-11,461 with these receptors is not detectable with PET due to their relative scarcity in the brain. See also * Befiradol * 8-OH-DPAT 8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonists to be disco ... References {{Serotonergics Serotonin receptor agonists PET radiotracers Naphthalenes Piperazines Triazines Methoxy compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1A Receptor
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor, or 5-HT receptor, 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 hyperpolarisation 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 rece ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Radioligand
A radioligand is a radioactive biochemical substance (in particular, a ligand that is radiolabeled) that is used for diagnosis or for research-oriented study of the receptor systems of the body. In a neuroimaging application the radioligand is injected into the pertinent tissue, or infused into the bloodstream. It binds to its receptor. When the radioactive isotope in the ligand decays it can be measured by positron emission tomography (PET) or single-photon emission computed tomography (SPECT). In ''in vivo'' systems it is often used to quantify the binding of a test molecule to the binding site of a radioligand. The higher the affinity of the molecule the more radioligand is displaced from the binding site and the increasing radioactive decay can be measured by scintillography. This assay is commonly used to calculate the binding constant of molecules to receptors. The transport of the radioligand is described by receptor kinetics. History Radioligands are credited wit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Positron Emission Tomography
Positron emission tomography (PET) is a functional imaging technique that uses radioactive substances known as radiotracers to visualize and measure changes in metabolic processes, and in other physiological activities including blood flow, regional chemical composition, and absorption. Different tracers are used for various imaging purposes, depending on the target process within the body. For example: * Fluorodeoxyglucose ( 18F">sup>18FDG or FDG) is commonly used to detect cancer; * 18Fodium fluoride">sup>18Fodium fluoride (Na18F) is widely used for detecting bone formation; * Oxygen-15 (15O) is sometimes used to measure blood flow. PET is a common imaging technique, a medical scintillography technique used in nuclear medicine. A radiopharmaceutical – a radioisotope attached to a drug – is injected into the body as a radioactive tracer, tracer. When the radiopharmaceutical undergoes beta plus decay, a positron is emitted, and when the positron interacts with an or ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT7 Receptor
The 5-HT7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) The 5-HT7 receptor is coupled to Gs (stimulates the production of the intracellular signaling molecule cAMP) and is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in various blood vessels. This receptor has been a drug development target for the treatment of several clinical disorders. The 5-HT7 receptor is encoded by the ''HTR7'' gene, which in humans is transcribed into 3 different splice variants. Function When the 5-HT7 receptor is activated by serotonin, it sets off a cascade of events starting with release of the stimulatory G protein Gs from the GPCR complex. Gs in turn activates adenylate cyclase which increases intracellular levels of the second messenger cAMP. The 5-HT7 receptor plays a role in smooth muscle relaxation within the vasculature a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Receptor D4
The dopamine receptor D4 is a dopamine D2-like G protein-coupled receptor encoded by the gene on chromosome 11 at 11p15.5. The structure of DRD4 was recently reported in complex with the antipsychotic drug nemonapride. As with other dopamine receptor subtypes, the D4 receptor is activated by the neurotransmitter dopamine. It is linked to many neurological and psychiatric conditions including schizophrenia and bipolar disorder, ADHD, addictive behaviors, Parkinson's disease, and eating disorders such as anorexia nervosa. A weak association has been drawn between DRD4 and borderline personality disorder. It is also a target for drugs which treat schizophrenia and Parkinson's disease. The D4 receptor is considered to be D2-like in which the activated receptor inhibits the enzyme adenylate cyclase, thereby reducing the intracellular concentration of the second messenger cyclic AMP. Genetics The human protein is coded by the ''DRD4'' on chromosome 11 located in 11p1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Befiradol
Befiradol (F-13,640; NLX-112) is an experimental drug being studied for the treatment of levodopa-induced dyskinesia. It is a potent and selective 5-HT1A receptor full agonist. Pharmacology In recombinant cell lines expressing human 5-HT1A receptors, befiradol exhibits high agonist efficacy for a variety of signal transduction read-outs, including ERK phosphorylation, G-protein activation, receptor internalization and adenylyl cyclase inhibition. In rat hippocampal membranes it preferentially activates GalphaO proteins. In neurochemical experiments, befiradol activated 5-HT1A autoreceptors in rat dorsal Raphe nucleus as well as 5-HT1A heteroreceptors on pyramidal neurons in the frontal cortex. It has powerful analgesic and antiallodynic effects comparable to those of high doses of opioid painkillers, but with fewer and less prominent side effects, as well as little or no development of tolerance with repeated use. A structure–activity relationship (SAR) study reveale ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
8-OH-DPAT
8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonists to be discovered. Originally believed to be selective for the 5-HT1A receptor, 8-OH-DPAT was later found to act as a 5-HT7 receptor agonist and serotonin reuptake inhibitor/ releasing agent as well. In animal studies, 8-OH-DPAT has been shown to possess antidepressant, anxiolytic, serenic, anorectic, antiemetic, hypothermic, hypotensive, bradycardic, hyperventilative, and analgesic effects. See also * 5-OH-DPAT 5-OH-DPAT is a synthetic compound that acts as a dopamine receptor agonist with selectivity for the D2 receptor and D3 receptor subtypes. Only the (''S'')-enantiomer is active as an agonist, with the (''R'')-enantiomer being a weak antagonist at ... * 7-OH-DPAT * Bay R 1531 * MDAT * UH-301 References External link ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Agonists
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is rel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PET Radiotracers
A pet, or companion animal, is an animal kept primarily for a person's company or entertainment rather than as a working animal, livestock, or a laboratory animal. Popular pets are often considered to have attractive appearances, intelligence, and relatable personalities, but some pets may be taken in on an altruistic basis (such as a stray animal) and accepted by the owner regardless of these characteristics. Two of the most popular pets are dogs and cats. Other animals commonly kept include rabbits; ferrets; pigs; rodents such as gerbils, hamsters, chinchillas, rats, mice, and guinea pigs; birds such as parrots, passerines, and fowls; reptiles such as turtles, lizards, snakes, and iguanas; aquatic pets such as fish, freshwater snails, and saltwater snails; amphibians such as frogs and salamanders; and arthropod pets such as tarantulas and hermit crabs. Small pets may be grouped together as pocket pets, while the equine and bovine group include the largest ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naphthalenes
Naphthalene is an organic compound with formula . It is the simplest polycyclic aromatic hydrocarbon, and is a white crystalline solid with a characteristic odor that is detectable at concentrations as low as 0.08 ppm by mass. As an aromatic hydrocarbon, naphthalene's structure consists of a fused pair of benzene rings. It is best known as the main ingredient of traditional mothballs. History In the early 1820s, two separate reports described a white solid with a pungent odor derived from the distillation of coal tar. In 1821, John Kidd cited these two disclosures and then described many of this substance's properties and the means of its production. He proposed the name ''naphthaline'', as it had been derived from a kind of naphtha (a broad term encompassing any volatile, flammable liquid hydrocarbon mixture, including coal tar). Naphthalene's chemical formula was determined by Michael Faraday in 1826. The structure of two fused benzene rings was proposed by Emil Erlen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piperazines
Substituted piperazines are a class of chemical compounds based on a piperazine core. Some are used as recreational drugs and some are used in scientific research. List of substituted piperazines Benzylpiperazines File:Benzylpiperazine.svg, 1-Benzylpiperazine File:MBZP.svg, 1-Methyl-4-benzylpiperazine File:DBZP.svg, 1,4-Dibenzylpiperazine File:MDBZP.svg, 3,4-Methylenedioxy-1-benzylpiperazine File:2C-B-BZP.svg, 4-Bromo-2,5-dimethoxy-1-benzylpiperazine File:Methoxypiperamide.png, Methoxypiperamide File:Sunifiram.svg , Sunifiram File:3-Methylbenzylpiperazine structure.png, 3-Methylbenzylpiperazine * 1-Benzylpiperazine (BZP) * 1-Methyl-4-benzylpiperazine (MBZP) * 1,4-Dibenzylpiperazine (DBZP) * 3,4-Methylenedioxy-1-benzylpiperazine (MDBZP) * 4-Bromo-2,5-dimethoxy-1-benzylpiperazine (2C-B-BZP) * Methoxypiperamide (MeOP, MEXP) ((4-methoxyphenyl)(4-methylpiperazin-1-yl)methanone) * Sunifiram (1-benzoyl-4-propanoylpiperazine) * 3-Methylbenzylpiperazine (3-MeBZP) Befuralin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Triazines
Triazines are a class of nitrogen-containing heterocycles. The parent molecules' molecular formula is . They exist in three isomeric forms, 1,3,5-triazines being common. Structure The triazines have planar six-membered benzene-like ring but with three carbons replaced by nitrogens. The three isomers of triazine are distinguished by the positions of their nitrogen atoms, and are referred to as 1,2,3-triazine, 1,2,4-triazine, and 1,3,5-triazine. Other aromatic nitrogen heterocycles are pyridines with one ring nitrogen atom, diazines with 2 nitrogen atoms in the ring, triazoles with 3 nitrogens in a 5 membered ring, and tetrazines with 4 ring nitrogen atoms. Uses Melamine A well known triazine is melamine (2,4,6-triamino-1,3,5-triazine). With three amino substituents, melamine is a precursor to commercial resins. Guanamines are closely related to melamine, except with one amino substituent replaced by an organic group. This difference is exploited in the use of gua ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
