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1-(indolizin-3-yl)-2-(methylamino)propan-1-one
1Z2MAP1O, also known as 1-(indolizin-3-yl)-2-(methylamino)propan-1-one, is a monoamine releasing agent and serotonin receptor receptor modulator, modulator of the indolizine class. It is an structural analog, analogue of BK-NM-AMT (β-keto-''N''-methyl-α-methyltryptamine) in which the indole ring (chemistry), ring has been replaced with an indolizine ring. 1Z2MAP1O has been found to be a serotonin releasing agent, serotonin and dopamine releasing agent as well as a weak serotonin 5-HT1B receptor, 5-HT1B receptor agonist and serotonin 5-HT2B receptor, 5-HT2B receptor receptor antagonist, antagonist. Conversely, its activity as a norepinephrine releasing agent was not reported, and it was inactive at the remaining sites of the 47screened biological target, targets. The drug's values for induction of monoamine release were 109nM for serotonin and 227nM for dopamine in Chinese hamster ovary cell, Chinese hamster ovary (CHO) cell (biology), cells expressing the human monoamine transp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Releasing Agent
A monoamine releasing agent (MRA), or simply monoamine releaser, is a drug that induces the release of one or more monoamine neurotransmitters from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitters and hence enhanced signaling by those neurotransmitters. The monoamine neurotransmitters include serotonin, norepinephrine, and dopamine; MRAs can induce the release of one or more of these neurotransmitters. MRAs work by reversing the direction of the monoamine transporters (MATs), including the serotonin transporter (SERT), norepinephrine transporter (NET), and/or dopamine transporter (DAT), causing them to promote efflux of non-vesicular cytoplasmic monoamine neurotransmitter rather than reuptake of synaptic monoamine neurotransmitter. Many, but not all MRAs, also reverse the direction of the vesicular monoamine transporter 2 (VMAT2), thereby additionally resulting in efflux of vesicular monoamine neuro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tactogen
Tactogen is a public benefit corporation and start-up pharmaceutical company based in Palo Alto, California that is developing novel MDMA-like entactogens and psychedelics as medicines. Its stated goal is to develop new MDMA-like drugs with improved effectiveness, tolerability, and safety, as well as gentleness and accessibility, for treatment of psychiatric disorders and other conditions. Tactogen was co-founded by neuroscientist Matthew J. Baggott and Luke Pustejovsky in 2020. Baggott is the chief executive officer (CEO) while Pustejovsky is the chief operating officer (COO). Drug candidates Tactogen has patented various novel entactogen-like compounds from different chemical families. These include benzofurans like 5-MAPB, 5-MBPB, and BK-5-MAPB, benzothiophenes like 5-MAPBT, α-alkyltryptamines like BK-NM-AMT and BK-5F-NM-AMT, indolizines like 2ZEDMA, 1ZP2MA, and Z2MAP1O, 2-aminoindanes like "BFAI", and non-racemic mixtures of enantiomers. It also has several dru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Releasing Agent
A dopamine releasing agent (DRA) is a type of drug which induces the release of dopamine in the Body (biology), body and/or brain. No binding selectivity, selective DRAs are currently known. However, non-selective DRAs, including norepinephrine–dopamine releasing agents (NDRAs) like amphetamine and methamphetamine, serotonin–norepinephrine–dopamine releasing agents (SNDRAs) like MDMA and mephedrone, and serotonin–dopamine releasing agents (SDRAs) like 5-chloro-αMT and BK-NM-AMT, are known. A closely related type of drug is a dopamine reuptake inhibitor (DRI). In contrast to the case of DRAs, many selective DRIs are known. Examples of selective DRIs include amineptine, modafinil, and vanoxerine. Selectivity No binding selectivity, selective and robust DRAs are currently known. The lack of known selective DRAs is related to the fact that it has proven extremely difficult to separate dopamine transporter (DAT) affinity (pharmacology), affinity from norepinephrine transpo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2ZEDMA
TACT908, also known as -(indolizin-1-yl)ethylimethylamine (2ZEDMA), is a serotonin receptor agonist which is under development for the treatment of cluster headaches. It is an positional isomer of the famous tryptamine serotonergic psychedelic ''N'',''N''-dimethyltryptamine (DMT) in which the indole ring has been replaced with an indolizine ring. The drug acts as a serotonin 5-HT1B and 5-HT2A receptor agonist. Its at the serotonin 5-HT2A receptor is 52nM ( ≈ 30% of that of serotonin) and its at the serotonin 5-HT1B receptor is 143nM. TACT908 is said to be a non-hallucinogenic serotonin 5-HT2A receptor agonist. It showed little or no activity at 45other screened targets, including the serotonin 5-HT1A, 5-HT2B, and 5-HT3 receptors as well as the monoamine transporters (MATs). Other serotonin receptors besides the preceding, such as the serotonin 5-HT2C receptor, were not assessed. The drug was a weak monoamine oxidase inhibitor (MAOI), specifically of monoamine oxidase A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Patent
A patent is a type of intellectual property that gives its owner the legal right to exclude others from making, using, or selling an invention for a limited period of time in exchange for publishing an sufficiency of disclosure, enabling disclosure of the invention."A patent is not the grant of a right to make or use or sell. It does not, directly or indirectly, imply any such right. It grants only the right to exclude others. The supposition that a right to make is created by the patent grant is obviously inconsistent with the established distinctions between generic and specific patents, and with the well-known fact that a very considerable portion of the patents granted are in a field covered by a former relatively generic or basic patent, are tributary to such earlier patent, and cannot be practiced unless by license thereunder." – ''Herman v. Youngstown Car Mfg. Co.'', 191 F. 579, 584–85, 112 CCA 185 (6th Cir. 1911) In most countries, patent rights fall under private la ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Transporter
The serotonin transporter (SERT or 5-HTT) also known as the sodium-dependent serotonin transporter and solute carrier family 6 member 4 is a protein that in humans is encoded by the SLC6A4 gene. SERT is a type of monoamine transporter protein that transports the neurotransmitter serotonin from the synaptic cleft back to the presynaptic neuron, in a process known as serotonin reuptake. This transport of serotonin by the SERT protein terminates the action of serotonin and recycles it in a sodium-dependent manner. Many antidepressant medications of the SSRI and tricyclic antidepressant classes work by binding to SERT and thus reducing serotonin reuptake. It is a member of the sodium:neurotransmitter symporter family. A repeat length polymorphism in the promoter of this gene has been shown to affect the rate of serotonin uptake and may play a role in sudden infant death syndrome, aggressive behavior in Alzheimer disease patients, post-traumatic stress disorder and depression ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine Transporter
The norepinephrine transporter (NET), also known as noradrenaline transporter (NAT), is a protein that in humans is encoded by the solute carrier family 6 member 2 (SLC6A2) gene. NET is a monoamine transporter and is responsible for the sodium-chloride (Na+/Cl−)-dependent reuptake of extracellular norepinephrine (NE), which is also known as noradrenaline. NET can also reuptake extracellular dopamine (DA). The reuptake of these two neurotransmitters is essential in regulating concentrations in the synaptic cleft. NETs, along with the other monoamine transporters, are the targets of many antidepressants and recreational drugs. In addition, altered NET availability is associated with ADHD. There is evidence that single-nucleotide polymorphisms in the NET gene (''SLC6A2'') may be an underlying factor in some of these disorders. Gene The norepinephrine transporter gene, SLC6A2 is located on human chromosome 16 locus 16q12.2. This gene is encoded by 14 exons. Based on the nucleotid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Transporter
The dopamine transporter (DAT, also sodium-dependent dopamine transporter) is a membrane-spanning protein coded for in humans by the ''SLC6A3'' gene (also known as ''DAT1''), that pumps the neurotransmitter dopamine out of the synaptic cleft back into cytosol. In the cytosol, other transporters sequester the dopamine into Vesicle (biology and chemistry), vesicles for storage and later release. Dopamine reuptake via DAT provides the primary mechanism through which dopamine is cleared from synapses, although there may be an exception in the prefrontal cortex, where evidence points to a possibly larger role of the norepinephrine transporter. DAT is implicated in a number of dopamine-related disorders, including ADHD, attention deficit hyperactivity disorder, bipolar disorder, clinical depression, eating disorders, and substance use disorders. The gene that encodes the DAT protein is located on chromosome 5, consists of 15 coding exons, and is roughly 64 base pair#Length measuremen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Transporter
Monoamine transporters (MATs) are proteins that function as integral Cell membrane, plasma-membrane Neurotransmitter transporter, transporters to regulate concentrations of extracellular monoamine neurotransmitters. The three major classes are serotonin transporters (SERTs), dopamine transporters (DATs), and norepinephrine transporters (NETs) and are responsible for the reuptake of their associated amine neurotransmitters (serotonin, dopamine, and norepinephrine). MATs are located just outside the synaptic cleft (peri-synaptically), transporting monoamine transmitter overflow from the synaptic cleft back to the cytoplasm of the pre-synaptic neuron. MAT regulation generally occurs through protein phosphorylation and post-translational modification. Due to their significance in neuronal signaling, MATs are commonly associated with drugs used to Psychiatric medication, treat mental disorders as well as recreational drugs. Compounds targeting MATs range from medications such as the wi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cell (biology)
The cell is the basic structural and functional unit of all life, forms of life. Every cell consists of cytoplasm enclosed within a Cell membrane, membrane; many cells contain organelles, each with a specific function. The term comes from the Latin word meaning 'small room'. Most cells are only visible under a light microscope, microscope. Cells Abiogenesis, emerged on Earth about 4 billion years ago. All cells are capable of Self-replication, replication, protein synthesis, and cell motility, motility. Cells are broadly categorized into two types: eukaryotic cells, which possess a Cell nucleus, nucleus, and prokaryotic, prokaryotic cells, which lack a nucleus but have a nucleoid region. Prokaryotes are single-celled organisms such as bacteria, whereas eukaryotes can be either single-celled, such as amoebae, or multicellular organism, multicellular, such as some algae, plants, animals, and fungi. Eukaryotic cells contain organelles including Mitochondrion, mitochondria, which ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chinese Hamster Ovary Cell
Chinese hamster ovary (CHO) cells are a family of immortalized cell lines derived from epithelial cells of the ovary of the Chinese hamster, often used in biological and medical research and commercially in the production of recombinant therapeutic proteins. They have found wide use in studies of genetics, toxicity screening, nutrition and gene expression, and particularly since the 1980s to express recombinant proteins. CHO cells are the most commonly used mammalian hosts for industrial production of recombinant protein therapeutics. History Chinese hamsters were first used in medical research in 1919, when Dr. E.T. Hsieh of the Peking Union Medical College used captured hamsters from the local fields for typing pneumococci. They were subsequently found by Jocelyn Smyly and Charles Young, two other doctors at the same institute, to be excellent vectors for transmission of kala-azar ( visceral leishmaniasis), facilitating ''Leishmania'' research. Unsuccessful attempts were m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
