|
CECXG
CECXG (3'-ethyl-LY-341,495) is a research drug which acts as a potent and selective antagonist for the group II metabotropic glutamate receptors ( mGluR2/3), with reasonable selectivity for mGluR3. While it is some five times less potent than LY-341,495 LY-341495 is a research drug developed by the pharmaceutical company Eli Lilly, which acts as a potent and selective orthosteric antagonist for the group II metabotropic glutamate receptors ( mGluR2/3). It is used in scientific research in sever ... at mGluR3, it has 38x higher affinity for mGluR3 over mGluR2, making it one of the few ligands available that is able to distinguish between these two closely related receptor subtypes. References Drugs developed by Eli Lilly and Company Xanthenes MGlu2 receptor antagonists MGlu3 receptor antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY-341,495
LY-341495 is a research drug developed by the pharmaceutical company Eli Lilly, which acts as a potent and selective orthosteric antagonist for the group II metabotropic glutamate receptors ( mGluR2/3). It is used in scientific research in several different areas, showing antidepressant effects in animal models, increasing the behavioural effects of hallucinogenic drugs in animal tests, and increasing the analgesic effects of μ-opioid agonists, as well as modulating dopamine receptor function. The 1-fluorocyclopropane analog has a superior pharmacokinetic profile and similar mGluR2/3 affinity, and making a prodrug A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be ... from this with the heptyl ester increases bioavailability still further. See also * CECXG References {{ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabotropic Glutamate Receptor 3
Metabotropic glutamate receptor 3 (mGluR3) is an inhibitory Gi/G0-coupled G-protein coupled receptor (GPCR) generally localized to presynaptic sites of neurons in classical circuits. However, in higher cortical circuits in primates, mGluR3 are localized post-synaptically, where they strengthen rather than weaken synaptic connectivity. In humans, mGluR3 is encoded by the ''GRM3'' gene. Deficits in mGluR3 signaling have been linked to impaired cognition in humans, and to increased risk of schizophrenia, consistent with their expanding role in cortical evolution. Structure In humans, mGluR3 is encoded by the GRM3 gene on chromosome 7. At least five protein-coding isoforms are predicted based on genomic information. The mGluR3 protein is a seven-pass transmembrane protein. Function L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. Glutamatergic neurotransmission is involved i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabotropic Glutamate Receptor
The metabotropic glutamate receptors, or mGluRs, are a type of glutamate receptor that are active through an indirect metabotropic receptor, metabotropic process. They are members of the group C GPCR family, group C family of G-protein-coupled receptors, or GPCRs. Like all glutamate receptor (biochemistry), receptors, mGluRs bind with glutamate, an amino acid that functions as an excitatory neurotransmitter. Function and structure The mGluRs perform a variety of functions in the central and peripheral nervous systems: For example, they are involved in learning, memory, anxiety, and the perception of pain. They are found in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, and the cerebral cortex, as well as other parts of the brain and in peripheral tissues. Like other metabotropic receptors, mGluRs have G protein-coupled receptor, seven transmembrane domains that span the cell membrane. Unlike ionotropic receptors, metabotropic glutamate receptors are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabotropic Glutamate Receptor 2
Metabotropic glutamate receptor 2 (mGluR2) is a protein that, in humans, is encoded by the ''GRM2'' gene. mGluR2 is a G protein-coupled receptor (GPCR) that couples with the Gi alpha subunit. The receptor functions as an autoreceptor for glutamate, that upon activation, inhibits the emptying of vesicular contents at the presynaptic terminal of glutamatergic neurons. Structure In humans, mGluR2 is encoded by the ''GRM2'' gene on chromosome 3. At least three protein-coding isoforms are predicted based on genomic information, as well as numerous non-coding isoforms. The mGluR2 protein is a seven-pass transmembrane protein. Function In humans, mGluR2 is only expressed in the brain, and not in any other tissue. In the brain, mGluR2 is expressed in neurons as well as astrocytes. Subcellularly, mGluR2 is predominantly positioned at the presynaptic terminal, although it is also expressed at the postsynaptic terminal. The metabotropic glutamate receptors are a family of G protein-co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drugs Developed By Eli Lilly And Company
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic disorders. Classification Pharmaceutical drugs are often classified into drug classes—groups of related drugs that have simila ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Xanthenes
Xanthene (9''H''-xanthene, 10''H''-9-oxaanthracene) is the organic compound with the formula CH2 6H4sub>2O. It is a yellow solid that is soluble in common organic solvents. Xanthene itself is an obscure compound, but many of its derivatives are useful dyes. Xanthene dyes Dyes that contain a xanthene core include bikaverin, fluorescein, eosins, and rhodamines. Xanthene dyes tend to be fluorescent, yellow to pink to bluish red, brilliant dyes. Many xanthene dyes can be prepared by condensation of derivates of phthalic anhydride with derivates of resorcinol or 3-aminophenol. Further reading * See also * Xanthone * Xanthydrol Xanthydrol is an organic chemical compound. Its formula is C13 H10 O2. Its total molecular weight is 198.221 g/ mol. Xanthydrol is used to test the levels of urea in the bloodstream. Synthesis Xanthydrol can be produced by the reduction of xa ... References {{Reflist Dyes Fungicides ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
