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| Formula | C10H12NO5P |
| Molar mass | 257.182 g·mol−1 |
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1-Amino-5-phosphonoindan-1-carboxylic acid (APICA) is a drug that is used in neuroscience research. It is a selective antagonist for the group II metabotropic glutamate receptors (mGluR2/3), and has been useful in the study of this receptor subfamily. [1] [2] [3] [4] [5]
Glutamic acid is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins. It is a non-essential nutrient for humans, meaning that the human body can synthesize enough for its use. It is also the most abundant excitatory neurotransmitter in the vertebrate nervous system. It serves as the precursor for the synthesis of the inhibitory gamma-aminobutyric acid (GABA) in GABAergic neurons.
The metabotropic glutamate receptors, or mGluRs, are a type of glutamate receptor that are active through an indirect metabotropic process. They are members of the group C family of G-protein-coupled receptors, or GPCRs. Like all glutamate receptors, mGluRs bind with glutamate, an amino acid that functions as an excitatory neurotransmitter.
SKF-82,958 is a synthetic compound of the benzazepine class that acts as a D1/D5 receptor full agonist. SKF-82,958 and similar D1-like-selective full agonists like SKF-81,297 and 6-Br-APB produce characteristic anorectic effects, hyperactivity and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine. SKF-82,958 was also subsequently found to act as an agonist of ERα with negligible activity at ERβ, making it a subtype-selective estrogen.
Fenobam is an imidazole derivative developed by McNeil Laboratories in the late 1970s as a novel anxiolytic drug with an at-the-time-unidentified molecular target in the brain. Subsequently, it was determined that fenobam acts as a potent and selective negative allosteric modulator of the metabotropic glutamate receptor subtype mGluR5, and it has been used as a lead compound for the development of a range of newer mGluR5 antagonists.
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.
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.
Metabotropic glutamate receptor 4 is a protein that in humans is encoded by the GRM4 gene.
Metabotropic glutamate receptor 5 is an excitatory Gq-coupled G protein-coupled receptor predominantly expressed on the postsynaptic sites of neurons. In humans, it is encoded by the GRM5 gene.
Metabotropic glutamate receptor 7 is a protein that in humans is encoded by the GRM7 gene.
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).
EGLU is a drug that is used in neuroscience research. It was one of the first compounds found that acts as a selective antagonist for the group II metabotropic glutamate receptors (mGluR2/3), and so has been useful in the characterization and study of this receptor subfamily.
MMPIP is a drug used in scientific research that acts as a selective antagonist for the metabotropic glutamate receptor subtype mGluR7. This receptor subtype appears to be involved in the downstream response to cocaine in the brain.
CPCCOEt is a drug used in scientific research, which acts as a non-competitive antagonist at the metabotropic glutamate receptor subtype mGluR1, with high selectivity although only moderate binding affinity. It is used mainly in basic research into the function of the mGluR1 receptor, including the study of behavioural effects in animals including effects on memory and addiction.
LY-307,452 is a drug used in neuroscience research, which was among the first compounds found that acts as a selective antagonist for the group II metabotropic glutamate receptors (mGluR2/3), and was useful in early studies of this receptor family, although it has largely been replaced by newer drugs such as LY-341,495. Its molecular formula is C21H25NO4
DCG-IV is a research drug which acts as a group-selective agonist for the group II metabotropic glutamate receptors (mGluR2/3). It has potent neuroprotective and anticonvulsant effects in animal studies, as well as showing anti-Parkinsonian effects, but also impairs the formation of memories.
LY-379,268 is a drug that is used in neuroscience research, which acts as a potent and selective agonist for the group II metabotropic glutamate receptors (mGluR2/3).
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 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.
PCCG-4 is a research drug which acts as a selective antagonist for the group II metabotropic glutamate receptors (mGluR2/3), with slight selectivity for mGluR2 although not sufficient to distinguish mGluR2 and mGluR3 responses from each other. It is used in research into the function of the group II metabotropic glutamate receptors.
MGS-0039 is a drug that is used in neuroscientific research, which acts as a potent and selective antagonist for group II of the metabotropic glutamate receptors (mGluR2/3). It produces antidepressant and anxiolytic effects in animal studies, and has been shown to boost release of dopamine and serotonin in specific brain areas. Research has suggested this may occur through a similar mechanism as that suggested for the similarly glutamatergic drug ketamine.
AZD 9272 is a drug which acts as a selective antagonist for the metabotropic glutamate receptor subtype mGluR5. It was unsuccessful in human trials as an analgesic, but continues to be widely used in research especially as its radiolabelled forms.
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