Metabotropic Glutamate Family Related Drug Discovery Products
Membrane proteins are the most successful class of therapeutic targets. Creative Biolabs has developed a comprehensive collection of membrane protein in vitro assays for drug discovery that cover most membrane protein targets.
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Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs' membrane preparations are useful for membrane protein research. We offer membrane preparations to study the role of membrane proteins in diseases. Membrane preparations from Creative Biolabs are quality-assured frozen membranes from cells expressing recombinant or natural receptors.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
Glutamate is now regarded as the main excitatory neurotransmitter and is directly engaged in a wide range of neuronal and glial activities. Glutamate is known to have the potential to act as a potent endogenous neurotoxic agent, which is proposed to play a critical role in the development or progression of a variety of neurological disorders. This is in addition to its well-documented involvement in learning and memory acquisition processes. A variety of ionotropic glutamate receptors and channels are the only mechanisms by which glutamate exerts its neurotransmitter effects. Moreover, it might increase phosphoinositide turnover with effects that are compatible with G-protein-coupled receptor mediation.
Fig.1 Multiple signalling pathways activated by the metabotropic glutamate receptor. (Hermans, 2001)
Creative Biolabs can offer high-quality metabotropic glutamate family in vitro assays and products to contribute to the success of your project:
Metabotropic Glutamate GPCR Assays 
GPCR Assay Kits 
GPCR Cell Lines 
GPCR Membranes 
Membrane Protein Tools
Overview of Metabotropic Glutamate Family
There are eight mammalian mGlu receptors in this family group. Based on their sequence similarity, preferred signal transduction methods, and relative pharmacology, these have been divided into three subgroups. Group I mGlus includes mGlu1 and mGlu5, which are coupled to phosphoinositide hydrolysis and are selectively activated by 3,5-dihydroxyphenylglycine (3,5-DHPG); group II comprises mGlu2 and mGlu3, which in recombinant systems are negatively coupled to adenylate cyclase; group III consists of mGlu4, mGlu6, mGlu7 and mGlu8, which are also negatively coupled to adenylate cyclase and are activated by 2-amino-4-phosphonobutyrate.
- Group I
In the CNS, immunoreactivity for mGlu1 has been widely seen, with Purkinje cells of the cerebellar cortex and mitral/tufted cells of the olfactory bulb exhibiting the strongest immunoreactivity. The other member of group I mGlus, known as mGlu5, has been found to have a distribution that is broadly complimentary to that of mGlu1 across the CNS. The cerebral cortex, hippocampus, subiculum, main and auxiliary olfactory bulbs, anterior olfactory nucleus, olfactory tubercle, striatum, nucleus accumbens, and lateral septal nucleus have all shown intense expression.
- Group II
The Golgi cells in the cerebellar cortex, the mitral cells of the accessory olfactory bulb, the exterior part of the anterior olfactory nucleus, and some neurons in the entorhinal and parasubicular cortices have been found to express mGlu2 at the highest levels. The thalamic reticular nucleus neurons express mGlu3 the most prominently, while it is widely expressed throughout the CNS. In numerous locations, including the corpus callosum and anterior commissure, glial cells also express mGlu3.
- Group III
Among group III mGlus, mGlu7 has the widest distribution, whereas mGlu6 is mostly found in the retina. The cerebellar granule cells are those where mGlu4 is expressed the most strongly. Compared to mGlu7, mGlu8 has a more constrained expression pattern. The main and auxiliary olfactory bulbs, anterior olfactory nucleus, piriform cortex, entorhinal cortex, pontine nuclei, and lateral reticular nucleus of the medulla oblongata all have prominent mGlu8 expression.
Fig.2 Distribution of mGlu receptors. (Ferraguti & Shigemoto, 2006)
References
- Hermans, E.; CHALLISS, R.J. Structural, signalling and regulatory properties of the group I metabotropic glutamate receptors: prototypic family C G-protein-coupled receptors. Biochemical Journal. 2001, 359(3): 465-484.
- Ferraguti, F.; Shigemoto, R. Metabotropic glutamate receptors. Cell and tissue research. 2006, 326(2): 483-504.
