The successful identification of hundreds of novel G-protein-coupled receptors (GPCRs) represents the greatest opportunity for novel drug development. Inspired by GPCR signaling, Creative Biolabs now provides a world-leading Magic™ GPCR cell line platform for receptor function studies. Our cell lines cover a wide range of GPCRs catering to the different needs. Here, we highly recommend the unique Magic™ M4 stable cell line to our customers all over the world.
Introduction to M4
Muscarinic acetylcholine receptors are acetylcholine receptors that form G protein-receptor complexes in certain neurons and other cells. They play vital roles as the main end-receptor stimulated by acetylcholine released from postganglionic fibers in the parasympathetic nervous system. By using selective radioactively labeled agonist and antagonist, 5 subtypes of muscarinic receptors have been determined, called M1-M5.
Fig. 1 Schematic representation of a hypothetical cholinergic synapse illustrating general synaptic localization and function of cholinergic receptors relevant to schizophrenia.1
The muscarinic acetylcholine M4 receptor is primarily found in the CNS, its distribution largely overlapping with that of M1 and M3 subtypes. M4 receptors function as inhibitory autoreceptors for acetylcholine, activation of which inhibits acetylcholine release in the striatum. M4 couples to the Galphai subunit which mediated signaling results in inhibition of adenylyl cyclases and reduction of cAMP levels.
Magic™ M4 Stable Cell Line
G-protein-coupled receptors (GPCRs) are the largest and most diverse group of membrane receptors in eukaryotes. These cell surface receptors act as an inbox for messages in the form of light energy, peptides, lipids, sugars, and proteins. Activation of a single G protein can affect the production of hundreds or even thousands of second messenger molecules (e.g. Ca2+, cAMP, DAG). Based on the idea that GPCR functions can be studied via second messengers, a special fluorescent biosensor was developed, which is extremely sensitive to activities of second messenger molecules. Upon GPCR motivation/inhibition, changes in second messengers will trigger rapid biosensors translocation from plasma membrane to cytosolic vesicles. This way, GPCR agonist/antagonist can be easily characterized/quantified by fluorescence position & intensity.
Magic™ M4 stable cell line was established by stable co-transfecting human M4 and cAMP-sensitive biosensor in U2OS cells. It has been validated using Isoproterenol as an M4 agonist in a High Content Analysis (HCA) platform and proved to be a highly efficient and convenient tool for assaying various compounds targeting M4.
Featured Advantages of Magic™ M4 Stable Cell Lines
In addition to M4, Creative Biolabs now offers many other Magic™ GPCR stable cell lines incorporated with cAMP-activated biosensors, including:
As a pioneer in the field of GPCR drug discovery and development, Creative Biolabs has successfully applied our special Magic™ GPCR stable cell lines to accelerate diverse custom projects. Now we provide well-established Magic™ biosensor cell line options to assess calcium-, cAMP-, DAG-related as well as multiplex pathway events of various GPCRs. If you cannot find your desired target in our catalog, we are always happy to establish a specific cell line upon custom request. Please don't hesitate to contact us for more information.
Reference
For Research Use Only.
