Muscarinic receptors are GPCRs that play a role in the parasympathetic nervous system. They consist of M1, M2, M3, M4, and M5 receptor subtypes, which are implicated in several physiological processes like peristalsis, micturition, and others. Several widespread illnesses, such as chronic obstructive pulmonary disease and asthma, are closely linked with dysfunctional muscarinic receptors. Targeting muscarinic receptors in the affected area is meaningful for the treatment of a variety of associated diseases. Accordingly, identifying muscarinic receptors may aid in the drug development of diseases.
Fig.1 M1 and M4 muscarinic acetylcholine receptors (mAChRs) expression in brain areas associated with psychosis.1
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Our Magic™ in vitro cell-based muscarinic receptor functional assay service incorporates a straightforward and efficient cell-based assay with muscarinic receptors functional assay that has the potential to be utilized to evaluate candidate samples and their capability to modulate muscarinic receptors. The principle of this assay is to examine the diacyl flux and calcium flux in response to G protein activation triggered by muscarinic receptors binding to ligands. During every stage of this procedure, our comprehensive, customized, and exceptional services will enable the diverse demands of global customers to be met.
Fig.2 The structure and signaling pathways of mAChRs.2
Our integrated Magic™ in vitro cell-based muscarinic receptor functional assay service overcomes the limits of traditional muscarinic receptor functional assays and has succeeded in achieving innovative developments in technology, applications, and other aspects. Our integrated Magic™ in vitro cell-based muscarinic receptor functional assay service can deliver significant benefits to global customers:
Representative Data 1: The cellular signaling and roles of two categories of muscarinic receptors, M1 (flag epitope-tagged) and hM3Dq (HA epitope-tagged), in Jurkat leukemic T cells may be activated by carbachol or clozapine, respectively. The results show that muscarinic receptor stimulation caused substantial calcium responses in Jurkat cells. When either muscarinic receptor was retrovirally transduced into primary mouse T cells, it was seen that both receptors were sensitive to stimulation, at least in terms of calcium increases, with carbachol or clozapine, respectively. In addition, transduction of PLCβ1, a vital mediator of response to superantigens in Jurkat cells, could strongly improve responses to stimulated muscarinic receptors in mouse T cells. Consequently, they demonstrated that co-expression of PLCβ1 and stimulation of M1 and synthetic hM3Dq receptors may activate primary murine T cells.
Fig.3 PLCβ1 significantly improves calcium responses in primary T cells with active muscarinic receptors.3
Representative Data 2: Expression of muscarinic receptor subtypes M1, M2, M3, and M4 has been evaluated in dASCs using RT-PCR. In addition, a western blotting assay was carried out to investigate M2 muscarinic receptor expression because of its crucial involvement in SCs9. This receptor subtype is present in ASCs and does not differ much amongst dASCs. Treatment with APE (Arecaidine Propargyl Ester) led to preferential activation of the M2 receptor, which in turn led to a significant decrease in cellular cAMP levels, proving the functionality of the M2 receptor in dASCs.
Fig.4 Muscarinic receptor subtypes expression.4
Constantly, in response to customers' feedback, Creative Biolabs endeavors the develop and improve technological innovations. For more details about our Magic™ in vitro cell-based muscarinic receptor functional assay service, please don't hesitate to contact us. We are eagerly anticipating forging long-term partnerships with customers all across the world.
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