Motilin GPCR Assays
Background of Motilin Receptor
Motilin receptor (MLN-R) belongs to the G-protein coupled receptor family and has motilin as its ligand. MLN-R is extensively found in the gastrointestinal (GI) region. MLN-R’s primary function is to maintain normal digestive progress and to send hunger signals from the gastrointestinal tract to the brain.
Fig.1. Structure of the Zebrafish MLN-R. (Uniprot ID F1QCD0; obtained from Alphafold)
Distribution and Function of Motilin Receptor
Despite the functional differences, MLN-R can be detected in the gastrointestinal region of many different animal species and is mostly found on muscle cells of the duodenum, jejunum, and other colons. MLN-R exerts beneficial actions in the treatment of gastric insufficiency, gastroparesis, and other digestive disorders. It also constitutes mammals' capability of vomiting.
Mechanism of Motilin Receptor
MLN-R specifically binds motilin and controls the regular contraction period with a high amplitude of digestive progress in the GI regions of mammals.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| MLN receptor | MLNR |
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Assay List of Motilin Receptor
Creative Biolabs can provide a range of assays of motilin receptor. You can choose the assay in the list or contact us for more information:
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| IP1 Assay | ||||
| S01YF-1122-KX624 | Magic™ Human Motilin In Vitro IP1 Assay | CHO-K1 | IP1 Assay | |
Published Data
| Paper Title | Roles of endothelial Motilin receptor and its signal transduction pathway in Motilin-induced left gastric artery relaxation in dogs |
| Journal | Frontiers in Physiology |
| Published | 2021 |
| Abstract | Motilin and motilin receptors are released cyclically during digestion and induce phase III gastric motility in fasted humans and dogs, promoting increased blood flow to the left gastric artery (LGA). The proven functional MLNR expression sites include the intestinal smooth muscle and myenteric plexus, and the expression of related RNA and protein has also been found in tissues other than the gastrointestinal tract. However, the same receptor may have different activation pathways for different downstream signaling molecules in different cell types. Research on the molecular basis and signal transduction pathway of MLNR regulating gastric artery blood flow on the gastrointestinal artery endothelial cell membrane has important physiological and pathological significance. Previous studies have demonstrated that MLNR antagonists inhibit motilin-induced relaxation of dog LGA in vitro or in vivo, suggesting that MLNR plays an irreplaceable role in this process. Therefore, the researchers focused on the specific functions of MLNR, G protein-coupled pathways, and relaxation mediators in motilin-induced LGA ring relaxation, and the role of the NO system in this process. |
| Result |
In this study, researchers constructed an in vitro model of LGA in dogs, and measured the motilin-induced relaxation of the LGA ring using wire myography and specific kits to detect the levels of NO and cGMP. Results showed that NO plays a key role in the process of MLNR-mediated LGA ring relaxation, in LGA endothelial cells, motilin induces relaxation through the NOS-NOsGC-cGMP and MLNR-GPR-PLC-IP3 signaling pathways. The surface calcium channel and prostaglandin I2 were also involved in this process, and antagonists of MLNR significantly inhibited the relaxation of LGA and the levels of NO and cGMP. These pathways constitute the molecular mechanism by which motilin and its receptors regulate LGA blood flow under physiological conditions. This research result may help to elucidate the specific molecular mechanism of gastroparesis in diabetic patients and improve the understanding of this complication.
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Fig.2. The role of MLNR and its antagonists in motilin-induced relaxation of canine LGA. (Li, 2021)
Reference
- Li, H.Y.; et al. Roles of endothelial Motilin receptor and its signal transduction pathway in Motilin-induced left gastric artery relaxation in dogs. Frontiers in Physiology. 2021, 12: 700430.
