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Target intelligence / Profile preview
Motilin Receptor (MLNR)
- Target
- MLNR
- Molecular classification
- G protein-coupled receptor, Receptor, GPCR, Class A GPCR
01
Overview
The motilin receptor (MLNR), also known as GPR38 or MTLR1, is a G protein-coupled receptor that binds the peptide hormone motilin. It plays a central role in regulating gastrointestinal motility, particularly during fasting, by mediating contraction of smooth muscle cells in the stomach and small intestine during phase III of the migrating motor complex (MMC). It is predominantly expressed on enteric neurons, GI tract smooth muscle cells, and, in some species, endothelial cells.
- Other names
- GPR38MTLR1
02
Mechanism of action
Activation of Gq proteins leading to phospholipase C activation, IP₃ production, intracellular Ca²⁺ mobilization, and smooth muscle contraction; activation of PLC-IP₃-NOS-NO-sGC-cGMP cascade resulting in vasorelaxation
03
Biological functions
Signal transductionRegulation of gastrointestinal motilitySmooth muscle contractionPepsin secretionPancreatic enzyme releaseVasorelaxation
04
Disease associations
GastroparesisIrritable bowel syndrome with constipation predominance
05
Safety considerations
Side effects associated with non-selective agonistsEfficacy limitations of current drugsNeed for selective modulation strategies
06
Interacting drugs
Motilin
1 more in the full profile.
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