Human MLNR

Figure. Concentration-dependent activation of MLNR by motilin

Reporter cells were transfected with either the expression plasmid for human motilin receptor (MLNR) or the mock plasmid and treated with various concentrations of motilin. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 590 pM.

motilin receptor
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
à la carte, Human non-orphan GPCRs

Motilin receptor

Motilin receptors are activated by motilin, a 22 amino-acid peptide derived from a precursor (MLN, P12872), which may also generate a motilin-associated peptide. There are significant species differences in the structure of motilin and its receptor. In humans and large mammals such as dog, activation of these receptors by motilin released from endocrine cells in the duodenal mucosa during fasting, induces propulsive phase III movements. This activity is associated with promoting hunger in humans. Drugs and other non-peptide compounds which activate the motilin receptor may generate a more long-lasting ability to increase cholinergic activity within the upper gut, to promote gastrointestinal motility; this activity is suggested to be responsible for the gastrointestinal prokinetic effects of certain macrolide antibiotics (often called motilides; e.g. erythromycin, azithromycin), although for many of these molecules the evidence is sparse. Relatively high doses may induce vomiting and in humans, nausea.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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