Overview: Motilin receptors (provisional nomenclature, see Foord et al., 2005) are activated by a 22 amino-acid peptide derived from a precursor (ENSG00000096395), which also generates motilin-associated peptide. These receptors are suggested to be responsible for the gastrointestinal prokinetic effects of motilides (particular macrolide antibiotics).
| Nomenclature | Motilin |
|---|---|
| Other names | MTLR1 (Feighner et al., 1999), GPR38 (Mckee et al., 1997) |
| Ensembl ID | ENSG00000102539 |
| Principal transduction | Gq/11 (Depoortere and Peeters, 1995); Feighner et al., 1999) |
| Rank order of potency | Motilin > ABT229, mitemcimal > erythromycin (Clark et al., 1999) |
| Selective agonists | ABT229 (Lartey et al., 1995), mitemcinal (Koga et al., 1994; Takanashi et al., 2007) |
| Selective antagonists | GM109 (Takanashi et al., 1995); pA2 7.2–7.5 Clark et al., 1999) |
| Probes | [125I]-Motilin (0.1 nM, Feighner et al., 1999) |
Glossary
Abbreviations:
- ABT229
8,9-anhydro-4′′-deoxy-3′-N-desmethyl-3′-N-ethylerythromycin B 6,9-hemiacetal
- GM109
phe-cyclo[Lys-Tyr(3-tBu)-β-Ala].trifluoroacetate
- mitemcinal
de(N-methyl)-11-deoxy-N-isopropyl-12-O-methyl-11-oxo-8,9-anhydroerythromycin A 6,9-hemiacetal fumaric acid, also known as GM611
Further Reading
De Smet B, Mitselos A, Depoortere I (2009). Motilin and ghrelin as prokinetic drug targets. Pharmacol Ther123: 207–223.
Foord SM, Bonner TI, Neubig RR, Rosser EM, Pin JP, Davenport AP et al. (2005). International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev57: 279–288.
Takeshita E, Matsuura B, Dong M, Miller LJ, Matsui H, Onji M (2006). Molecular characterization and distribution of motilin family receptors in the human gastrointestinal tract. J Gastroenterol41: 223–230.
References
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