The rabbit motilin receptor: molecular characterisation and pharmacology

Br J Pharmacol. 2003 Nov;140(5):948-54. doi: 10.1038/sj.bjp.0705505. Epub 2003 Sep 22.

Abstract

Following identification of the human motilin receptor, we isolated the rabbit orthologue by PCR amplification and found this to be 85% identical to the open reading frame of the human receptor. The protein encoded was 84% identical to the human polypeptide. In HEK293T cells transfected with the rabbit receptor, motilin concentration-dependently increased intracellular calcium mobilisation (pEC50=9.25). After transfection with Go1alpha, motilin similarly stimulated [35S]GTPgammaS binding (pEC50=8.87). Using both systems, similar values were obtained with the human receptor, with rank-order potencies of motilin=[Nle13]-motilin>erythromycin; ghrelin was ineffective. In circular muscle preparations of rabbit gastric antrum, [Nle13]-motilin 0.1-30 nM concentration-dependently increased the amplitude of electrically-evoked, neuronally-mediated contractions (pEC50=8.3); higher concentrations increased the muscle tension (30-3000 nM). Both responses to [Nle13]-motilin faded rapidly during its continual presence. Rat or human ghrelin 0.01-10 microM were without activity. Erythromycin 30-3000 nM and 10 microM, respectively, increased neuronal activity and muscle tension in rabbit stomach. Unlike [Nle13]-motilin, the increase in neuronal activity did not fade during continual presence of submaximally-effective concentrations of erythromycin; some fade was observed at higher concentrations. We conclude that the pharmacology of the rabbit motilin receptor is similar to the human orthologue and, when expressed as a recombinant, comparable to the native receptor. However, in terms of their ability to increase neuronal activity in rabbit stomach, [Nle13]-motilin and erythromycin are distinguished by different response kinetics, reflecting different rates of ligand degradation and/or interaction with the receptor.

MeSH terms

  • Animals
  • Base Sequence / genetics
  • Cell Line
  • Dose-Response Relationship, Drug
  • Humans
  • In Vitro Techniques
  • Male
  • Molecular Sequence Data
  • Motilin / pharmacology
  • Muscle Contraction / drug effects
  • Muscle Contraction / physiology
  • Protein Binding / drug effects
  • Protein Binding / physiology
  • Pyloric Antrum / drug effects
  • Pyloric Antrum / metabolism
  • Rabbits
  • Receptors, Gastrointestinal Hormone / agonists
  • Receptors, Gastrointestinal Hormone / chemistry*
  • Receptors, Gastrointestinal Hormone / genetics
  • Receptors, Gastrointestinal Hormone / metabolism*
  • Receptors, Neuropeptide / agonists
  • Receptors, Neuropeptide / chemistry*
  • Receptors, Neuropeptide / genetics
  • Receptors, Neuropeptide / metabolism*

Substances

  • Receptors, Gastrointestinal Hormone
  • Receptors, Neuropeptide
  • motilin receptor
  • Motilin