Target Validation Information
Target ID T62306
Target Name Motilin receptor
Target Type
Clinical Trial
Drug Potency against Target MOTILIN Drug Info Ki = 0.36 nM [528545]
Action against Disease Model Camicinal GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of h uMan and rabbit gastrointestinal motility. In rabbit gastric antr uM, GSK962040 300 nmol L(-1)-10 micromol L(-1) caused a prolonged facilitation of the amplitude of cholinergically mediated contractions, to a maxim uM of 248 +/- 47% at 3 micromol L(-1). In h uMan-isolated stomach, GSK962040 10 micromol L(-1), erythromycin 10 micromol L(-1) and [Nle13]-motilin 100 nmol L(-1), each caused muscle contraction of similar amplitude. In conscious rabbits, intravenous doses of 5 mg kg(-1) GSK962040 or 10 mg kg(-1) erythromycin significantly increased faecal output over a 2-h period. [530085] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations The effect of motilin on food intake was investigated in nonfood-deprived mice. A significant increase in food intake was observed 1 h after ICV administration of motilin (3 nmol/mouse) and continued for 2 h. This effect was attenuated markedly by the motilin receptor antagonist GM-109 (0.3-3 nmol/mouse) in a dose-related manner. GM-109 alone had no effect on food intake. These results indicate that motilin receptors are present in the brain and may have a role in the regulation of food intake. [530085]
References
Ref 530085Neurogastroenterol Motil. 2009 Jun;21(6):657-64, e30-1.GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility.
Ref 528545J Med Chem. 2006 Nov 30;49(24):7190-7.Discovery of a new class of macrocyclic antagonists to the human motilin receptor.

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