title: Mosapride citrate increases postprandial glucagon-like peptide-1, insulin, and gene expression of sweet taste receptors.
abstract: OBJECTIVE
  Mosapride citrate-a prokinetic agent-improves hemoglobin A1c levels in diabetic patients; however, the underlying mechanism is unclear. We aimed to clarify this mechanism.
  
  
  METHODS
  Preprandial and postprandial (90 min after a meal) blood was obtained from 12 healthy men, and serum insulin and plasma active glucagon-like peptide-1 concentrations were measured. Measurements were also taken after the administration of 5 mg of mosapride citrate three times per day after every meal for 14 days. In addition, C57BL/6 mice were permitted free access to water containing 0.04 % domperidone (D group) or 0.02 % mosapride citrate (M group) for 2 weeks (four mice per group). T1r2 (taste receptor, type 1, member 2), T1r3, and Gnat3 (guanine nucleotide-binding protein, alpha transducing 3) mRNA expression levels of the stomach, duodenum, and proximal and mid-jejunum were evaluated.
  
  
  RESULTS
  In human subjects, postprandial plasma active glucagon-like peptide-1 and serum insulin concentrations after administration of mosapride citrate were significantly higher than those pre-administration (4.8 ± 2.2 pmol/L, 45.6 ± 41.6 μIU/mL, and 3.7 ± 1.2 pmol/L, 34.1 ± 28.4 μIU/mL, respectively). The mouse expression levels of T1r2 and Gnat3 in the proximal jejunum and mid-jejunum in the M group (4.1 ± 1.8-fold, 3.1 ± 1.6-fold, and 4.6 ± 0.8-fold, 3.1 ± 0.9-fold increases, respectively), were significantly higher than those of the control group.
  
  
  CONCLUSIONS
  The administration of mosapride citrate for 2 weeks enhanced postprandial plasma active glucagon-like peptide-1 and serum insulin concentration and increased the expression of sweet taste receptors in the upper intestine.
authors.affiliation: Department of Gastroenterology and Nephrology, Graduate School of Medicine, Chiba University, Inohana 1-8-1, Chuo-Ku, Chiba City, 260-8670, Japan, d-maruoka@biscuit.ocn.ne.jp.
authors.forename: Daisuke
authors.initials: D
authors.lastname: Maruoka
authors.forename: Makoto
authors.initials: M
authors.lastname: Arai
authors.forename: Takeshi
authors.initials: T
authors.lastname: Tanaka
authors.forename: Kenichiro
authors.initials: K
authors.lastname: Okimoto
authors.forename: Arata
authors.initials: A
authors.lastname: Oyamada
authors.forename: Shoko
authors.initials: S
authors.lastname: Minemura
authors.forename: Masaru
authors.initials: M
authors.lastname: Tsuboi
authors.forename: Tomoaki
authors.initials: T
authors.lastname: Matsumura
authors.forename: Tomoo
authors.initials: T
authors.lastname: Nakagawa
authors.forename: Tatsuo
authors.initials: T
authors.lastname: Kanda
authors.forename: Tatsuro
authors.initials: T
authors.lastname: Katsuno
authors.forename: Fumio
authors.initials: F
authors.lastname: Imazeki
authors.forename: Osamu
authors.initials: O
authors.lastname: Yokosuka
mesh_terms: D000328:Adult; D000818:Animals; D001549:Benzamides / Q000008:administration & dosage*; D004334:Drug Administration Schedule; D005765:Gastrointestinal Agents / Q000008:administration & dosage*; D052216:Glucagon-Like Peptide 1 / Q000097:blood*; D006801:Humans; D007328:Insulin / Q000097:blood*; D007413:Intestinal Mucosa / Q000187:drug effects / Q000378:metabolism; D007583:Jejunum / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008810:Mice, Inbred C57BL; D009025:Morpholines / Q000008:administration & dosage*; D019518:Postprandial Period; D012333:RNA, Messenger / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D013649:Taste; D013997:Time Factors; D015293:Transducin / Q000235:genetics / Q000378:metabolism; D015854:Up-Regulation
chemical_list: D001549:Benzamides; D005765:Gastrointestinal Agents; D007328:Insulin; D009025:Morpholines; D012333:RNA, Messenger; D043562:Receptors, G-Protein-Coupled; C431926:taste receptors, type 1; D052216:Glucagon-Like Peptide 1; D015293:Transducin; C062720:mosapride