The effects of NN414, a SUR1/Kir6.2 selective potassium channel opener in subjects with type 2 diabetes.
Reducing the workload of the beta cell by inhibiting insulin secretion may provide beneficial effects for patients with type 2 diabetes. The aim of this study was to investigate the effect of NN414, a beta cell selective potassium channel opener in patients with type 2 diabetes. 24 patients were treated for seven days (placebo, 1.5, 4.5, and 10 mg/kg). In accordance with the pharmacological profile a significant and selective inhibition of insulin secretion was observed (1 h post dose). There were no statistically significant effects on overall glycaemic control. Based on OGTT derived parameters a borderline significant improvement in beta-cell function (1st and 2nd phase insulin secretion) was observed from Day 1 to Day 7.
Zdravkovic
M
M
Novo Nordisk A/S, Global Development, Denmark. mzd@novonordisk.com
Kruse
M
M
Rost
K L
KL
Møss
J
J
Kecskes
A
A
D018528:ATP-Binding Cassette Transporters / Q000819:agonists* / Q000378:metabolism; D000368:Aged; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000008:administration & dosage*; D003499:Cyclic S-Oxides / Q000008:administration & dosage*; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy* / Q000378:metabolism*; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D007328:Insulin / Q000378:metabolism*; D000078790:Insulin Secretion; D050417:Insulin-Secreting Cells / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D015221:Potassium Channels / Q000819:agonists* / Q000378:metabolism; D024661:Potassium Channels, Inwardly Rectifying / Q000819:agonists* / Q000378:metabolism; D011955:Receptors, Drug / Q000819:agonists* / Q000378:metabolism; D064233:Sulfonylurea Receptors; D013997:Time Factors
C577507:ABCC8 protein, human; D018528:ATP-Binding Cassette Transporters; D019086:Bridged Bicyclo Compounds, Heterocyclic; D003499:Cyclic S-Oxides; D007328:Insulin; C475618:NN 414; D015221:Potassium Channels; D024661:Potassium Channels, Inwardly Rectifying; D011955:Receptors, Drug; D064233:Sulfonylurea Receptors