145084-28-2
基本信息
YM 022 >=98% (HPLC)
(R)-N-(2,3-Dihydro-1-(2-(2-methylphenyl)-2-oxoethyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)-N'-(3-methylphenyl)urea
(R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA
N-[(3R)-2,3-Dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N′-(3-methylphenyl)-urea
Urea, N-[(3R)-2,3-dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)-
物理化學(xué)性質(zhì)
常見問題列表
CCR1 68 pM (Ki) |
CCR2 63 nM (Ki) |
YM022 inhibits binding to canine pancreas CCK-A receptor in a dose-dependent manner, with an IC
50
value for [
3
H]devazepide binding of 136 nM.
YM022 inhibits the binding of [
125
I]CCK-8 to canine cloned gastrin/CCK-B receptor in a dose-dependent manner, with an IC
50
value for [
125
I]CCK-8 binding of 0.73 nM.
Selectivity [ratio of (IC
50
for gastrin/CCK-B receptor)/(IC
50
for CCK-A receptor)] of YM022 is 186.
YM022 (intravenous injection; 0.01-1 μM/kg) dose-dependently inhibits pentagastrin- and peptone meal-induced acid secretion with ED
50
values of 0.0261 and 0.0654 μmol/kg, respectively, without affecting histamine- or methacholine-induced acid secretion.
YM022 (subcutaneous injection; 300 μmol/kg; single dose) lowers the oxyntic mucosal HDC activity and raises the serum gastrin concentration in a dose-dependent manner (measured 24 h after dosage). Maximum enzyme inhibition is achieved at a dose of 300 μmol/kg ?for YM022 and the inhibition of HDC lasts for 4 weeks. At sacrifice, drug residues can be seen at the injection site for as long as 4 (YM022) weeks after injection in rat.
YM022 is suspended in 2% Methocel for oral ingestion and in PEG300 for subcutaneous injection.
Animal Model: | Rat |
Dosage: | 300 μmol/kg |
Administration: | Subcutaneous injection; 300 μmol/kg; single dose |
Result: | Suppressed the ECL cell activity for at least 4 as manifested in greatly reduced HDC activity, greatly elevated serum gastrin level. |