145455-35-2
145455-35-2 結構式
基本信息
L-692
L-692,585
L 692585,L692585
3-[[(2R)-2-hydroxypropyl]amino]-3-methyl-N-[(3R)-2-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-4,5-dihydro-3H-1-benzazepin-3-yl]butanamide
3-[[(2R)-2-Hydroxypropyl]amino]-3-methyl-N-[(3R)-2,3,4,5-tetrahydro-2-oxo-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-1-benzazepin-3-yl]-butanamide
Butanamide, 3-[[(2R)-2-hydroxypropyl]amino]-3-methyl-N-[(3R)-2,3,4,5-tetrahydro-2-oxo-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-1-benzazepin-3-yl]-
物理化學性質
常見問題列表
Ki: 0.8 nM (GHS-R1a)
L-692585 (10 μM; 2 min) produces a prompt transient increase in [Ca
2+
]
i
, following by the sustained decline to a plateau above the basal level in GH cells.
L-692585 (0.01-10 μM; 2 min) induces release of growth hormone (GH) in a dose-dependent manner from isolated porcine somatotropes.
L-692585 (100 nM) signi?cantly increases the number and size of plaques, and it also causes a signi?cant increase in total secretion index (TSI) .
L-692585 (0.01-0.1 mg/kg; i.v. once daily for 2 weeks) increases peak plasma GH levels and total GH release.
L-692585 (0.005-0.1 mg/kg; a single i.v.) significantly increases peak GH concentrations 4.3-fold at a dose of 0.005 mg/kg, 7-fold at a dose of 0.02 mg/kg, and 21-fold at a dose of 0.10 mg/kg in vivo.
| Animal Model: | Beagles (1-1.5 years old ; weighting 8.5-16.0 kg) |
| Dosage: | 0.01, 0.1 mg/kg |
| Administration: | I.v. once daily for 2 weeks |
| Result: | Increased the peak plasma GH levels and total GH release on days 1, 8 and 15 in a dose-dependent manner, and no desensitization was evident. |