化合物 T22898
化合物 T22898 用途与合成方法
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) significantly increases the number and size of plaques, and it also causes a significant 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. |
