| Description |
L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release[1][2].
|
| Related Catalog |
|
| Target |
Ki: 0.8 nM (GHS-R1a)[1]
|
| In Vitro |
L-692585 (10 µM; 2 min) produces a prompt transient increase in [Ca2+]i, following by the sustained decline to a plateau above the basal level in GH cells[2]. L-692585 (0.01-10 µM; 2 min) induces release of growth hormone (GH) in a dose-dependent manner from isolated porcine somatotropes[2]. L-692585 (100 nM) significantly increases the number and size of plaques, and it also causes a significant increase in total secretion index (TSI) [2].
|
| In Vivo |
L-692585 (0.01-0.1 mg/kg; i.v. once daily for 2 weeks) increases peak plasma GH levels and total GH release[3]. 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[3]. Animal Model: Beagles (1-1.5 years old ; weighting 8.5-16.0 kg)[3] 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.
|
| References |
[1]. Smith RG, et, al. Peptidomimetic regulation of growth hormone secretion. Endocr Rev. 1997 Oct; 18(5): 621-45. [2]. Glavaski-Joksimovic A, et, al. Mechanism of action of the growth hormone secretagogue, L-692,585, on isolated porcine somatotropes. J Endocrinol. 2002 Dec; 175(3): 625-36. [3]. Jacks T, et, al. Effects of acute and repeated intravenous administration of L-692,585, a novel non-peptidyl growth hormone secretagogue, on plasma growth hormone, IGF-1, ACTH, cortisol, prolactin, insulin, and thyroxine levels in beagles. J Endocrinol. 1994 Nov; 143(2): 399-406.
|
