L-692585

L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a K_i of 0.8 nM. L-692585 acts directly on somatotropes causing GH release^[1][2]. IC50 & 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) signi?cantly increases the number and size of plaques, and it also causes a signi?cant 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].