Fmoc-DL-Leu-OH acts as a partial agonist of the neurotensin NTS1 receptor ( NTS1R ) with an EC 50 of 215.50 μM. Fmoc-DL-Leu-OH triggers intracellular calcium mobilization, and its activity is blocked by selective NTS1R antagonists. Fmoc-DL-Leu-OH can be used in the research of schizophrenia [1].
In Vitro, Fmoc-DL-Leu-OH (Compound 1) acts as a partial agonist of human NTS1R expressed in CHOK1 cells, with an EC50 of 215.50 μM and a potency reaching 60% of the maximum potency of NT[1]. Fmoc-DL-Leu-OH (50 μM) exhibited agonist activity at human NTS1R expressed in CHOK1 cells, which was blocked by the selective NTS1R antagonist SR-48692 with an IC50 of 3.79 nM[1]. Fmoc-DL-Leu-OH (60 min) shows no detectable binding to human NTS1R in a [3H]neurotensin competitive binding assay performed using stably transfected CHOK1 cell membranes[1].
References:
[1]. Fan Y, et al. The identification of neurotensin NTS1 receptor partial agonists through a ligand-based virtual screening approach. Bioorg Med Chem Lett. 2008;18(21):5789-5791.
In Vitro, Fmoc-DL-Leu-OH (Compound 1) acts as a partial agonist of human NTS1R expressed in CHOK1 cells, with an EC50 of 215.50 μM and a potency reaching 60% of the maximum potency of NT[1]. Fmoc-DL-Leu-OH (50 μM) exhibited agonist activity at human NTS1R expressed in CHOK1 cells, which was blocked by the selective NTS1R antagonist SR-48692 with an IC50 of 3.79 nM[1]. Fmoc-DL-Leu-OH (60 min) shows no detectable binding to human NTS1R in a [3H]neurotensin competitive binding assay performed using stably transfected CHOK1 cell membranes[1].
References:
[1]. Fan Y, et al. The identification of neurotensin NTS1 receptor partial agonists through a ligand-based virtual screening approach. Bioorg Med Chem Lett. 2008;18(21):5789-5791.