DeLeon, Chelsea; Pemberton, Kyle; Green, Michael; Kalajdzic, Vanja; Rosato, Martina; Xu, Fenglian; Arnatt, Christopher published the artcile< Novel GPER Agonist, CITFA, Increases Neurite Growth in Rat Embryonic (E18) Hippocampal Neurons>, Recommanded Product: 2-Bromo-4-isopropylaniline, the main research area is GPER GPER30 agonist CITFA neurite growth hippocampus antagonist neurodevelopment; Estrogen; G-protein coupled estrogen receptor (GPER/GPR30); agonist; antagonist neurodevelopment; calcium signaling; embryonic primary culture; hippocampus; neurite outgrowth.
Numerous studies have reported neuroprotective and procognitive effects of estrogens. The estrogen 17β-estradiol (E2) activates both the classical nuclear estrogen receptors ERα and ERβ as well as the G protein-coupled estrogen receptor (GPER). The differential effects of targeting the classical estrogen receptors over GPER are not well-understood. A limited number of selective GPER compounds have been described. In this study, 10 novel compounds were synthesized and exhibited half-maximal effective concentration values greater than the known GPER agonist G-1 in calcium mobilization assays performed in nonadherent HL-60 cells. Of these compounds, 2-cyclohexyl-4-isopropyl-N-((5-(tetrahydro-2H-pyran-2-yl)furan-2-yl)methyl)aniline, referred to as CITFA, significantly increased axonal and dendritic growth in neurons extracted from embryonic day 18 (E18) fetal rat hippocampal neurons. Confirmation of the results was performed by treating E18 hippocampal neurons with known GPER-selective antagonist G-36 and challenging with either E2, G-1, or CITFA. Results from these studies revealed an indistinguishable difference in neurite outgrowth between the treatment and control groups, exhibiting that neurite outgrowth in response to G-1 and CITFA originates from GPER activation and can be abolished with pretreatment of an antagonist. Subsequent docking studies using a homol. model of GPER showed unique docking poses between G-1 and CIFTA. While docking poses differed between the ligands, CIFTA exhibited more favorable distance, bond angle, and strain for hydrogen-bonding and hydrophobic interactions.
ACS Chemical Neuroscience published new progress about Biological ion transport, calcium. 51605-97-1 belongs to class bromides-buliding-blocks, and the molecular formula is C9H12BrN, Recommanded Product: 2-Bromo-4-isopropylaniline.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary