WebSep 10, 2024 · GlyT2 inhibitors in the series, inhibiting GlyT2 with IC 50 concentrations of 25.5 nM and 54.6 nM, respectively (Table 1). Interestingly, when the head group is converted to the D-configuration the Lys analogue ( 18ω9-D-Lys) retains potency while the Trp analogue ( 18ω9-D-Trp) is inactive (Table 1) (Mostyn, Wilson, et al., 2024). WebSep 1, 2016 · ALX1393 is a potent GlyT2 inhibitor with an IC 50 of 10–25 nM and an approximate 200-fold selectivity for GlyT2 over GlyT1 (Caulfield et al., 2001, Mingorance-Le Meur et al., 2013) (Fig. 2).ALX1393 has been studied in animal models of pain using either intravenous or intrathecal injections (Xu et al., 2005, Morita et al., 2008, Haranishi et al., …
Structural Determinants of the Neuronal Glycine Transporter 2 for the ...
WebOct 1, 2012 · This study also further demonstrated that additional suppression of GlyT2 by selective GlyT2 inhibitors in the spinal cord is effective in reducing CYP-induced … WebThe present work has provided insight into the structural features of GlyT2 inhibitors that will be important for the future design of novel inhibitors of GlyT2. The structural basis of inhibitor activity reported here may provide insights that are applicable to the broader development of new compounds that could target homologous ... smith and lockwood rockmart ga
Christopher Cioffi Faculty
WebMay 28, 2016 · ALX1393 is a potent, complete GlyT2 blocker which causes prolonged inhibition of transport. When administered to mice suffering from chronic pain by direct … WebSep 24, 2008 · At inhibitory synapses, glycine and GABA are accumulated into synaptic vesicles by the same vesicular transporter VGAT/VIAAT (vesicular GABA transporter/vesicular inhibitory amino acid transporter), enabling a continuum of glycine, GABA, and mixed phenotypes. Many fundamental aspects of the presynaptic … WebMar 26, 2013 · The specific transport mediated by GlyT1 or GlyT2 was calculated as the difference between the [3 H]glycine uptake in the absence (total transport) and in the presence of the GlyT1 inhibitor, Org 24598 (10 μM), or GlyT2 inhibitors, ALX 1393 (200 nM) and amoxapine (1 μM), except when otherwise indicated. smith and lockwood rockmart