Tiagabine-d6

Tiagabine-d6 (NO050328-d6) is deuterium labeled Tiagabine. Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively[1].

1217672-34-8

NO050328-d6; NO328-d6; TGB-d6

12352005

GABA Receptor; Isotope-Labeled Compounds

Membrane Transporter/Ion Channel; Neuronal Signaling; Others

Neuroscience-Neuromodulation

Neurological Disease

OC([C@H](CCC1)CN1CC/C=C(C2=C(C=CS2)C([2H])([2H])[2H])\C3=C(C=CS3)C([2H])([2H])[2H])=O

C20H19D6NO2S2

381.58

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Braestrup C, et al. (R) -N-[4,4-bis (3-methyl-2-thienyl) but-3-en-1-yl]nipecotic acid binds with high affinity to the brain gamma-aminobutyric acid uptake carrier. J Neurochem. 1990 Feb;54 (2) :639-47.|[3]Sheehan, D.V., et al., An open-label study of tiagabine in panic disorder. Psychopharmacol Bull, 2007. 40 (3) : p. 32-40.|[4]Henjum, S. and B. Hassel, High-affinity GABA uptake and GABA-metabolizing enzymes in pig forebrain white matter: a quantitative study. Neurochem Int, 2007. 50 (2) : p. 365-70.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-B0696S/

Isotope-Labeled Compounds

No Development Reported