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Guvacine hydrochloride

رقم الكتالوجGC14659

Guvacine hydrochloride عبارة عن قلويد من جوز أريكا كاتشو ، يعمل كمثبط للناقل GABA ، وينتقل انتقائية متواضعة لناقلات GABA المستنسخة مع IC50s من 14 ميكرومتر (الإنسان GAT-1) ، 39 ميكرومتر (الفئران GAT-1) ، 58 ميكرومتر (الفئران GAT-2) ، 119 ميكرومتر (الإنسان GAT-3) ، 378 ميكرومتر (الجرذ GAT-3) ، و 1870 ميكرومتر (الإنسان BGT-3)

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Guvacine hydrochloride التركيب الكيميائي

Cas No.: 6027-91-4

الحجم السعر المخزون الكميّة
100mg
139٫00
Ship Within 7 Days

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).

Guvacine hydrochloride is a potent inhibitor of GABA transporter, dispalys modest selectivity forcloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3). Guvacine has low affinity at hBGT-1 (IC50 >1 mM)[1]. Guvacine hydrochloride is a potent inhibitor of GABA uptake, but does not inhibit sodium-independent GABA binding, and is weak or inactive as a GABA receptor agonist[2]. Guvacine inhibits the uptake GABA and β-alanine with IC50s of 23 ± 2 μM, 66 ± 11 μM in the Cat spinal cord, and 8 ± 1 μM, 123 ± 28 μM in the rat cerebral cortex, respectively[3].

References:
[1]. Borden LA, et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24.
[2]. Krogsgaard-Larsen P, et al. Structure-activity studies on the inhibition of GABA binding to rat brain membranes by muscimol and related compounds. J Neurochem. 1978 Jun;30(6):1377-82.
[3]. Lodge D, et al. Effects of the Areca nut constituents arecaidine and guvacine on the action of GABA in the cat central nervous system. Brain Res. 1977 Nov 18;136(3):513-22.

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