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Guvacine hydrochloride

Guvacine hydrochloride

Cat#
ALK-0030
Product Name
Guvacine hydrochloride
CAS No.
6027-91-4
Description
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).
Structural Formula
Guvacine hydrochloride
MW
163.6
MF
C6H10ClNO2
Purity
0.9973
Appearance
Solid
Solubility
H2O : 41.67 mg/mL(254.71 mM;Need ultrasonic) DMSO : 1 mg/mL(6.11 mM;ultrasonic and warming and heat to 80°C)
Source
Plants >Palmae > Areca catechuL.
Storage
-20℃, sealed storage, away from moisture and light
Shipping
Room temperature in continental US; may vary elsewhere.
SMILES
O=C(C1=CCCNC1)O.[H]Cl
In Vitro
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). 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. 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.
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