GUVACINE HYDROCHLORIDE Property

Melting point:

316 °C (decomp)

storage temp. 

Inert atmosphere,Room Temperature

solubility 

H2O: soluble

form 

solid

color 

white

Safety

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36

WGK Germany 

3

HazardClass 

IRRITANT

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

GUVACINE HYDROCHLORIDE Chemical Properties,Usage,Production

Chemical Properties

Beige Solid

Uses

Guvacine Hydrochloride is a GABA uptake inhibitor (hGABA T-1, rGABA T-2, hGABA T-3 and hBGT-1) (1,2,3). Gamma-Aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the mammalian brain (4). Guvacine Hydrochloride may be useful for treating neuropsychiatric disorders.

Uses

Guvacine Hydrochloride is a GABA uptake inhibitor and it is used for the treatment of neurodegenerative diseases.

Biological Activity

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).

in vitro

Guvacine hydrochloride is a potent inhibitor of GABA transporter, 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 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.