Overview
Alternative Name SR 95531
Lyophilized Powder yes
Source Synthetic
MW: 287.32
Purity: >98% (HPLC)
Effective concentration 0.1-10 µM.
Structure
Chemical name 4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl]butanoic acid.
Molecular formula C15H17N3O3.
CAS No.: 105538-73-6
PubChem CID 107896
Activity Gabazine is a competitive antagonist of the GABA(A) receptor, selectively inhibiting GABA-evoked currents (IC50 = 0.44 µM), but not currents evoked by pentobarbiton and etomidate1. It is also a low-affinity glycine receptor antagonist (KB = 191 µM)2.
References-Activity
- Uchida, I. et al. (1996) Eur. J. Pharmacol. 307, 89.
- Beato, M. et al. (2007) J. Physiol. 580, 171.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Soluble in methanol. Centrifuge all product preparations before use (10000 x g, 5 min).
Storage of solutions Up to three months at -20°C.
Our bioassay
Alomone Labs Gabazine inhibits GABA(A) receptors expressed in Xenopus oocytes.Time course of GABA(A) α1/β2 currents, activated by a continuous application (top dotted line) of 0.1 µM γ-Aminobutyric acid (#G-110), and inhibited by 1 µM Gabazine (#G-215), as indicated, while membrane potential was held at -60 mV.
Scientific background
Gabazine (SR-95531) is a specific, competitive and potent antagonist of GABA(A) receptors. The compound also blocks glycine receptors but with lower affinity. SR-95531 acts as an allosteric inhibitor of GABA(A) receptor channel opening1,2 and blocks GABA-evoked currents with an IC50 of 0.44 µM1. When SR 95531 was administered intravenously it was shown to cause seizures in mice3.
GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate the GABA action, a major inhibitory neurotransmitter, throughout the central nervous system (CNS) and play an important role in inhibiting cell excitation in the CNS. The GABA(A) receptor is considered to be a major target of anti-seizure drugs4,5.
Target GABA(A), Glycine receptors
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
Citations
