Molecular Formula | C15H18BrN3O3 |
Molar Mass | 368.23 |
Melting Point | 200 °C(Solv: ethanol (64-17-5)) |
Solubility | Soluble in DMSO |
Appearance | solid |
Color | white |
Storage Condition | Store at RT |
Use | Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor. |
In vitro study | Both bicuculline and Gabazine (SR 95531) have been characterized as competitive inhibitors of GABA binding to the GABA A receptor. Gabazine is more potent than bicuculline at blocking currents elicited by GABA, with an IC 50 for currents elicited by 3 μM GABA of ~0.2 μM and a Hill coefficient of 1.0. Gabazine reduces the currents elicited by 10 μM alphaxalone by ~30%, for responses of receptors containing wildtype β2 subunits. The concentration of Gabazine requires producing half the maximal block is ~0.2 μM. Gabazine also could only produce a partial block of currents gated by 300 μM pentobarbital. The maximal reduction, again, is ~30%, and the concentration of Gabazine required to produce half the maximal block is ~0.15 μM. |
WGK Germany | 3 |
Reference Show more | 1: Müller S, Guli X, Hey J, Einsle A, Pfanz D, Sudmann V, Kirschstein T, Köhling R. Acute epileptiform activity induced by gabazine involves proteasomal rather than lysosomal degradation of K(Ca)2.2 channels. Neurobiol Dis. 2018 Apr;112:79-84. doi: 10.1016/j.nbd.2018.01.005. Epub 2018 Jan 9. PubMed PMID: 29330041. 2: Eroli F, Loonen ICM, van den Maagdenberg AMJM, Tolner EA, Nistri A. Differential neuromodulatory role of endocannabinoids in the rodent trigeminal sensory ganglion and cerebral cortex relevant to pain processing. Neuropharmacology. 2018 Mar 15;131:39-50. doi: 10.1016/j.neuropharm.2017.12.013. Epub 2017 Dec 7. PubMed PMID: 29225040. 3: Megat S, Shiers S, Moy JK, Barragan-Iglesias P, Pradhan G, Seal RP, Dussor G, Price TJ. A Critical Role for Dopamine D5 Receptors in Pain Chronicity in Male Mice. J Neurosci. 2018 Jan 10;38(2):379-397. doi: 10.1523/JNEUROSCI.2110-17.2017. Epub 2017 Nov 22. PubMed PMID: 29167404; PubMed Central PMCID: PMC5761615. 4: Cattano C, Calò A, Di Franco A, Firmamento R, Quattrocchi F, Sdiri K, Guidetti P, Milazzo M. Ocean acidification does not impair predator recognition but increases juvenile growth in a temperate wrasse off CO(2) seeps. Mar Environ Res. 2017 Dec;132:33-40. doi: 10.1016/j.marenvres.2017.10.013. Epub 2017 Oct 24. PubMed PMID: 29110937. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.716 ml | 13.578 ml | 27.157 ml |
5 mM | 0.543 ml | 2.716 ml | 5.431 ml |
10 mM | 0.272 ml | 1.358 ml | 2.716 ml |
5 mM | 0.054 ml | 0.272 ml | 0.543 ml |
biological activity | Gabazine is a selective competitive antagonist of GABAA receptor, and its IC50 value to GABA receptor is ~ 0.2 μM. |
target | 0.2 μM (GABA receptor). |
in vitro study | both bicuculline and Gabazine (SR 95531) have been characterized as competitive inhibitors of GABA binding to the GABA A receptor. Gabazine is more potent than bicuculline at blocking currents elicited by GABA, with an IC 50 for currents elicited by 3 μM GABA of ~ 0.2 μM and a Hill coefficient of 1.0. Gabazine reduces the currents elicited by 10 μM alphaxalone by ~ 30%, for responses of receptors containing wildtype β2 subunits. The concentration of Gabazine requires producing half the maximal block is ~ 0.2 μ m. Gabazine also could only produce a partial block of currents gated by 300 μ m pentobarbital. The maximal reduction, again, is ~ 30%, and the concentration of Gabazine required to produce half the maximal block is ~ 0.15 μM. |