CAS 104104-50-9|SR-95531
| Common Name | SR-95531 | ||
|---|---|---|---|
| CAS Number | 104104-50-9 | Molecular Weight | 368.226 |
| Density | / | Boiling Point | 474.4ºC at 760 mmHg |
| Molecular Formula | C15H18BrN3O3 | Melting Point | 200 ºC (ethanol ) |
| MSDS | USA | Flash Point | 240.7ºC |
Names
| Name | 2-(3-carboxypropyl)-3-amino-6-(4-methoxyphenyl)pyridazinium bromide |
|---|---|
| Synonym | More Synonyms |
SR-95531 BiologicalActivity
| Description | Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor. |
|---|---|
| Related Catalog | Signaling Pathways >>Membrane Transporter/Ion Channel >>GABA ReceptorSignaling Pathways >>Neuronal Signaling >>GABA ReceptorResearch Areas >>Neurological Disease |
| Target | 0.2 μM (GABA receptor)[1]. |
| In Vitro | Both bicuculline and Gabazine (SR 95531) have been characterized as competitive inhibitors of GABA binding to the GABAA receptor. Gabazine is more potent than bicuculline at blocking currents elicited by GABA, with an IC50 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[1]. |
| References | [1]. Ueno S, et al. Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J Neurosci. 1997 Jan 15;17(2):625-34. |
Chemical & Physical Properties
| Boiling Point | 474.4ºC at 760 mmHg |
|---|---|
| Melting Point | 200 ºC (ethanol ) |
| Molecular Formula | C15H18BrN3O3 |
| Molecular Weight | 368.226 |
| Flash Point | 240.7ºC |
| Exact Mass | 367.053131 |
| PSA | 89.32000 |
| Appearance of Characters | solid white |
| Vapour Pressure | 8.33E-10mmHg at 25°C |
| InChIKey | GFZHNFOGCMEYTA-UHFFFAOYSA-N |
| SMILES | Br.COc1ccc(-c2ccc(=N)n(CCCC(=O)O)n2)cc1 |
| Storage condition | Store at RT |
| Water Solubility | DMSO: 30 mg/mL |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
Articles50
More Articles| Effect of gabazine on sensory stimulation train evoked response in mouse cerebellar Purkinje cells. Pharmazie 70(2) , 129-34, (2015) Cerebellar Purkinje cells (PCs) respond to sensory stimulation via climbing fiber and mossy fiber-granule cell pathways, and generate motor-related outputs according to internal rules of integration a... | |
| A hard-wired priority map in the superior colliculus shaped by asymmetric inhibitory circuitry. J. Neurophysiol. 114 , 662-76, (2015) The mammalian superior colliculus (SC) is a laminar midbrain structure that translates visual signals into commands to shift the focus of attention and gaze. The SC plays an integral role in selecting... | |
| Neurotransmission to parasympathetic cardiac vagal neurons in the brain stem is altered with left ventricular hypertrophy-induced heart failure. Am. J. Physiol. Heart Circ. Physiol. 309 , H1281-7, (2015) Hypertension, cardiac hypertrophy, and heart failure (HF) are widespread and debilitating cardiovascular diseases that affect nearly 23 million people worldwide. A distinctive hallmark of these cardio... |
Synonyms
| MFCD00055135 |
| 4-[6-Imino-3-(4-methoxyphenyl)pyridazin-1(6H)-yl]butanoic acid hydrobromide (1:1) |
| Pyridazinium, 6-amino-1-(3-carboxypropyl)-3-(4-methoxyphenyl)-, bromide (1:1) |
| 6-Amino-1-(3-carboxypropyl)-3-(4-methoxyphenyl)pyridazin-1-ium bromide |
| 2-(3-carboxypropyl)-6-(4-methoxyphenyl)pyridazin-3(2H)-iminium bromide |
| Gabazine |
| SR-95531 |
