104104-50-9
104104-50-9 structure
- Name: SR-95531
- Chemical Name: 2-(3-carboxypropyl)-3-amino-6-(4-methoxyphenyl)pyridazinium bromide
- CAS Number: 104104-50-9
- Molecular Formula: C15H18BrN3O3
- Molecular Weight: 368.226
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
- Create Date: 2018-08-04 11:41:16
- Modify Date: 2024-01-06 14:02:15
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Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
| Name | 2-(3-carboxypropyl)-3-amino-6-(4-methoxyphenyl)pyridazinium bromide |
|---|---|
| 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 |
| Description | Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor. |
|---|---|
| Related Catalog | |
| 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 |
| 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 | solid white |
| Vapour Pressure | 8.33E-10mmHg at 25°C |
| Storage condition | Store at RT |
| Water Solubility | DMSO: 30 mg/mL |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |