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104104-50-9

104104-50-9 structure
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
  • 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

[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.

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