SR-95531

Modify Date: 2024-01-06 14:02:15

SR-95531 Structure
SR-95531 structure
Common Name SR-95531
CAS Number 104104-50-9 Molecular Weight 368.226
Density N/A Boiling Point 474.4ºC at 760 mmHg
Molecular Formula C15H18BrN3O3 Melting Point 200 ºC (ethanol )
MSDS USA Flash Point 240.7ºC

 Use of SR-95531


Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.

 Names

Name 2-(3-carboxypropyl)-3-amino-6-(4-methoxyphenyl)pyridazinium bromide
Synonym More Synonyms

 SR-95531 Biological Activity

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.

 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
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
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Price: ¥660/10 mM * 1 mL in DMSO

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