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BS43265
BIO-X

SR 95531 HBr

GABAA receptor antagonist that displaces [3H]-GABA in membranes of rat brain (Ki value 0.15 µM). Has greater affinity for GABAA than bicuculline (20-fold greater). Inhibits Cl- current induced by GABA, but not pentobarbitone. Low-affinity inhibitor of glycine receptors.

Technical Data

CAS No: 104104-50-9
Synonyms: 6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide; Gabazine
Product Code: BS43265
MDL No: MFCD00055135
Chemical Formula: C15H17N3O3·HBr
Molecular Weight: 368.23

Literature

References
  • Heaulme M et al (1986). Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site. Brain Res 384(2):224-31.
  • Uchida I et al (1996). The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons. Eur J Pharmacol 307(1):89-96.
  • Beato M et al (2007). The kinetics of inhibition of rat recombinant heteromeric alpha1beta glycine receptors by the low-affinity antagonist SR-95531. J Physiol 580(Pt 1):171-9.

Solubility

Stability

Datasheets


SR 95531 HBr

CAS No:
104104-50-9
Synonyms:
6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
Gabazine
MDL No:
MFCD00055135
Chemical Formula:
Molecular Weight:
368.23
Product Structure
References:
1. Heaulme M et al (1986). Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site. Brain Res 384(2):224-31.
2. Uchida I et al (1996). The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons. Eur J Pharmacol 307(1):89-96.
3. Beato M et al (2007). The kinetics of inhibition of rat recombinant heteromeric alpha1beta glycine receptors by the low-affinity antagonist SR-95531. J Physiol 580(Pt 1):171-9.

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