Famiraprinium (also known as SR-95103) is a GABAA receptor antagonist used in scientific research.[1]

Famiraprinium
Names
IUPAC name
4-(6-Imino-5-methyl-3-phenylpyridazin-1-yl)butanoic acid
Other names
SR-95103
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
UNII
  • InChI=1S/C15H17N3O2/c1-11-10-13(12-6-3-2-4-7-12)17-18(15(11)16)9-5-8-14(19)20/h2-4,6-7,10,16H,5,8-9H2,1H3,(H,19,20)
    Key: LLZVAIDABZBAGE-UHFFFAOYSA-N
  • HCl: InChI=1S/C15H17N3O2.ClH/c1-11-10-13(12-6-3-2-4-7-12)17-18(15(11)16)9-5-8-14(19)20;/h2-4,6-7,10,16H,5,8-9H2,1H3,(H,19,20);1H
    Key: MDCYBLVSLOPFAZ-UHFFFAOYSA-N
  • CC1=CC(=NN(C1=N)CCCC(=O)O)C2=CC=CC=C2
  • HCl: CC1=CC(=NN(C1=N)CCCC(=O)O)C2=CC=CC=C2.Cl
Properties
C15H17N3O2
Molar mass 271.320 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).

It antagonizes certain GABAA receptors with an inhibition constant of 2.2 μM.[2]

Effects

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Like other GABA antagonists, it triggers epilepsy-like symptoms. These effects can be antagonized by GABAA agonists like muscimol, proving it is an antagonist.[3]

References

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  1. ^ Schmitt, P.; Di Scala, G.; Brandao, M. L.; Karli, P. (1985-11-05). "Behavioral effects of microinjections of SR 95103, a new GABA-A antagonist, into the medial hypothalamus or the mesencephalic central gray". European Journal of Pharmacology. 117 (2): 149–158. doi:10.1016/0014-2999(85)90599-0. ISSN 0014-2999. PMID 3000802.
  2. ^ Chambon, J. P.; Feltz, P.; Heaulme, M.; Restle, S.; Schlichter, R.; Biziere, K.; Wermuth, C. G. (March 1985). "An arylaminopyridazine derivative of gamma-aminobutyric acid (GABA) is a selective and competitive antagonist at the GABAA receptor site". Proceedings of the National Academy of Sciences of the United States of America. 82 (6): 1832–1836. doi:10.1073/pnas.82.6.1832. ISSN 0027-8424. PMC 397367. PMID 2984669.
  3. ^ Santucci, V.; Fournier, M.; Chambon, J. P.; Biziere, K. (1985-08-15). "Electroencephalographic study of SR 95103, a GABAA antagonist: interaction with inhibitory amino acids and muscimol". European Journal of Pharmacology. 114 (2): 219–222. doi:10.1016/0014-2999(85)90630-2. ISSN 0014-2999. PMID 2995080.