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Chemical Compound Review:

AG-J-64235 4-(6-imino-5-methyl-3-phenyl- pyridazin-1...

Synonyms: ACMC-20mbvy, SR-95103, CTK0H6570, AR-1F9272, AC1L2PI8, ...

This record was replaced with 125959.

Schmitt, P. et al., Santucci, V. et al., Bonaventure, N. et al., Worms, P. et al., Chambon, J.P. et al.

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High impact information on 4-(6-imino-5-methyl-3-phenyl-pyridazin-1-yl)butanoic acid

SR 95103 displaced [3H]GABA from rat brain membranes with an apparent Ki of 2.2 microM and a Hill number near 1 [1].
Two pyridazinyl GABA derivatives, SR 95103 and SR 42641 have recently been described as selective GABAA receptor antagonists [2].
When GABA antagonists (picrotoxin, bicuculline methiodide and SR 95103) were intravitreally injected in the frog, they increased the number of spikes of transient retinal ganglion cells, as well as the duration of the response [3].
When injected into the medial hypothalamus (MH) or into the dorsal part of the mesencephalic central gray (CG), SR 95103 produced a dose-dependent behavioral activation together with jumps [4].
Behavioral effects of microinjections of SR 95103, a new GABA-A antagonist, into the medial hypothalamus or the mesencephalic central gray [4].

Anatomical context of 4-(6-imino-5-methyl-3-phenyl-pyridazin-1-yl)butanoic acid

When injected into the CG or into the deep layers of the superior colliculus, SR 95103 proved to affect the rat's reactivity to tactile stimuli as evidenced by ipsilateral 'neglect' combined with contralateral hyperreactivity expressed as withdrawal reactions and jumping [4].

Associations of 4-(6-imino-5-methyl-3-phenyl-pyridazin-1-yl)butanoic acid with other chemical compounds

In this study, the electroencephalographic (EEG) effects of SR 95103 were investigated as well as its central interaction with inhibitory amino acids and muscimol [5].

Analytical, diagnostic and therapeutic context of 4-(6-imino-5-methyl-3-phenyl-pyridazin-1-yl)butanoic acid

The behavioral effects of unilateral microinjections of SR 95103, a new GABA-A receptor antagonist, into periventricular structures were studied [4].
These results suggest that the EEG effects of SR 95103 are due to the specific GABAA antagonistic properties of this compound [5].

References

An arylaminopyridazine derivative of gamma-aminobutyric acid (GABA) is a selective and competitive antagonist at the GABAA receptor site. Chambon, J.P., Feltz, P., Heaulme, M., Restle, S., Schlichter, R., Biziere, K., Wermuth, C.G. Proc. Natl. Acad. Sci. U.S.A. (1985) [Pubmed]
Behavioural evidence for a selective GABA-A antagonistic activity of SR 95103 and SR 42641 after intrastriatal injection in mice. Worms, P., Chambon, J.P., Biziere, K. Eur. J. Pharmacol. (1987) [Pubmed]
Anisotropic inhibition in the receptive field surround of the frog retinal ganglion cells, evidenced by bicuculline and SR 95103, a new GABA antagonist. Bonaventure, N., Wioland, N., Jardon, B. Eur. J. Pharmacol. (1986) [Pubmed]
Behavioral effects of microinjections of SR 95103, a new GABA-A antagonist, into the medial hypothalamus or the mesencephalic central gray. Schmitt, P., Di Scala, G., Brandao, M.L., Karli, P. Eur. J. Pharmacol. (1985) [Pubmed]
Electroencephalographic study of SR 95103, a GABAA antagonist: interaction with inhibitory amino acids and muscimol. Santucci, V., Fournier, M., Chambon, J.P., Biziere, K. Eur. J. Pharmacol. (1985) [Pubmed]

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