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Chemical Compound Review

Tocris-1262     4-[6-imino-3-(4- methoxyphenyl)pyridazin-1...

Synonyms: CHEMBL32503, SureCN5529434, CHEBI:147035, SPBio_002425, BPBio1_000771, ...
 
 
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Disease relevance of Tocris-1262

  • In contrast to bipolar cells, the ganglion cell GABA responses were strongly reduced by both bicuculline and SR95531 [1].
 

High impact information on Tocris-1262

  • In some experiments, bicuculline or SR95531 reversed a component of the GABA suppression of synaptic transmission [2].
  • In saturating (10 mM) GABA, the half-inhibitory concentrations of SR95531 (IC50) when coapplied with GABA to alpha1beta1gamma2S or alpha1beta1 receptors were 49 and 210 microM for the peak and 18 and 130 microM for the plateau current, respectively [3].
  • The dual binding-site model gives insights into the differential effects of GABA and SR95531 on the peak and plateau currents [3].
  • Dorsal root-evoked dorsal root potentials (DR-DRPs), reflecting depolarization of primary afferent terminals by endogenously released substances, were depressed by the GABAA receptor antagonist SR95531 and alpha,beta-meATP [4].
  • The high potency and efficacy of isoguvacine and ZAPA distinguishes RDLac homo-oligomers from bicuculline-insensitive vertebrate GABAC receptors, while the low potency of SR95531 and 3-APS distinguishes them from GABAA receptors [5].
 

Chemical compound and disease context of Tocris-1262

  • Diazoxide (700-1000 microM), another blocker of AMPA receptor desensitization, abolished directional selectivity in ON-OFF DS ganglion cells without the need of adding SR95531 to the bathing solution [6].
 

Anatomical context of Tocris-1262

  • We have compared the effects of microiontophoretic application of the GABA(A)-receptor antagonists bicuculline (BIC) and gabazine (SR95531) on responses to pure tones and to sinusoidally amplitude-modulated (AM) tones in cells recorded extracellularly from primary auditory cortex (AI) of Mongolian gerbils [7].
  • High affinity binding of [3H]gamma-aminobutyric acid (GABA) to neuronal membranes from different parts of cat visual cortex was tested for sensitivity to GABA(A) agonists isoguvacine and THIP, GABA(A) antagonist SR95531 and GABA(B) agonist baclofen [8].
 

Associations of Tocris-1262 with other chemical compounds

 

Analytical, diagnostic and therapeutic context of Tocris-1262

  • Microinjection of selective GABAA receptor antagonists bicuculline methiodide and SR95531 produced a significant increase in tail-flick (TF) latency [11].
  • In the grafts, GABAA receptor organization detected by autoradiography using [3H] labeled SR95531 was restored for more than 1 year after the graft [12].

References

  1. A novel GABA receptor on bipolar cell terminals in the tiger salamander retina. Lukasiewicz, P.D., Maple, B.R., Werblin, F.S. J. Neurosci. (1994) [Pubmed]
  2. A novel GABA receptor modulates synaptic transmission from bipolar to ganglion and amacrine cells in the tiger salamander retina. Lukasiewicz, P.D., Werblin, F.S. J. Neurosci. (1994) [Pubmed]
  3. The mechanism of SR95531 inhibition at GABA receptors examined in human alpha1beta1 and alpha1beta1gamma2S receptors. Lindquist, C.E., Laver, D.R., Birnir, B. J. Neurochem. (2005) [Pubmed]
  4. Localization and function of ATP and GABAA receptors expressed by nociceptors and other postnatal sensory neurons in rat. Labrakakis, C., Tong, C.K., Weissman, T., Torsney, C., MacDermott, A.B. J. Physiol. (Lond.) (2003) [Pubmed]
  5. Agonist pharmacology of two Drosophila GABA receptor splice variants. Hosie, A.M., Sattelle, D.B. Br. J. Pharmacol. (1996) [Pubmed]
  6. Responses of directionally selective retinal ganglion cells to activation of AMPA glutamate receptors. Jensen, R.J. Vis. Neurosci. (1999) [Pubmed]
  7. Differential effects of iontophoretic in vivo application of the GABA(A)-antagonists bicuculline and gabazine in sensory cortex. Kurt, S., Crook, J.M., Ohl, F.W., Scheich, H., Schulze, H. Hear. Res. (2006) [Pubmed]
  8. Neurochemical correlates of gamma-aminobutyrate (GABA) inhibition in cat visual cortex. Balcar, V.J., Dreher, B. Life Sci. (1990) [Pubmed]
  9. Characterization of the binding of [3H]CGP54626 to GABAB receptors in the male bullfrog (Rana catesbeiana). Asay, M.J., Boyd, S.K. Brain Res. (2006) [Pubmed]
  10. The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons. Uchida, I., Cestari, I.N., Yang, J. Eur. J. Pharmacol. (1996) [Pubmed]
  11. GABA-mediated inhibition in rostral ventromedial medulla: role in nociceptive modulation in the lightly anesthetized rat. Heinricher, M.M., Kaplan, H.J. Pain (1991) [Pubmed]
  12. Striatal grafts in infarct striatopallidum increase GABA release, reorganize GABAA receptor and improve water-maze learning in the rat. Aihara, N., Mizukawa, K., Koide, K., Mabe, H., Nishino, H. Brain Res. Bull. (1994) [Pubmed]
 
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