(+)-Bicuculline
Bicuculline is a neuromodulatory GABA-A receptor antagonist used to study regional variation of GABA receptors and the role of GABA-A receptors in motor disorders, pain, seizure, nociception, anxiety, and memory. Through its inhibition of GABA-A receptors, bicuculline potentiates activation at NMDA receptors and produces membrane depolarization, inhibiting K+ conductance and prolonging Ca2+-dependent action potentials in neurons. Specific rotation +130 (20 D, chloroform c=2)
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18829151
| Cas No. |
485-49-4 |
|---|---|
| Purity |
≥98% |
| Formula |
C20H17NO6 |
| Formula Wt. |
367.35 |
| IUPAC Name |
(6R)-6-[(5S)-6-methyl-7,8-dihydro-5H-[1,3]dioxolo[4,5-g]isoquinolin-5-yl]-6H-furo[3,4-g][1,3]benzodioxol-8-one |
| Appearance |
White to off white powder |
product targets : Filovirus inhibitors
Dela Peña IJ, Lee HL, Yoon SY, et al. The ethanol extract of Cirsium japonicum increased chloride ion influx through stimulating GABA(A) receptor in human neuroblastoma cells and exhibited anxiolytic-like effects in mice. Drug Discov Ther. 2013 Feb;7(1):18-23. PMID: 23524939.
Torkaman-Boutorabi A, Soltani S, Oryan S, et al. Involvement of the dorsal hippocampal GABA-A receptors in histamine-induced facilitation of memory in the Morris water maze. Pharmacol Biochem Behav. 2013 Apr;105:142-50. PMID: 23438692.
Ionov ID, Roslavtseva LA. Coadministration of bicuculline and NMDA induces paraplegia in the rat. Brain Res. 2012 Apr 27;1451:27-33. PMID: 22445063
Ji G, Neugebauer V. Pain-related deactivation of medial prefrontal cortical neurons involves mGluR1 and GABA(A) receptors. J Neurophysiol. 2011 Nov;106(5):2642-52. PMID: 21880942.
Costa LG, Doctor SV, Murphy SD. Antinociceptive and hypothermic effects of trimethyltin. Life Sci. 1982 Sep 13;31(11):1093-102. PMID: 6890611.
Heyer EJ, Nowak LM, Macdonald RL. Membrane depolarization and prolongation of calcium-dependent action potentials of mouse neurons in cell culture by two convulsants: bicuculline and penicillin. Brain Res. 1982 Jan 28;232(1):41-56. PMID: 7055710.
