(-)-Bicuculline methiodide

mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail

Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.

Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody

Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay

SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.

Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
(-)-Bicuculline methiodide is an antagonist of γ-aminobutyric acid-A (GABAA) receptor, with IC50 value of 500 μM for GABA binding [1].
Three classes of GABA receptors have been characterized based on their pharmacology, namely GABAA, GABAB and GABAC receptors, among which GABAA and GABAC receptors are ligand-gated chloride (Cl-) channels. GABA receptors play important roles in central nervous system by responding to the inhibitory neurotransmitter GABA [2].
On synaptic membranes of chick cerebellum at birth, (-)-bicuculline methiodide acted as a less potent convulsant than (+)-Bicuculline methiodide which was more effective in displacing GABA binding, with an IC50 value of 10 μM [1]. In C. elegans, (-)-bicuculline methiodide at the concentration of 10 μM did not inhibit UNC-49B homomeric or UNC-49B/C heteromeric receptors which are UNC-49 subunits most closely related to the bicuculline- and benzodiazepine-insensitive RDL GABA receptors of insects. (-)-Bicuculline methiodide was used to confirm that the UNC-49 receptors were pharmacologically distinct from the mammalian GABAA receptors [3].
References:
[1]. Fiszer De Plazas S. Ontogenesis of GABA receptor sites in chick embryo cerebellum. Brain Research, 1982, 255(2): 263-275.
[2]. Goutman J D, Calvo D J. Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptor. British Journal of Pharmacology, 2004, 141(4): 717-727.
[3]. Bamber B A, Twyman R E, Jorgensen E M. Pharmacological characterization of the homomeric and heteromeric UNC-49 GABA receptors in C. elegans. British Journal of Pharmacology, 2003, 138(5): 883-893.
Physical Appearance | Yellow solid |
Storage | Store at RT |
M.Wt | 509.3 |
Cas No. | 40709-69-1 |
Formula | C21H20INO6 |
Solubility | <10.19mg/ml in H2O; <25.46mg/ml in DMSO |
Chemical Name | (S)-6,6-dimethyl-5-((R)-8-oxo-6,8-dihydro-[1,3]dioxolo[4,5-e]isobenzofuran-6-yl)-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-6-ium iodide |
SDF | Download SDF |
Canonical SMILES | O=C1O[[email protected]](C(C=C2)=C1C3=C2OCO3)[[email protected]](C4=C5)[N+](C)(C)CCC4=CC6=C5OCO6.[I-] |
Shipping Condition | Ship with blue ice, or upon other requests. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
