CAS NO: | 40709-69-1 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
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 |
Canonical SMILES | O=C1O[C@H](C(C=C2)=C1C3=C2OCO3)[C@H](C4=C5)[N+](C)(C)CCC4=CC6=C5OCO6.[I-] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
(-)-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]. InC. 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 inC. elegans. British Journal of Pharmacology, 2003, 138(5): 883-893.