Bicuculline methiodide

Names

[ Name ]:
Bicuculline methiodide

[Synonym ]:
bicuculine methiodide

Biological Activity

[Description]:

Bicuculline methiodide is a potent GABA(A) receptors blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[In Vitro]

Bicuculline methiodide (30 μM) 促进 N-甲基-d-天冬氨酸 (NMDA) 刺激，促进多巴胺神经元的爆发性放电[1]。研究表明，反奖励中枢外侧缰核（LHb）的簇状放电是抑郁症发生的充分条件。LHb神经元常分为三类：沉默型（silent）, 强直放电型（tonic-firing），簇状放电型（burst-firing）[2]。

[References]

[1]. Johnson SW, et al. Bicuculline methiodide potentiates NMDA-dependent burst firing in rat dopamine neurons by blocking apamin-sensitive Ca2+-activated K+ currents. Neurosci Lett. 1997 Aug 1;231(1):13-6.

[2]. Yang Y, et al. Ketamine blocks bursting in the lateral habenula to rapidly relieve depression[J]. Nature, 2018, 554(7692): 317-322.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₂₀INO₆

[ Molecular Weight ]:
509.29

[ Exact Mass ]:
509.03400

[ PSA ]:
63.22000

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Transparent and flexible low noise graphene electrodes for simultaneous electrophysiology and neuroimaging.

Nat. Commun. 5 , 5259, (2014)

Calcium imaging is a versatile experimental approach capable of resolving single neurons with single-cell spatial resolution in the brain. Electrophysiological recordings provide high temporal, but li...

Simultaneous monitoring of presynaptic transmitter release and postsynaptic receptor trafficking reveals an enhancement of presynaptic activity in metabotropic glutamate receptor-mediated long-term depression.

J. Neurosci. 33(13) , 5867-77, (2013)

Although the contribution of postsynaptic mechanisms to long-term synaptic plasticity has been studied extensively, understanding the contribution of presynaptic modifications to this process lags beh...

Effects of nitric oxide synthase blockade on dorsal vagal stimulation-induced pancreatic insulin secretion

Brain Res. 1394 , 62-70, (2011)

We and others have previously shown that the dorsal motor nucleus of the vagus (DMV) is involved in regulation of pancreatic exocrine secretion. Many pancreatic preganglionic neurons within the DMV ar...