Prototypic, competitive GABAA receptor antagonist
Methochloride salt form of (+)-bicuculline.
Prototypic, competitive GABAA receptor antagonist which displaces GABA from the agonist binding site to prevent receptor activation.
Also acts as a negative allosteric inhibitor of channel opening to inhibit GABAA receptor activation by anaesthetic agents.
Additionally shows activity at SK calcium-activated potassium channels, nicotinic acetylcholine receptors and acetylcholinesterase.
Reversibly and competitively blocks GABAA receptor mediated currents. Widely used to isolate glutamate receptor mediated EPSCs (excitatory postsynaptic potentials).
Shows convulsant action and induces epilepsy.
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[R-(R*,S*)]-5-(6,8-Dihydro-8-oxofuro[3,4-e]-1,3-benzodioxol-6-yl)-5,6,7,8-tetrahydro- 6,6-dimethyl-1,3-dioxolo[4,5-g]isoquinolinium chloride
The GABAA receptor antagonist bicuculline is commonly used to reduce levels of inhibition by blocking the actions of the neurotransmitter GABA. It is commonly used at concentrations of 100 μM and above. Bicuculline methochloride from Hello Bio reduces both spontaneous inhibitory post synaptic currents (IPSC) and evoked IPSCs (see Fig 1 above). It was effective at 1 μM with complete receptor blockade at 100 μM.
#Protocol 1: Evoked and spontaneous inhibitory post synaptic currents (IPSCs)
- Whole cell voltage clamp recordings were obtained from layer V neurons of the mouse prelimbic cortex brain slice.
- A stimulating electrode was placed in layers II/III and IPSCs were evoked by a single square (150 μs) pulse every 10 sec at a stimulus intensity that gave a reliable IPSC.
- IPSCs were evoked at a range of neuron holding voltages to measure the reversal potential of the current to ensure it was GABAergic.
- Neurons were held at 0mV and IPSCs continuously stimulated and recorded in response to 5 min applications of varying concentrations of Bicuculline methochloride until complete receptor inhibition.
- Spontaneous IPSCs were recorded before and after addition of Bicuculline methochloride by holding the neuron at 0mV and recording for 10 sec.
- All recordings for IPSCs were made in the presence of AMPAR antagonists.
Storing and Using Your Product
Soluble in water (100mM)
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
References for (-)-Bicuculline methochloride
Advantages of an antagonist: bicuculline and other GABA antagonists.Johnston GA (2013) Br J Pharmacol 169(2) : 328-36.PubMedID: 23425285
Differential effects of iontophoretic in vivo application of the GABA(A)-antagonists bicuculline and gabazine in sensory cortex.Kurt S et al (2006) Hear Res 212(1-2) : 224-35.PubMedID: 16442250
[Bicuculline inhibits airway remodeling in a murine model of chronic asthma].Zhu T et al (2010) Nan Fang Yi Ke Da Xue Xue Bao 30(4) : 842-6.PubMedID: 20423862
Neurotoxicity of propofol on rat hypoglossal motoneurons in vitro.Monni et al(2017) Neurosci Lett S0304-3940(17) : 30531-1PubMedID: 28676256
Propofol protects rat hypoglossal motoneurons in an in vitro model of excitotoxicity by boosting GABAergic inhibition and reducing oxidative stressGhezzi et al (2017) Neuroscience pii: S0306-4522(17)30747-9. : doi: 10.1016/j.neuroscience.201PubMedID: 29069620
Limiting habenular hyperactivity ameliorates maternal separation-driven depressive-like symptoms.Tchenio et al(2017) Nat Commun 8(1) : 1135PubMedID: 29074844
Acetylcholine release inhibits distinct excitatory inputs onto hippocampal CA1 pyramidal neurons via different cellular and network mechanismsMcQuiston et al (2019) bioRxiv : doi: http://dx.doi.org/10.1101/5
Reviews & Product Guides
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I purchase (-)-Bicuculline methochloride from Hello Bio and use it in our experiments to block GABAA receptors