Methiodide 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.
Freebase, methochloride and methobromide salts also available.
The GABAA receptor antagonist bicuculline is commonly used to reduce levels of inhibition by blocking the actions of the neurotransmitter GABA. Bicuculline is commonly used at concentrations of 100 μM and above.
Bicuculline methiodide from Hello Bio reduces both spontaneous inhibitory post synaptic currents (IPSC) and evoked IPSCs (see Fig 1 above). It was effective at concentrations of 1 mM with complete receptor blockade at 100 μM.
#Protocol 1: Evoked and spontaneous inhibitory post synaptic currents (IPSCs)
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