Bicuculline
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Bicuculline
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| Systematic (IUPAC) name | |
| Bicuculline | |
| Identifiers | |
| CAS number | 485-49-4 |
| ATC code | ? |
| PubChem | 10237 |
| Chemical data | |
| Formula | C20H17NO6 |
| Mol. weight | 367.352 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Bicuculline (BIC) is a light-sensitive competitive antagonist of GABAA receptors. Since it blocks the inhibitory action of GABA receptors, the action of bicuculline mimics epilepsy. This property is utilised in laboratories across the world in the in vitro study of epilepsy, generally in cortical neurons in prepared brain slices from rodents.(for instance in paired-pulse experiments)
The action of bicuculline is primarily on the ionotropic GABAA receptor, which is a ligand-gated ion channel concerned chiefly with the passing of chloride ions across the cell membrane, thus promoting an inhibitory influence on the target neuron. This receptor is the major target for benzodiazepines and related anxiolytic drugs.
The half-maximal (EC50) effect of bicuculline on GABAA receptors is 3 μM.
In addition to being a potent GABAA receptor antagonist, bicuculine can be used to block Ca2+-activated potassium channels.
Sensitivity to bicuculline is defined by IUPHAR as a major criterion in the definition of GABAA receptors - however in recent years a new class of ionotropic GABA receptor, defined variously as GABAA0R or GABAC has been characterised, which is insensitive to both benzodiazepines and bicuculline.
A water soluble form of bicuculline, bicuculline methiodide, is soluble in water to a concentration of 10 mg/mL.
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