Bicuculline

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Bicuculline
Clinical data
ATC code
  • none
Identifiers
  • (6R)-6-[(5S)-6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinolin-5-yl]furo[3,4-e][1,3]benzodioxol-8(6H)-one
JSmol)
Melting point215 °C (419 °F)
  • O=C1O[C@H](c3c1c2OCOc2cc3)[C@@H]5c4cc6OCOc6cc4CCN5C
  • InChI=1S/C20H17NO6/c1-21-5-4-10-6-14-15(25-8-24-14)7-12(10)17(21)18-11-2-3-13-19(26-9-23-13)16(11)20(22)27-18/h2-3,6-7,17-18H,4-5,8-9H2,1H3/t17-,18+/m0/s1 checkY
  • Key:IYGYMKDQCDOMRE-ZWKOTPCHSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Bicuculline is a

GABAA receptors.[1] It was originally identified in 1932 in plant alkaloid extracts[2] and has been isolated from Dicentra cucullaria, Adlumia fungosa, and several Corydalis species (all in subfamily Fumarioideae, previously known as family Fumariaceae). Since it blocks the inhibitory action of GABA receptors, the action of bicuculline mimics epilepsy; it also causes convulsions. This property is utilized in laboratories around the world in the in vitro study of epilepsy, generally in hippocampal or cortical neurons in prepared brain slices from rodents. This compound is also routinely used to isolate glutamatergic
(excitatory amino acid) receptor function.

The action of bicuculline is primarily on the

z-drugs, and related anxiolytic
drugs.

The half-maximal inhibitory concentration (IC50) of bicuculline on GABAA receptors is 3 μM.[citation needed]

In addition to being a potent GABAA receptor antagonist, bicuculline can be used to block Ca2+-activated potassium channels.[3]

Sensitivity to bicuculline is defined by

IUPHAR
as a major criterion in the definition of GABAA receptors 

See also

References

  1. PMID 23425285
    .
  2. doi:10.1139/cjr32-078
    .
  3. S2CID 7033568
    .
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