Bicuculline

Bicuculline ((+) -Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM) . Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP) . Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice[1][2][3][4].

Product Specifications

CAS Number

[485-49-4]

Product Name Alternative

(+) -Bicuculline

UNSPSC

12352005

Hazard Statement

H300, H311+H331, H400

Target

GABA Receptor

Type

Natural Products

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/__addition__-Bicuculline.html

Purity

99.97

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

Smiles

O=C1O[C@@H]([C@H]2N(C)CCC3=C2C=C(OCO4)C4=C3)C5=CC=C(OCO6)C6=C51

Molecular Formula

C20H17NO6

Molecular Weight

367.35

Precautions

H300, H311+H331, H400

References & Citations

[1]Johnston GA. Advantages of an antagonist: bicuculline and other GABA antagonists. Br J Pharmacol. 2013;169 (2) :328-336.|[2]Khawaled R, et al. Bicuculline block of small-conductance calcium-activated potassium channels. Pflugers Arch. 1999;438 (3) :314-321.|[3]Huang SH, et al. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA (A) receptors. Eur J Pharmacol. 2003;464 (1) :1-8.|[4]Baram TZ, et al. Bicuculline induced seizures in infant rats: ontogeny of behavioral and electrocortical phenomena. Brain Res Dev Brain Res. 1990 Dec 15;57 (2) :291-5. |[5]P Gass, et al. Induction of immediate early gene encoded proteins in the rat hippocampus after bicuculline-induced seizures: differential expression of KROX-24, FOS and JUN proteins. Neuroscience. 1992;48 (2) :315-24. |[6]Jianshe Ma, et al. Determination of bicuculline in rat plasma by liquid chromatography mass spectrometry and its application in a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Mar 15:953-954:143-6.