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  4. Bicuculline methobromide

Bicuculline methobromide  (Synonyms: (+)-Bicuculline methobromide; d-Bicuculline methobromide)

Cat. No.: HY-100783B
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Bicuculline methobromide is a selective GABAA Receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders.

For research use only. We do not sell to patients.

Bicuculline methobromide Chemical Structure

Bicuculline methobromide Chemical Structure

CAS No. : 66016-70-4

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Description

Bicuculline methobromide is a selective GABAA Receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders[1][2].

In Vitro

Bicuculline methobromide (1 μM and 3 μM) attains the maximal response of GABA. Bicuculline methobromide appears to shift the dose–response curves of GABA in parallel to the right without decreasing GABA maximal response, suggesting that it is a competitive antagonist at human α1β2γ2L GABAA receptors expressed in Xenopus oocytes[3].
Bicuculline methobromide (1-100 μM; 2 min; applied as outside-out patches) potently blocks both Apamin (HY-P0256)-sensitive small-conductance calcium-activated potassium channels (SK2) currents and Apamin-insensitive SK1 currents in Xenopus oocytes[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bicuculline methobromide (subcutaneous injection, 1.25-3 mg/kg) can cause clonus-tonic convulsions in a dose-dependent manner in mice and these convulsions are enhanced by injection of the μ-opioid agonist morphine[1].
Bicuculline methobromide (subcutaneous injection, 1.5-3.2 mg/kg) induces male Swiss S mice generalized seizures with a CD50 (convulsant dose) of 2.2 mg/kg for clonus and CD50 of 2.4 mg/kg for tonus. Seizures induced by Bicuculline at the dose of 3.2 mg/kg can be blocked by pretreatment (i.p.) with the NMDA antagonists MK-801, CPP and CGS 19755[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

462.29

Formula

C21H20BrNO6

CAS No.
SMILES

C[N+]1([C@](C2=C(CC1)C=C3C(OCO3)=C2)([H])[C@@]4([H])C5=C(C6=C(OCO6)C=C5)C(O4)=O)C.[Br-]

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Bicuculline methobromide
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