2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. (+)-Bicuculline methochloride

(+)-Bicuculline methobromide is a potent GABAA blocker. (+)-Bicuculline methobromide alters membrane properties and firing pattern. (+)-Bicuculline methobromide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. (+)-Bicuculline methobromide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.

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(+)-Bicuculline methochloride Chemical Structure

(+)-Bicuculline methochloride Chemical Structure

CAS No. : 53552-05-9

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(+)-Bicuculline methochloride Related Antibodies

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Description

(+)-Bicuculline methobromide is a potent GABAA blocker. (+)-Bicuculline methobromide alters membrane properties and firing pattern. (+)-Bicuculline methobromide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. (+)-Bicuculline methobromide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current[1].

IC50 & Target

GABAA[1]
In Vitro

(+)-Bicuculline methobromide (30 μM) promotes N-methyl-d-aspartate (NMDA) stimulation to facilitate burst firing in dopamine neurons[1].
Cluster discharges in the lateral habenular nucleus (LHb) of the antireward center are sufficient conditions for depression to occur. LHb neurons are usually classified into three types: silent, tonic-firing, burst-firing[2].

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

(+)-Bicuculline methochloride Related Antibodies
In Vivo

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

(-)-Bicuculline methobromide (0.6 nmol/rat) attenuates the antiallodynic effect of Neurotropin[3].
(-)-Bicuculline methobromide can be used in animal modeling to create epilepsy models and is capable of crossing the blood-brain barrier[4].

1. Induction of epilepsy[4]
Background
(-)-Bisculline methoromide can inhibit the synthesis and release of GABA, and weaken GABA's inhibition of neuronal activity in the SN reticular region (SNr), leading to epilepsy.
Specific Mmodeling Methods
Rat: Sprague-Dawley (SD) • male or female • 2 weeks old
Administration: 12.5, 25, 50 or 100 ng/0.25 μL • inject into SN or corpus striatum through bilateral catheter implantation
Note
(1) Dissolve (-)-Bicuculine methoromide in distilled water and administer at a volume of 0.25 μL.
(2) Simultaneously administer bilateral infusions at a rate of 0.25 μ L/min, and after the infusion is completed, insert the catheter in situ for an additional minute to prevent drug reflux.
(3) Due to the short-lived effect of (-) - Bicuculine methoromide in SN, rats were tested 5 minutes after completing the infusion.
Modeling Indicators
Behavioral observation: Shortened the latency period of epileptic seizures, causing stereotyped behaviors such as excessive sniffing or licking, chewing movements, head twitching, and slow or occasional circling.
Correlated Product(s): Muscimol (HY-N2313)
Opposite Product(s): /

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

Animal Model: Rat L5-SNL model[2]
Dosage: 0.6 nmol/rat
Administration: Intrathecal injection, 5 minutes before administration of Neurotropin (100 NU/kg, i.v.)
Result: Attenuated the antiallodynic effect of Neurotropin.
Molecular Weight

417.84

Formula

C21H20ClNO6
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.[Cl-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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(+)-Bicuculline methochloride Related Classifications

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Help & FAQs
  • 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.

Keywords:

(+)-Bicuculline methochloride53552-05-9GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorBicucullinemethobromideGABA(A)afterhyperpolarizationsAHPsneuronsInhibitorinhibitorinhibit

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