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(+)-BICUCULLINE METHOCHLORIDE

(+)-BICUCULLINE METHOCHLORIDE Structure
(+)-BICUCULLINE METHOCHLORIDE structure
CAS No.
38641-83-7
Chemical Name:
(+)-BICUCULLINE METHOCHLORIDE
Synonyms
(+)-BICUCULLINE METHOCHLORIDE;1(S),9(R)-(-)-Bicuculline methchloride;1(s),9(r)-(-)-bicuculline methochloride
CBNumber:
CB6503174
Molecular Formula:
C21H20NO6.Cl
Molecular Weight:
417.843
MDL Number:
MFCD00055233
MOL File:
38641-83-7.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-04-24 14:58:18
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(+)-BICUCULLINE METHOCHLORIDE Properties

storage temp. 2-8°C
solubility H2O: >10mg/mL
form powder
color Green
Water Solubility Soluble in water (100mM)
InChIKey RLJKFAMYSYWMND-GRTNUQQKSA-M
SMILES [Cl-].C[N+]1(C)CCc2cc3OCOc3cc2[C@H]1[C@@H]4OC(=O)c5c6OCOc6ccc45
FDA UNII I3UNE1K4AF
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

PPE Eyeshields, Gloves, type N95 (US)
Safety Statements  24/25
RIDADR  UN 1544 6.1/PG 2
WGK Germany  3
Storage Class 6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects

(+)-BICUCULLINE METHOCHLORIDE price More Price(16)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich B7686 1(S),9(R)-(?)-Bicuculline methchloride ≥97% (HPLC), powder 38641-83-7 25mg $317 2026-04-30 Buy
Sigma-Aldrich B7686 1(S),9(R)-(?)-Bicuculline methchloride ≥97% (HPLC), powder 38641-83-7 125mg $1120 2023-01-07 Buy
Biosynth NBA64183 1(S),9(R)-(-)-Bicuculline methchloride 38641-83-7 100mg $975 2026-06-04 Buy
ChemScene CS-0141957 Bicuculline methochloride 99.80% 38641-83-7 5mg $103 2026-06-04 Buy
ChemScene CS-0141957 Bicuculline methochloride 99.80% 38641-83-7 10mg $162 2026-06-04 Buy
Product number Packaging Price Buy
B7686 25mg $317 Buy
B7686 125mg $1120 Buy
NBA64183 100mg $975 Buy
CS-0141957 5mg $103 Buy
CS-0141957 10mg $162 Buy

(+)-BICUCULLINE METHOCHLORIDE Chemical Properties,Uses,Production

Uses

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

Biochem/physiol Actions

1(S),9(R)-()-Bicuculline methchloride is a GABAA receptor antagonist, which blocks Ca2+-activated potassium (SK) channels.

in vivo

Bicuculline methochloride can be used in animal modeling to create epilepsy models. Intracerebral injection of Bicuculline methochloride causes an increase in capillary blood flow in the epileptic focus (the specific region where seizures originate), with local blood flow increasing to 42.5 red blood cells per second (compared to 27.8 red blood cells per second in areas away from the epileptic focus)[5].

Induction of epilepsy[5]
Background
Epileptic seizures are closely related to the imbalance between neuronal excitability and inhibition, leading to abnormal neuronal discharges. Bicuculline methochloride is a GABAA receptor (GABAA receptor) antagonist that can inhibit inhibitory neurotransmission, induce excitatory neuronal activity, and cause population bursts (indicating that a large number of neurons fire action potentials simultaneously), thereby inducing epileptic seizures[5].
Specific Modeling Methods
Mice: C57BL6 male and female 20-30 g
Administration: 2.5 mM Intracranial Injection (deep layers of the somatosensory cortex) single dose
Note
(1) Dissolve 2.5 mM bicuculline methochloride in physiological saline.
(2) Inject bicuculline methochloride by inserting a glass micropipette with a diameter of 20-50 μm into the deep layers of the mouse somatosensory cortex.
(3) Surgical operation precautions:
a. Fix an insulated metallic head frame above the planned craniotomy area, and make a craniotomy with a diameter of approximately 3 mm over the mouse somatosensory cortex, removing the dura mater to expose the brain tissue.
b. Gently rinse the exposed area with artificial cerebrospinal fluid (composition of artificial cerebrospinal fluid: 125 mM NaCl, 3 mM KCl, 26 mM NaHCO3, 10 mM glucose, 1.1 mM NaH2PO4, 2 mM CaCl2, 1 mM MgSO4) to maintain the physiological environment of the brain tissue.
c. Cover the craniotomy with a phosphate-buffered saline solution containing 1% agarose (pH 7.4) and place a glass coverslip on the metal frame to protect the exposed brain tissue.
Modeling Indicators
Electrophysiological changes: A large number of neurons in the deep layers of the mouse somatosensory cortex fire electrical signals simultaneously, producing electrical signals characterized by interictal spikes (Note: Interictal Spikes (IISs) refer to the brief, high-amplitude voltage deflections observed in the electroencephalogram (EEG), which are typically associated with epileptic seizures).
Blood flow changes: In the somatosensory cortex of mice injected with bicuculline methochloride, capillary blood flow significantly increases.
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storage

Room temperature

References

[1] Y Yajima, et al. Effects of differential modulation of mu-, delta- and kappa-opioid systems on bicuculline-induced convulsions in the mouse. Brain Res. 2000 Apr 17;862(1-2):120-6. DOI:10.1016/s0006-8993(00)02096-5
[2] W A Turski, et al. Excitatory amino acid antagonists protect mice against seizures induced by bicuculline. Brain Res. 1990 Apr 23;514(1):131-4. DOI:10.1016/0006-8993(90)90444-g
[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. DOI:10.1016/s0014-2999(03)01344-x
[4] Khawaled R, et al. Bicuculline block of small-conductance calcium-activated potassium channels. Pflugers Arch. 1999 Aug;438(3):314-21. DOI:10.1007/s004240050915
[5] Hirase H, et al. Capillary level imaging of local cerebral blood flow in bicuculline-induced epileptic foci. Neuroscience. 2004;128(1):209-16. DOI:10.1016/j.neuroscience.2004.07.002

(+)-BICUCULLINE METHOCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

(+)-BICUCULLINE METHOCHLORIDE Suppliers

Global( 11)Suppliers
Supplier Tel Email Country ProdList Advantage
Sigma-Aldrich 021-61415566 800-8193336 orderCN@merckgroup.com China 51389 80
TargetMol Chemicals Inc. 4008200310 15002144251 marketing@tsbiochem.com China 24951 58
Nantong QuanYi Biotechnology Co., Ltd 0513-66337626 18051384581 sales@chemhifuture.com China 5987 58
Chengdu Peter-like Biotechnology Co., Ltd. 028-81700200 13308200041 2851167782@qq.com China 10763 58
Zhejiang Huida Biotech Co., Ltd. 0571-89903022 18679456698 zilong@hizyme.com China 7853 58
Supplier Advantage
Sigma-Aldrich 80
TargetMol Chemicals Inc. 58
Nantong QuanYi Biotechnology Co., Ltd 58
Chengdu Peter-like Biotechnology Co., Ltd. 58
Zhejiang Huida Biotech Co., Ltd. 58

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1(s),9(r)-(-)-bicuculline methochloride 1(S),9(R)-(-)-Bicuculline methchloride (+)-BICUCULLINE METHOCHLORIDE 38641-83-7 AntagonistsCell Signaling and Neuroscience GABAergics Neurotransmission Neurotransmitters New Products