ChemicalBook CAS DataBase List (+)-BICUCULLINE METHOCHLORIDE

(+)-BICUCULLINE METHOCHLORIDE

Product Name(+)-BICUCULLINE METHOCHLORIDE
CAS38641-83-7
CBNumberCB6503174
MFC21H20NO6.Cl
MW417.843
MDL NumberMFCD00055233
MOL File38641-83-7.mol
MSDS FileSDS

Chemical 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

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

Product number	Packaging	Price	Product description	Buy
Sigma-Aldrich B7686	25mg	$317	1(S),9(R)-(?)-Bicuculline methchloride ≥97% (HPLC), powder	Buy
Sigma-Aldrich B7686	125mg	$1120	1(S),9(R)-(?)-Bicuculline methchloride ≥97% (HPLC), powder	Buy
Biosynth NBA64183	100mg	$975	1(S),9(R)-(-)-Bicuculline methchloride	Buy
ChemScene CS-0141957	5mg	$103	Bicuculline methochloride 99.80%	Buy
ChemScene CS-0141957	10mg	$162	Bicuculline methochloride 99.80%	Buy

(+)-BICUCULLINE METHOCHLORIDE Chemical Properties,Usage,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 GABA_A 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.

Correlated Product(s): /

Opposite Product(s): /

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

Preparation Products And Raw materials

(+)-BICUCULLINE METHOCHLORIDE 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	5984	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

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