(-)-Bicuculline methiodide - CAS 40709-69-1
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
GABA Receptor
(-)-Bicuculline methiodide is the methiodide salt of (+)-bicuculline, which is a potent antagonist of GABAA receptors.
Brife Description:
GABAA receptor antagonist
≥99% by HPLC
[R-(R,S)]-5-(6,8-Dihydro-8-oxofuro[3,4-e]-1,3-benzodioxol-6-yl)-5,6,7,8-tetrahydro-6,6-dimethyl-1,3-dioxolo[4,5-g]isoquinolinium iodide
Canonical SMILES:
1.Rebound bursts in GABAergic neurons of the thalamic reticular nucleus in postnatal mice.
Wang X;Yu G;Hou X;Zhou J;Yang B;Zhang L Physiol Res. 2010;59(2):273-80. Epub 2009 Jun 19.
Whole cell patch-clamp recordings from GABAergic cells of thalamic reticular nucleus (RTN) in thalamocortical slices made from postnatal day 6 (P6) to 10 (P10) were used to investigate the pattern of rebound bursts (RBs) triggered by an injection of hyperpolarizing current into RTN cells. The number of RBs in the RTN and the overlying Na(+)/K(+) spikes changed in an age-dependent manner. The generation of RBs depended largely on the amplitude of the after-hyperpolarizations (AHPs). RB patterns in response to hyperpolarizing current injection into relay cells were markedly different from RB patterns in RTN cells with an after-depolarization. GABA(A) receptor antagonist bicuculline methiodide (BMI) changed burst firing patterns, increasing the duration of RB and decreasing the amplitude of AHP in RTN cells. Furthermore, local puffs of NMDA in the presence of BMI induced RBs. K(+) channel blocker 4-aminopyridine partially mimicked the effect of BMI on AHPs. The shapes of RBs were altered by a selective CaMKII inhibitor KN-62, but not by an inactive analog KN-04.
2.Bicuculline increases Ca2+ transients in rat cerebellar granule cells through non-GABA(A) receptor associated mechanisms.
Mestdagh N;Wülfert E Neurosci Lett. 1999 Apr 16;265(2):95-8.
The effects of bicuculline methiodide (bicuculline) and gabazine, two GABA(A) antagonists, on cytosolic calcium increases (Ca2+ transients) in rat cerebellar granule cells were examined using Fluo-3-spectrofluorometry. Bicuculline (25 microM) markedly potentiated Ca2+ transients caused by KCl (25 mM) and by A23187 (4 microM) whereas gabazine (25 microM) had no effect. Calcium increases caused by glutamate (2 microM), N-methyl-D-aspartic acid (200 microM), trans-1-amino-cyclopentane-1,3 dicarboxylate (200 microM), thapsigargin (1 microM) or caffeine (5 mM) were not altered by bicuculline. Thapsigargin, which depletes intracellular Ca2+ stores, had no effect on either KCl- or A23187-induced Ca2+ transients, but completely blocked bicuculline-induced potentiation of Ca2+ increases. Our data suggest that bicuculline triggers calcium release when calcium entry is evoked by KCl or A23187 and that this effect is not mediated via GABA(A) receptor blockade.
3.Gamma-aminobutyric acid enhancement of potassium-stimulated release of [3H]norepinephrine by multiple mechanisms in rat cortical slices.
Peoples RW;Giridhar J;Isom GE Biochem Pharmacol. 1991 Jan 1;41(1):119-23.
Gamma-Aminobutyric acid (GABA) and GABAA agonists enhance stimulated release of [3H]norepinephrine [( 3H]NA) in several regions of the rat brain. In this study, the mechanisms by which GABA and GABAergic agonists augment potassium-stimulated release of [3H]NA from rat frontal cortical slices were examined. GABA enhanced potassium-stimulated [3H]NA release, but did not alter release of [3H]NA evoked by the calcium ionophore A23187, 10(-5) M, either in the presence or the absence of extracellular calcium. The effect of GABA on potassium-stimulated [3H]NA release was apparently reduced by the GABAA antagonist bicuculline methiodide, 10(-4) M, and by the selective inhibitor of GABA uptake SKF 89976A, 10(-5) M, but was abolished only when bicuculline methiodide and SKF 89976A were present in combination. The GABAA agonist muscimol enhanced potassium-stimulated release of [3H]NA in a manner similar to GABA. In addition, nipecotic acid, a substrate for GABA uptake, enhanced potassium-stimulated [3H]NA release. Thus, GABA appears to enhance potassium-stimulated [3H]NA release by acting upon both GABA uptake and GABAA receptors. The GABAA receptors involved in this effect may be a subtype of GABAA receptors since they are not modulated by benzodiazepines.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related GABA Receptor Products

CAS 1215833-62-7 DMCM hydrochloride

DMCM hydrochloride
(CAS: 1215833-62-7)

DMCM hydrochloride is a benzodiazepine inverse agonist exhibiting anxiogenic and potent convulsant activity.

CAS 123557-91-5 rac BHFF

rac BHFF
(CAS: 123557-91-5)

BHFF is a positive allosteric modulator of GABAB receptor that increases the potency and efficacy of GABA. BHFF displays anxiolytic activity in vivo.

CAS 123691-29-2 CGP 36216 hydrochloride

CGP 36216 hydrochloride
(CAS: 123691-29-2)

CGP 36216 hydrochloride is a selective GABAB antagonist that is active to presynaptic receptors but inactive to postsynaptic receptors.

CAS 125-33-7 Primidone

(CAS: 125-33-7)

Primidone, a pyrimidinedione derivative, could be used as an anticonvulsant agent especially against epilepsy unspecified.

CAS 69308-37-8 (R)-baclofen

(CAS: 69308-37-8)

(R)-baclofen a selective GABAB agonist.

CAS 78755-81-4 Flumazenil

(CAS: 78755-81-4)

Flumazenil is a GABAA receptor antagonist and the only GABAA receptor antagonist on the market today.

CAS 220860-50-4 CP-457920

(CAS: 220860-50-4)

CP-457920, also called as NGD 971, is a selective α5 GABAA receptor inverse agonist (Ki of ~ 1 ng/mL). CP-457920 was progressed into clinical studies for the tr...

CAS 111205-55-1 CGS 20625

CGS 20625
(CAS: 111205-55-1)

CGS 20625 is a partial agonist for the benzodiazepine binding site of the GABAA receptor used as an anti-anxiety drug. It acts as a central benzodiazepine recep...

CAS 155569-91-8 Emamectin Benzoate

Emamectin Benzoate
(CAS: 155569-91-8)

Emamectin Benzoate is the Emamectin derivative. Emamectin, also called as Proclaim, is widely used as an insecticide because of its chloride channel activation ...

RuBi GABA trimethylphosphine

RuBi GABA trimethylphosphine is the modified version of RuBi-GABA, which inhibits neural activity in vivo and is suitable for use as alternative for GABA agonis...

CAS 53188-20-8 Etomidate Hydrochloride

Etomidate Hydrochloride
(CAS: 53188-20-8)

Etomidate hydrochloride is a GABAA receptor agonist used for the induction of general anaesthesia.

CAS 371962-01-5 ZAPA sulfate

ZAPA sulfate
(CAS: 371962-01-5)

ZAPA sulfate acts as an agonist at low affinity GABAA receptors and is thus a useful ligand to investigate GABA receptors linked to benzodiazepine receptors. ZA...

CAS 145645-62-1 NNC 711

NNC 711
(CAS: 145645-62-1)

NNC 711 is a GABA uptake inhibitor by GAT-1 with IC50 values of 0.04, 171, 1700 and 622 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1. NNC 711 is an anticonvulsantag...

CAS 602-41-5 Thiocolchicoside

(CAS: 602-41-5)

Thiocolchicoside is a semi-synthetic derivative of colchicine, an anti-inflammatory glycoside extracted from the flower seeds of superba gloriosa. Thiocolchicos...

CAS 1135210-68-2 Tracazolate hydrochloride

Tracazolate hydrochloride
(CAS: 1135210-68-2)

Tracazolate hydrochloride is a subtype-selective GABAA receptor modulator that potentiates or inhibits recombinant GABAA function depending on subunit combinati...

CAS 73604-30-5 (-)-Bicuculline methobromide

(-)-Bicuculline methobromide
(CAS: 73604-30-5)

(-)-Bicuculline methobromide is the methobromide salt of (+)-bicuculline, which is a potent antagonist of GABAA receptors.

CAS 66548-69-4 CL 218872

CL 218872
(CAS: 66548-69-4)

CL 218872 has been found to be a benzodiazepine agonist and has been found to exhibit anxiolytic and anticonvulsant activities.

CAS 160296-13-9 SB 205384

SB 205384
(CAS: 160296-13-9)

SB 205384 is a GABAA receptor modulator. SB 205384 potentiates α6, α3 and α5-subunit-containing receptors (EC50 = 280, 695 and 730 nM, respectively). It exhibit...

CAS 205881-86-3 SL 651498

SL 651498
(CAS: 205881-86-3)

SL 651498 is a GABAA agonist selectively for subtype α2, and has the potential for the treatment of anxiety.

CAS 40709-69-1 (-)-Bicuculline methiodide

(-)-Bicuculline methiodide
(CAS: 40709-69-1)

(-)-Bicuculline methiodide is the methiodide salt of (+)-bicuculline, which is a potent antagonist of GABAA receptors.

Chemical Structure

CAS 40709-69-1 (-)-Bicuculline methiodide

Quick Inquiry

Verification code

Featured Items