(+)-Bicuculline (1-100μM) dose-dependently inhibits the Cl- conductance generated by 40 μM GABA. (+)-Bicuculline inhibits GABA(A) α2/β1/γ2 currents activated by γ-Aminobutyric acid, (+)-Bicuculline concentration from 10 nM to 2 μM progressively decreased the amplitude of GABA-activated ion currents. Furthermore, (+)-bicuculine also blocks small-conductance calcium-activated potassium channels.
|Animal models||Fischer-344 virgin female rats of Ovariectomy|
|Formulation||sesame oil + 10% DMSO|
|Dosages||3.5 mg/kg daily|
|Administration||via osmotic subcutaneous pumps|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL|
The GABAA antagonist bicuculline attenuates progesterone-induced memory impairments in middle-aged ovariectomized rats.
Braden BB, et al. Front Aging Neurosci. 2015 Aug 14;7:149. PMID: 26321945.
Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors.
Huang SH, et al. Eur J Pharmacol. 2003 Mar 7;464(1):1-8. PMID: 12600688.
|Related GABA Receptor Products|
Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
Tiagabine Hydrochloride is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
Tiagabine is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
Pentylenetetrazol displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.
L-cycloserine irreversibly inhibit GABA pyridoxal 5′-phosphate-dependent aminitransferase in E. coli, as well in the brains of various animals in a time-dependent manner, results in increased levels of gamma-aminobutyric acid (GABA), which is an inhibitory neurotransmitter in vivo.
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