(+)-Bicuculline

製品コードS7071 バッチS707107

化学情報

	Synonyms	d-Bicuculline	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₁₇NO₆
	分子量	367.35	CAS No.	485-49-4
Solubility (25°C)*	体外	DMSO	73 mg/mL warmed with 50ºC water bath (198.72 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	(+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABA_A receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
in vitro	(+)-Bicuculline (1-100μM) dose-dependently inhibits the Cl^- conductance generated by 40 μM GABA. (+)-Bicuculline also inhibits the agonist action of GABA at 40 μM at α₁β₂γ_2L receptors. (+)-Bicuculline at 1 and 3 μM increases GABA EC50 values 1.6 times (41.0-67.0 μM) and 3.6 times (36.1-129.0 μM), respectively. Atα₁β₂γ_2L GABA_A receptors, (+)-bicuculline displays the general property of the competitive antagonist, producing a parallel shift of GABA concentration-effect curves and having no effect on the maximal response of GABA. ^[1] In addition to being a potent GABAA receptor antagonist, (+)-bicuculine also blocks Ca²⁺-activated potassium channels. ^[2]

製品説明

(+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABA_A receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.

in vitro

(+)-Bicuculline (1-100μM) dose-dependently inhibits the Cl^- conductance generated by 40 μM GABA. (+)-Bicuculline also inhibits the agonist action of GABA at 40 μM at α₁β₂γ_2L receptors. (+)-Bicuculline at 1 and 3 μM increases GABA EC50 values 1.6 times (41.0-67.0 μM) and 3.6 times (36.1-129.0 μM), respectively. Atα₁β₂γ_2L GABA_A receptors, (+)-bicuculline displays the general property of the competitive antagonist, producing a parallel shift of GABA concentration-effect curves and having no effect on the maximal response of GABA. ^[1] In addition to being a potent GABAA receptor antagonist, (+)-bicuculine also blocks Ca²⁺-activated potassium channels. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Electrophysiogical recording
キナーゼアッセイ	Receptor activity is measured with two-electrode voltage- clamp techniques 2-8 days after injection. Recording microelectrodes are fabricated with a micropipette puller and filled with 3 M KCl solution. Oocytes are placed in a cell bath and voltage clamped at 60 mV. Cells are continuously superfused with ND96 buffer. The currents elicited in response to the application of drugs are recorded using a Geneclamp 500 amplifier, a Mac Lab 2e recorder, and Chart version 3.5.2 program on a Macintosh Quadra 605 computer. Drugs are tested for direct activation of GABA at GABA_A receptors. For measurements of inhibitory action of drugs on receptor activation, drugs are added to the buffer solution containing GABA at the concentration producing 10%, 50%, 75%, 90% and 100% of the effect (GABA EC10, EC50, EC75, EC90 and EC100) at the receptors for constructing GABA inhibition dose-response curves. The same procedure, but with a fixed concentration of antagonists and increasing concentrations of GABA, is applied to construct GABA dose-response curves. A washout period of 3-5 min is allowed between each drug application to prevent receptor desensitisation.

参考

カスタマーフィードバック

: , , Sci Rep, 2014, 4:7270.

: Data from [Data independently produced by , , Br J Pharmacol, 2016, 173(10):1693-702.]

: Data from [Data independently produced by , , Sci Rep, 2016, 6: 19266.]

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人間や獣医の診断であるか治療的な使用のためにでない。

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