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CAS No.: 485-49-4

(+)-荷包牡丹碱 Catalog No. CSN10435

Synonyms: (+)-Bicuculline;d-Bicuculline;毕扣扣灵碱

(+)-Bicuculline is an antagonist of GABAA receptor with IC50 of 2 μM and also shows inhibition of Ca(2+)-activated potassium channels.

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技术信息

生物活性

描述(+)-Bicuculline is a light-sensitive competitive antagonist of GABA-A receptor^[3]. Bicuculline (25 mM) markedly potentiated Ca2+ transients caused by KCl (25 mM) and by A23187 (4 mM) whereas gabazine (25 mM) had no effect. 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^[4]. Bicuculline (20-100 micrometers) depressed the GABA-evoked conductance increase in a reversible manner, the double reciprocal transformation of the GABA dose/conductance curves remaining linear. Combinations of bicuculline and picrotoxinin also depressed the GABA response in a manner expected from the combination of two "mixed" non-competitive antagonists. Bicuculline (like picrotoxinin and picrotoxin) behaves as a "mixed" non-competitive rather than a pure non-competitive antagonist of GABA on lobster muscle^[5]. Intracerebroventricular administration of 0.3 and 0.5 nmol of bicuculline produces an increase in blood pressure and a slight bradycardia in non-epileptic Wistar rats. The blood pressure response to intracerebroventricular bicuculline is significantly potentiated in epileptic WAG/Rij rats. Additionally, the pressor effect of 0.5 nmol of bicuculline is not attenuated by bilateral electrolytic ablation of the central nucleus of the amygdala in WAG/Rij rats^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7222 mL
- 13.6109 mL
- 27.2218 mL
- 5 mM
- 0.5444 mL
- 2.7222 mL
- 5.4444 mL
- 10 mM
- 0.2722 mL
- 1.3611 mL
- 2.7222 mL

技术信息

CAS号

485-49-4

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H17NO6

运输

蓝冰

分子量

367.35

别名

(+)-Bicuculline;d-Bicuculline;毕扣扣灵碱

溶解度

DMSO	51.0 mg/mL (138.8 mM)
Water	insoluble

动物实验配方

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