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Bicuculline

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Chemical Structure| 485-49-4 同义名 : 荷包牡丹碱 ;d-Bicuculline;NSC 32192;BRN 0098786;Bicucullin;Bicculine;(+)-Bicuculline
CAS号 : 485-49-4
货号 : A658573
分子式 : C20H17NO6
纯度 : 98+%
分子量 : 367.352
MDL号 : MFCD00005006
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(136.11 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • GABAA receptor

    GABAA receptor, IC50:2 μM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.61mL

2.72mL

1.36mL

27.22mL

5.44mL

2.72mL
参考文献

[1]Huang SH, Duke RK, et al. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors. Eur J Pharmacol. 2003 Mar 7;464(1):1-8.

[2]Khawaled R, Bruening-Wright A, et al. Bicuculline block of small-conductance calcium-activated potassium channels. Pflugers Arch. 1999 Aug;438(3):314-21.

[3]Srivastava A, Tandon P, Jain S, Asthana BP. Antagonistic properties of a natural product-Bicuculline with the gamma-aminobutyric acid receptor: studied through electrostatic potential mapping, electronic and vibrational spectra using ab initio and density functional theory. Spectrochim Acta A Mol Biomol Spectrosc. 2011 Dec 15;84(1):144-55

[4]Mestdagh N, Wülfert E. Bicuculline increases Ca2+ transients in rat cerebellar granule cells through non-GABA(A) receptor associated mechanisms. Neurosci Lett. 1999 Apr 16;265(2):95-8

[5]Smart TG, Constanti A. A re-examination of the GABA-inhibitory action of bicuculline on lobster muscle. Eur J Pharmacol. 1981 Mar 5;70(1):25-33

[6]Karson AB, Aker R, Ateş N, Onat F. Cardiovascular effects of intracerebroventricular bicuculline in rats with absence seizures. Epilepsy Res. 1999 Apr;34(2-3):231-9