Bicuculline (Synonyms: (+)-Bicuculline; d-Bicuculline)
Bicuculline ((+)-Bicuculline; d-Bicuculline) 作為驚厥生物堿,是一種競(jìng)爭(zhēng)性的神經(jīng)遞質(zhì) GABAA 受體拮抗劑 (IC50=2 μM)。Bicuculline還能阻斷 Ca2+ 激huo鉀 (SK) 通道,并隨后阻斷慢后超極化(slow AHP)。
生物活性
Bicuculline ((+)-Bicuculline; d-Bicuculline), as a convulsant alkaloid, is a competitive neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+-activated potassium (SK) channels and subsequently blocks the slow afterhyperpolarization (slow AHP) [1][2][3].
IC50 & Target
IC50: 2 μM (GABAA)[3]
體外研究(In Vitro)
Bicuculline ((+)-Bicuculline; d-Bicuculline) (1 and 3 μM) attains the maximal response of GABA. Bicuculline appears to shift the dose–response curves of GABA in parallel to the right without decreasing GABA maximal response, suggesting that it is a competitive antagonist at α1β2γ2L GABAAreceptors[3].
分子量:367.35
性狀:Solid
Formula:C20H17NO6
CAS 號(hào):485-49-4
中文名稱:(+)-荷包牡丹堿;右旋荷包牡丹堿;比枯枯靈;山烏龜堿;畢枯枯林;右旋比扣扣靈堿
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性數(shù)據(jù)
DMSO : 50 mg/mL (136.11 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.7222 mL | 13.6110 mL | 27.2220 mL |
5 mM | 0.5444 mL | 2.7222 mL | 5.4444 mL |
10 mM | 0.2722 mL | 1.3611 mL | 2.7222 mL |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶
- 1.
請(qǐng)依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution
- 2.
請(qǐng)依序添加每種溶劑: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution
- 3.
請(qǐng)依序添加每種溶劑: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution
參考文獻(xiàn)
[1]. Johnston GA. Advantages of an antagonist: bicuculline and other GABA antagonists. Br J Pharmacol. 2013;169(2):328-336. [Content Brief]
[2]. Khawaled R, et al. Bicuculline block of small-conductance calcium-activated potassium channels. Pflugers Arch. 1999;438(3):314-321. [Content Brief]
[3]. Huang SH, et al. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors. Eur J Pharmacol. 2003;464(1):1-8. [Content Brief]
注:產(chǎn)品僅用于科研