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(-)-双甲基溴甲烷

(-)-双甲基溴甲烷用途

甲基溴双瓜氨酸是一种选择性GABAA受体拮抗剂,IC50值为3μM。甲基溴双瓜氨酸可诱导哺乳动物阵挛性强直性惊厥,也可用于阻断Ca2+激活的钾通道。甲基溴双瓜氨酸可用于癫痫和其他相关精神疾病的研究[1][2]。

(-)-双甲基溴甲烷名称

[ CAS 号 ]:
66016-70-4

[ 中文名 ]:
(-)-双甲基溴甲烷

[ 英文名 ]:
(-)-BICUCULLINE METHBROMIDE

[英文别名 ]:

(-)-Bicuculline methbromide,1(S),9(R)
(-)-Bicuculine Methbromide
Bicuculline methobromide
(-)-Bicuculline Methbromide
HMS2234F21

(-)-双甲基溴甲烷生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[体外研究]

1μM和3μM的甲基溴双瓜氨酸对GABA的反应最大。甲基溴双瓜氨酸似乎使GABA的剂量-反应曲线向右平行移动,而不会降低GABA的最大反应,这表明它是爪蟾卵母细胞中表达的人α1β2γ2L GABAA受体的竞争性拮抗剂[3]。甲基溴双瓜氨酸(1-100μM；2分钟；作为外向贴片施用)可有效阻断爪蟾卵母细胞中Apamin(HY-P0256)敏感的小电导钙激活钾通道(SK2)电流和Apamin不敏感的SK1电流[4]。

[体内研究]

甲基溴双瓜氨酸(皮下注射,1.25-3 mg/kg)可引起小鼠阵挛性强直性惊厥,并呈剂量依赖性,注射μ-阿片类激动剂吗啡可增强这些惊厥[1]。甲基溴双瓜氨酸(皮下注射,1.5-3.2 mg/kg)诱导雄性Swiss S小鼠全身性发作,阵挛的CD50(惊厥剂量)为2.2 mg/kg,强直的CD50为2.4 mg/kg。用NMDA拮抗剂MK-801、CPP和CGS 19755[2]预处理(i.p.)可阻断剂量为3.2 mg/kg的比库瓜氨酸诱发的癫痫发作。

[参考文献]

[1]. Y Yajima, et al. Effects of differential modulation of mu-, delta- and kappa-opioid systems on bicuculline-induced convulsions in the mouse. Brain Res. 2000 Apr 17;862(1-2):120-6.

[2]. W A Turski, et al. Excitatory amino acid antagonists protect mice against seizures induced by bicuculline. Brain Res. 1990 Apr 23;514(1):131-4.

[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.

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

(-)-双甲基溴甲烷物理化学性质

[ 分子式 ]:
C₂₁H₂₀BrNO₆

[ 分子量 ]:
462.29100

[ 精确质量 ]:
461.04700

[ PSA ]:
63.22000

(-)-双甲基溴甲烷MSDS

详细MSDS(安全技术说明书)

(-)-双甲基溴甲烷安全信息

[ 符号 ]:

GHS06, GHS09

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H311 + H331-H410

[ 警示性声明 ]:
P261-P264-P273-P280-P301 + P310-P311

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
24/25

[ 危险品运输编码 ]:
UN 1544 6.1/PG 2

(-)-双甲基溴甲烷文献

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Increased c-Fos expression in select lateral parabrachial subnuclei following chemical versus electrical stimulation of the dorsal periaqueductal gray in rats.

Brain Res. 974(1-2) , 153-66, (2003)

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