Brevetoxin-3

Brevetoxin-3用途

Brevetoxin-3 (PbTx-3) 是一种有效的变构电压门控 Na+ 通道 (Na+ channels) 激活剂,具有多个活性中心 (A 环内酯,R 侧链的 C-42)。Brevetoxin-3 (PbTx-3) 对电压敏感的 Na+ 通道的位点 5 具有高亲和力,抑制 Na+ 通道的失活并延长这些通道的平均打开时间。Brevetoxin-3 (PbTx-3) 可导致气道高反应性 (AHR) 延长和肺部炎症。

Brevetoxin-3名称

[ CAS 号 ]:
85079-48-7

[ 中文名 ]:
短毒素3(PbTx-3)

[ 英文名 ]:
Brevetoxin-3

[英文别名 ]:

GB 3 toxin
T-17 toxin
Brevetoxin PbTx 3
PbTx 3
GB 3
[3H]-PbTx 3
Brevetoxin T17
brevetoxin-3
Toxin T-17
Ptychodiscus brevis toxin 3

Brevetoxin-3生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 炎症/免疫

[ 靶点 ]

IC50: voltage-gated Na+ channel[1]

[体外研究]

Brevetoxin-3(PbTx-3)(30-500nm)在稳态条件下(维持在-50mv的去极化)产生一个更负的膜电位,从而观察到单通道活性[1]。

[体内研究]

Brevetoxin-3(PbTx-3)(气管内滴注；2.8μg/kg；妊娠15-18天)在胎盘和胎儿中0.5小时内检测到放射性。在给药后48小时内,胎儿体内的灯盏花素当量浓度约为0.3 ng/g,因此胎儿的计算剂量为19 ng/g h。注射brevetoxin后,胎儿中的brevetoxin当量浓度为0.1ng/g,低于大多数母体组织中的浓度[3]。动物模型：妊娠期CD-1小鼠[3]剂量：2.8μg/kg给药：气管内滴注；2.8μg/kg；妊娠15-18天结果：显示孕产妇急性暴露后,灯盏花素或其代谢物在胎盘转运

[参考文献]

[1]. Jeglitsch G,et al. Brevetoxin-3 (PbTx-3) and its derivatives modulate single tetrodotoxin-sensitive sodium channels in rat sensory neurons.J Pharmacol Exp Ther. 1998 Feb;284(2):516-25.

[2]. Zaias J,et al. Repeated exposure to aerosolized brevetoxin-3 induces prolonged airway hyperresponsiveness and lung inflammation in sheep.Inhal Toxicol. 2011 Mar;23(4):205-11.

[3]. Benson JM, et al. Placental transport of brevetoxin-3 in CD-1 mice.Toxicon. 2006 Dec 15;48(8):1018-26. Epub 2006 Aug 18.

Brevetoxin-3物理化学性质

[ 密度 ]:
1.187g/cm3

[ 分子式 ]:
C₅₀H₇₂O₁₄

[ 分子量 ]:
897.09800

[ 精确质量 ]:
896.49200

[ PSA ]:
159.06000

[ LogP ]:
5.26550

[ 折射率 ]:
1.52

Brevetoxin-3毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XW5885000

CHEMICAL NAME :: Toxin T-17

CAS REGISTRY NUMBER :: 85079-48-7

LAST UPDATED :: 198509

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 520 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - fasciculations Behavioral - tremor Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: TOXIA6 Toxicon. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 OBW, UK) V.1- 1962- Volume(issue)/page/year: 20,457,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 170 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - fasciculations Behavioral - tremor Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: TOXIA6 Toxicon. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 OBW, UK) V.1- 1962- Volume(issue)/page/year: 20,457,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 94 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - fasciculations Behavioral - tremor Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: TOXIA6 Toxicon. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 OBW, UK) V.1- 1962- Volume(issue)/page/year: 20,457,1982

Brevetoxin-3

Brevetoxin-3用途

Brevetoxin-3名称

Brevetoxin-3生物活性

Brevetoxin-3物理化学性质

Brevetoxin-3毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

Brevetoxin-3安全信息

Brevetoxin-3上下游产品

Brevetoxin-3上游产品

Brevetoxin-3下游产品

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