蕈青霉素

蕈青霉素用途

Paxilline 是一种来自 Penicillium paxilli 的吲哚生物碱霉菌毒素,通过封闭通道的阻断机制有效地抑制 BK 通道。 Paxilline 也能抑制肌质网 Ca2+ 刺激的 ATP 酶 (SERCA),对不同亚型的 SERCA 作用的 IC50 值为介于 5 μM-50 μM 之间。 Paxilline 具有显着的抗惊厥活性。

蕈青霉素名称

[ CAS 号 ]:
57186-25-1

[ 中文名 ]:
蕈青霉素

[ 英文名 ]:
Paxilline

[英文别名 ]:

PAXILINE
PAXILLINE,PENICILLIUM PAXILLI
DPNI-caged-GABA
MFCD00083464
paxilline from penicillium paxilli
Paxilline 1
Paxilline

蕈青霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 5-50 μM (SERCA)[2], BK channel[1]

[参考文献]

[1]. Zhou Y, et al. Paxilline inhibits BK channels by an almost exclusively closed-channel block mechanism. J Gen Physiol. 2014 Nov;144(5):415-40.

[2]. Bilmen JG, et al. The mechanism of inhibition of the sarco/endoplasmic reticulum Ca2+ ATPase by paxilline. Arch Biochem Biophys. 2002 Oct 1;406(1):55-64.

[3]. Sheehan JJ, et al. Anticonvulsant effects of the BK-channel antagonist paxilline. Epilepsia. 2009 Apr;50(4):711-20.

蕈青霉素物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
648.8±55.0 °C at 760 mmHg

[ 熔点 ]:
252ºC

[ 分子式 ]:
C₂₇H₃₃NO₄

[ 分子量 ]:
435.555

[ 闪点 ]:
346.2±31.5 °C

[ 精确质量 ]:
435.240967

[ PSA ]:
82.55000

[ LogP ]:
3.77

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.661

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
Soluble in DMSO, acetone or chloroform.

蕈青霉素MSDS

详细MSDS(安全技术说明书)

蕈青霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DJ2830000

CAS REGISTRY NUMBER :: 57186-25-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C27-H33-N-O4

MOLECULAR WEIGHT :: 435.61

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >227 mg/kg

TOXIC EFFECTS :: Behavioral - tremor

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 41,1868,1988

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 41KEAL "Toxicology, Biochemistry and Pathology of Mycotoxins," Uraguchi, K. and M. Yamazaki, eds., New York, John Wiley & Sons, Inc., 1978 Volume(issue)/page/year: -,108,1978

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Bird - chicken

DOSE/DURATION :: >100 mg/kg

TOXIC EFFECTS :: Behavioral - tremor

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 41,1868,1988

蕈青霉素安全信息

[ 符号 ]:

GHS05, GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H311-H315-H318-H331-H335

[ 警示性声明 ]:
P261-P280-P301 + P310-P305 + P351 + P338-P311

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R23/24/25

[ 安全声明 (欧洲) ]:
26-36/37/39-45

[ 危险品运输编码 ]:
UN 2811 6

[ WGK德国 ]:
3

[ RTECS号 ]:
DJ2830000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
29419090

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蕈青霉素文献

Large-conductance calcium-activated potassium current modulates excitability in isolated canine intracardiac neurons.

Am. J. Physiol. Cell Physiol. 304(3) , C280-6, (2013)

We studied principal neurons from canine intracardiac (IC) ganglia to determine whether large-conductance calcium-activated potassium (BK) channels play a role in their excitability. We performed whol...

Mitochondrial K+ channels are involved in ischemic postconditioning in rat hearts.

J. Physiol. Sci. 62(4) , 325-32, (2012)

The mitochondrial calcium-activated potassium channel (mitoK(Ca)) and the mitochondrial ATP-sensitive potassium channel (mitoK(ATP)) are both involved in cardiac preconditioning. Here, we examined whe...

Methamphetamine inhibits voltage-gated potassium currents in NG108-15 cells: possible contribution of large-conductance calcium-activated potassium channels.

Toxicol. Lett. 223(2) , 139-45, (2013)

Methamphetamine (MA), a highly abused amphetamine-like psychostimulant, has surged in popularity worldwide in the last decade. Repeated MA exposure has been shown to affect the alternative splice vari...

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