青霉震颤素 A

青霉震颤素 A用途

Penitrem A 是由青霉菌产生的吲哚二萜神经毒性生物碱,是一种选择性的 BK 通道拮抗剂,对多种恶性肿瘤具有抗增殖、抗侵袭作用。Penitrem A 能刺激脑皮质突触体增加内源性谷氨酸、GABA 和天门冬氨酸的自发释放,能诱发动物产生震颤综合征。

点击显示

青霉震颤素 A名称

[ CAS 号 ]:
12627-35-9

[ 中文名 ]:
青霉震颤素

[ 英文名 ]:
PENITREM A

[英文别名 ]:

MFCD00083465
PENITREM A
4-Methylhistamine dihydrochloride
Tremortin A

青霉震颤素 A生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[ 靶点 ]

BK channel[1]

[参考文献]

[1]. Goda AA, et al. The Maxi-K (BK) Channel Antagonist Penitrem A as a Novel Breast Cancer-Targeted Therapeutic. Mar Drugs. 2018 May 11;16(5).

[2]. Norris PJ, et al. Actions of tremorgenic fungal toxins on neurotransmitter release. J Neurochem. 1980 Jan;34(1):33-42.

青霉震颤素 A物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 分子式 ]:
C₃₇H₄₄ClNO₆

[ 分子量 ]:
634.201

[ 精确质量 ]:
633.285706

[ PSA ]:
107.47000

[ LogP ]:
6.46

[ 折射率 ]:
1.698

[ 储存条件 ]:
-20°C

青霉震颤素 A毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RY7535000

CHEMICAL NAME :: Penitrem A

CAS REGISTRY NUMBER :: 12627-35-9

LAST UPDATED :: 199304

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C37-H44-Cl-N-O6

MOLECULAR WEIGHT :: 634.27

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 :: 10 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 :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1100 ug/kg

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

REFERENCE :: CTOXAO Clinical Toxicology. (New York, NY) V.1-18, 1968-81. For publisher information, see JTCTDW. Volume(issue)/page/year: 17,45,1980

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 500 ug/kg

TOXIC EFFECTS :: Behavioral - tetany Liver - fatty liver degeneration Nutritional and Gross Metabolic - body temperature increase

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 35,311,1976

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Bird - chicken

DOSE/DURATION :: 42 mg/kg

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

REFERENCE :: VHTODE Veterinary and Human Toxicology. (American College of Veterinary and Comparative Toxicology, Publication Office, Comparative Toxicology, Manhattan, KS 66506) V.19- 1977- Volume(issue)/page/year: 32(Suppl),63,1990 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 3 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: TOXIA6 Toxicon. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 OBW, UK) V.1- 1962- Volume(issue)/page/year: 16,92,1978

点击显示

青霉震颤素 A安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H310-H330

[ 警示性声明 ]:
P260-P264-P280-P284-P302 + P350-P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T+: Very toxic;

[ 风险声明 (欧洲) ]:
R26/27/28

[ 安全声明 (欧洲) ]:
S45;S36/S37/S39

[ 危险品运输编码 ]:
UN 2811 6

[ RTECS号 ]:
RY7535000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

青霉震颤素 A合成路线

详细合成路线

青霉震颤素 A上下游产品

青霉震颤素 A上游产品

青霉震颤素 A下游产品

青霉震颤素 A文献

5-hydroxytryptamine has an endothelium-derived hyperpolarizing factor-like effect on coronary flow in isolated rat hearts.

J. Biomed. Sci. 22 , 42, (2015)

5-hydroxytryptamine (5-HT)-induced coronary artery responses have both vasoconstriction and vasorelaxation components. The vasoconstrictive effects of 5-HT have been well studied while the mechanism(s...

Small molecule regulators of autophagy identified by an image-based high-throughput screen.

Proc. Natl. Acad. Sci. U. S. A. 104 , 19023-8, (2007)

Autophagy is a lysosome-dependent cellular catabolic mechanism mediating the turnover of intracellular organelles and long-lived proteins. Reduction of autophagy activity has been shown to lead to the...

Mechanisms underlying activation of transient BK current in rabbit urethral smooth muscle cells and its modulation by IP3-generating agonists.

Am. J. Physiol. Cell Physiol. 305(6) , C609-22, (2013)

We used the perforated patch-clamp technique at 37°C to investigate the mechanisms underlying the activation of a transient large-conductance K(+) (tBK) current in rabbit urethral smooth muscle cells....

更多文献