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左色满卡林

左色满卡林用途

LevCromakalim 是 ATP 敏感性的 K+ 通道 (KATP) 激活剂。

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左色满卡林名称

[ CAS 号 ]:
94535-50-9

[ 中文名 ]:
左色满卡林

[ 英文名 ]:
Levcromakalim

[英文别名 ]:

levcromakelim
levcromakalim
lemakalim

左色满卡林生物活性

[ 描述 ]:

LevCromakalim 是 ATP 敏感性的 K+ 通道 (KATP) 激活剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 心血管疾病

[ 靶点 ]

K+ channel[1]

[体外研究]

LevCromakalim(Cromakalim)以格列本脲敏感的方式完全抑制自发性收缩。 LevCromakalim(5μM)抑制自发性收缩,其通过格列本脲回收。 LevCromakalim(1,5和10μM)抑制相位收缩至对照的34±21.1％,20.1±20.0％和0％(分别为n = 5; P <0.05)。格列本脲逆转由LevCromakalim(5μM)引起的自发等长收缩对对照的84±1.5％的抑制(n = 5; P <0.05)。 LevCromakalim(20和100μM)也抑制催产素(OXT)(10nM)诱导的阶段性收缩至对照的34±21.4％和14±12.6％(分别为n = 6和4; P <0.05)。格列本脲逆转LevCromakalim(100μM)对自发等长收缩的抑制,达到对照的79±3.5％(n = 4; P <0.05)。克罗马卡林以格列本脲敏感的方式抑制OXT的强直收缩[2]。用特定的通道开放剂LevCromakalim(Cromakalim)检查KATP通道的功能。 LevCromakalim在年轻和年老的肠系膜动脉(MA)中诱导剂量依赖性舒张;放松与年龄没有区别。然而,响应于旧MA中的高盐(HS)饮食,松弛显着降低(P <0.05)。 LevCromakalim(10-4 M)的最大扩张在年轻MA中为97±3％,而在年轻盐动脉中为98±1％,而旧MA中的扩张为99±0.7％,而在此为85±5％。老盐动脉(P <0.05)[3]。

[激酶实验]

将LevCromakalim（Cromakalim）溶于10％DMSO和Krebs溶液中[3]。通过用乙酰胆碱（ACh; 10nM-10μM）进行浓度 - 响应实验来测试内皮依赖性舒张。通常，将MA暴露于每剂ACh至少6分钟，并确定最大响应。用10μM格列本脲（选择性KATP通道抑制剂）和LevCromakalim（Cromakalim）（10nM至100μM）（KATP通道开放剂）检查KATP通道的功能。在ACh前10分钟向动脉浴中加入格列本脲不会改变我们组中任何MA的被动最大内径。血管直径变化表示为预收缩血管扩张的百分比（％），计算[3]。

[参考文献]

[1]. Matsumoto T, et al. Tunicamycin-Induced Alterations in the Vasorelaxant Response in Organ-Cultured Superior Mesenteric Arteries of Rats. Biol Pharm Bull. 2016;39(9):1475-81.

[2]. Hong SH, et al. Regulation of myometrial contraction by ATP-sensitive potassium (KATP) channel via activation of SUR2B and Kir 6.2 in mouse. J Vet Med Sci. 2016 Aug 1;78(7):1153-9.

[3]. Whidden MA, Altered potassium ATP channel signaling in mesenteric arteries of old high salt-fed rats. J Exerc Nutrition Biochem. 2016 Jun;20(2):58-64.

[相关活性小分子]

左色满卡林物理化学性质

[ 密度 ]:
1.31g/cm3

[ 沸点 ]:
482.3ºC at 760mmHg

[ 分子式 ]:
C₁₆H₁₈N₂O₃

[ 分子量 ]:
286.32600

[ 闪点 ]:
245.5ºC

[ 精确质量 ]:
286.13200

[ PSA ]:
73.56000

[ LogP ]:
1.69158

[ 储存条件 ]:
2-8℃

左色满卡林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DJ2177500

CHEMICAL NAME :: 2H-1-Benzopyran-6-carbonitrile, 3,4-dihydro-3-hydroxy-2,2-dimethyl-4-(2-oxo-1-pyrroli dinyl)-, (3S-trans)-

CAS REGISTRY NUMBER :: 94535-50-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C16-H18-N2-O3

MOLECULAR WEIGHT :: 286.36

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2500 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22(Suppl 7),S1425,1994

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22(Suppl 7),S1425,1994

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >750 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22(Suppl 7),S1425,1994

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >4 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22(Suppl 7),S1425,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 273 mg/kg/13W-C

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - changes in circulation Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22(Suppl 7),S1425,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 110 mg/kg/52W-C

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - changes in circulation Cardiac - changes in heart weight Related to Chronic Data - changes in ovarian weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22(Suppl 7),S1425,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 18 mg/kg/13W-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22(Suppl 7),S1425,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 37 mg/kg/52W-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22(Suppl 7),S1425,1994

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左色满卡林安全信息

[ 海关编码 ]:
2934999090

左色满卡林合成路线

详细合成路线

左色满卡林上下游产品

左色满卡林上游产品

左色满卡林下游产品

左色满卡林海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%