产品名称
二氮嗪,
InChI key
GDLBFKVLRPITMI-UHFFFAOYSA-N
InChI
1S/C8H7ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-4H,1H3,(H,10,11)
SMILES string
CC1=Nc2ccc(Cl)cc2S(=O)(=O)N1
form
powder
solubility
0.1 M NaOH: soluble
H2O: insoluble
methanol: soluble
originator
Schering Plough
Quality Level
Gene Information
human ... KCNA1(3736), KCNJ11(3767), KCNJ8(3764), KCNMA1(3778)
mouse ... Kcnj1(56379), Kcnj11(16514)
rat ... Gria1(50592), Kcna1(24520), Kcnj1(24521), Kcnj11(83535), Kcnj8(25472)
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相关类别
Application
二氮嗪已用于二氮嗪输注。 也用于防止 K + 诱导的胞吐作用的去极化。
Biochem/physiol Actions
血管平滑肌和胰岛 β 细胞中的选择性 ATP 敏感性 K + 通道激活剂-细胞;抗高血压药。
Features and Benefits
该化合物由Schering Plough开发。要浏览其他药物开发化合物和批准的药物/候选药物列表,单击此处。
General description
二氮嗪是一种非利尿性苯并噻二嗪类药物,用于治疗低血糖、血管性血友病、急性和恶性高血压。作为 β 细胞 KATP 通道开放剂,二氮嗪可防止胰岛素的分泌。
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
Diazoxide for Lowering Insulin Levels in Breast Cancer Patients.
Fink MK and Klement RJ
Oncologist, 22(4), 491-491 (2017)
Pharmacological Preconditioning with Diazoxide in the Experimental Hypothermic Circulatory Arrest Model
Haapanen H, et al.
The Heart Surgery Forum (2017)
Glucose-dependent granule docking limits insulin secretion and Is decreased in human type 2 diabetes
Gandasi NR, et al.
Cell Metabolism, 27(2), 470-478 (2018)
T Grimmsmann et al.
British journal of pharmacology, 123(5), 781-788 (1998-04-16)
1. The direct effects of diazoxide on mitochondrial membrane potential, Ca2+ transport, oxygen consumption and ATP generation were investigated in mouse pancreatic B-cells and rat liver mitochondria. 2. Diazoxide, at concentrations commonly used to open adenosine 5'-triphosphate (ATP)-dependent K+-channels (K(ATP)
N D'hahan et al.
Proceedings of the National Academy of Sciences of the United States of America, 96(21), 12162-12167 (1999-10-16)
The pharmacological phenotype of ATP-sensitive potassium (K(ATP)) channels is defined by their tissue-specific regulatory subunit, the sulfonylurea receptor (SUR), which associates with the pore-forming channel core, Kir6.2. The potassium channel opener diazoxide has hyperglycemic and hypotensive properties that stem from
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