Mequitazine (BioDeep_00000009382)

 

Secondary id: BioDeep_00000858514

human metabolite blood metabolite


代谢物信息卡片


10-{1-azabicyclo[2.2.2]octan-3-ylmethyl}-10H-phenothiazine

化学式: C20H22N2S (322.1504)
中文名称: 美喹他嗪
谱图信息: 最多检出来源 Homo sapiens(blood) 43.39%

分子结构信息

SMILES: C(C1CN2CCC1CC2)N1C2=CC=CC=C2SC2=CC=CC=C12
InChI: InChI=1S/C20H22N2S/c1-3-7-19-17(5-1)22(18-6-2-4-8-20(18)23-19)14-16-13-21-11-9-15(16)10-12-21/h1-8,15-16H,9-14H2

描述信息

Mequitazine is a histamine H1 antagonist (antihistamine). It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
R - Respiratory system > R06 - Antihistamines for systemic use > R06A - Antihistamines for systemic use > R06AD - Phenothiazine derivatives
D018377 - Neurotransmitter Agents > D018494 - Histamine Agents > D006633 - Histamine Antagonists
C308 - Immunotherapeutic Agent > C29578 - Histamine-1 Receptor Antagonist
Same as: D01324
Mequitazine is a potent, and long-acting histamine H1 antagonist.

同义名列表

11 个代谢物同义名

10-{1-azabicyclo[2.2.2]octan-3-ylmethyl}-10H-phenothiazine; Mequitazine tartrate, (R-(r*,r*))-isomer; 3-Methylquinuclidinyl-10-phenothiazine; Mequitazine hydrochloride; mequitazine; Quitadrill; Kitazemin; Primalan; Mircol; LM-209; Mequitazine



数据库引用编号

15 个数据库交叉引用编号

分类词条

相关代谢途径

Reactome(0)

BioCyc(0)

PlantCyc(0)

代谢反应

0 个相关的代谢反应过程信息。

Reactome(0)

BioCyc(0)

WikiPathways(0)

Plant Reactome(0)

INOH(0)

PlantCyc(0)

COVID-19 Disease Map(0)

PathBank(0)

PharmGKB(0)

1 个相关的物种来源信息

在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有:

  • PubMed: 来源于PubMed文献库中的文献信息,我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表,这个列表按照代谢物同时出现的文献数量降序排序,取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
  • NCBI Taxonomy: 通过文献数据挖掘,得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序,取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
  • Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
  • Chemical Reaction: 在化学反应过程中,存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。

点击图上的相关代谢物的名称,可以跳转到相关代谢物的信息页面。

亚细胞结构定位 关联基因列表
Cytoplasm 10 ATN1, BCL2, DPF2, HMGB1, JAK2, KLF4, NLRP3, PLA2G12A, XDH, ZMYND8
Peripheral membrane protein 2 HMGB1, JAK2
Endoplasmic reticulum membrane 1 BCL2
Nucleus 10 ATN1, BCL2, DPF2, HMGB1, JAK2, KLF4, LMNB1, MLLT3, NLRP3, ZMYND8
cytosol 8 BCL2, DPF2, JAK2, KLF4, LIPE, MLLT3, NLRP3, XDH
centrosome 1 DPF2
nucleoplasm 8 ATN1, DPF2, HMGB1, JAK2, KLF4, LMNB1, MLLT3, ZMYND8
Cell membrane 2 HMGB1, LIPE
Multi-pass membrane protein 1 CACNA1I
Golgi apparatus membrane 1 NLRP3
cell junction 1 ATN1
cell surface 2 BMP2, HMGB1
dendritic shaft 1 ZMYND8
glutamatergic synapse 1 JAK2
Golgi membrane 1 NLRP3
postsynapse 1 JAK2
Cytoplasm, cytosol 2 LIPE, NLRP3
endosome 1 HMGB1
plasma membrane 8 BCHE, BMP2, CACNA1I, HMGB1, IFNLR1, IGHE, JAK2, KNG1
Membrane 7 BCL2, CACNA1I, IFNLR1, JAK2, LIPE, LMNB1, NLRP3
caveola 2 JAK2, LIPE
extracellular exosome 2 KNG1, MLLT3
endoplasmic reticulum 3 BCL2, HMGB1, NLRP3
extracellular space 7 BCHE, BMP2, HMGB1, IGHE, IL5, KNG1, XDH
perinuclear region of cytoplasm 1 ATN1
mitochondrion 2 BCL2, NLRP3
protein-containing complex 1 BCL2
intracellular membrane-bounded organelle 2 BMP2, DPF2
Single-pass type I membrane protein 2 IFNLR1, IGHE
Secreted 6 BCHE, BMP2, HMGB1, IL5, NLRP3, PLA2G12A
extracellular region 8 BCHE, BMP2, HMGB1, IGHE, IL5, KNG1, NLRP3, PLA2G12A
cytoplasmic side of plasma membrane 1 JAK2
Mitochondrion outer membrane 1 BCL2
Single-pass membrane protein 1 BCL2
mitochondrial outer membrane 1 BCL2
Extracellular side 1 HMGB1
anchoring junction 1 ATN1
transcription regulator complex 1 KLF4
Nucleus membrane 1 BCL2
Bcl-2 family protein complex 1 BCL2
nuclear membrane 2 BCL2, LMNB1
dendritic spine 1 ZMYND8
microtubule cytoskeleton 1 KLF4
nucleolus 1 ZMYND8
Membrane raft 1 JAK2
pore complex 1 BCL2
focal adhesion 1 JAK2
Peroxisome 1 XDH
sarcoplasmic reticulum 1 XDH
collagen-containing extracellular matrix 1 KNG1
intermediate filament 1 LMNB1
Cytoplasm, cytoskeleton, microtubule organizing center 1 NLRP3
Inflammasome 1 NLRP3
interphase microtubule organizing center 1 NLRP3
NLRP3 inflammasome complex 1 NLRP3
nuclear inner membrane 1 LMNB1
chromatin 3 DPF2, KLF4, ZMYND8
IgE immunoglobulin complex 1 IGHE
Chromosome 3 HMGB1, MLLT3, ZMYND8
cytoskeleton 1 JAK2
Secreted, extracellular space 1 KNG1
blood microparticle 2 BCHE, KNG1
[Isoform 2]: Cell membrane 1 IGHE
nuclear envelope 1 LMNB1
Endomembrane system 2 JAK2, NLRP3
endosome lumen 1 JAK2
Lipid droplet 1 LIPE
Membrane, caveola 1 LIPE
microtubule organizing center 1 NLRP3
euchromatin 2 JAK2, KLF4
myelin sheath 1 BCL2
ficolin-1-rich granule lumen 1 HMGB1
secretory granule lumen 1 HMGB1
endoplasmic reticulum lumen 2 BCHE, KNG1
nuclear matrix 2 ATN1, LMNB1
transcription repressor complex 1 HMGB1
platelet alpha granule lumen 1 KNG1
voltage-gated calcium channel complex 1 CACNA1I
transcription elongation factor complex 1 MLLT3
nBAF complex 1 DPF2
SWI/SNF complex 1 DPF2
nuclear envelope lumen 1 BCHE
nuclear lamina 1 LMNB1
endoplasmic reticulum-Golgi intermediate compartment 1 HMGB1
extrinsic component of cytoplasmic side of plasma membrane 1 JAK2
condensed chromosome 1 HMGB1
extrinsic component of plasma membrane 1 JAK2
granulocyte macrophage colony-stimulating factor receptor complex 1 JAK2
interleukin-12 receptor complex 1 JAK2
interleukin-23 receptor complex 1 JAK2
site of DNA damage 1 ZMYND8
[Isoform 3]: Cell membrane 1 IGHE
[Isoform 1]: Secreted 1 IGHE
IgE B cell receptor complex 1 IGHE
immunoglobulin complex, circulating 1 IGHE
Nucleus lamina 1 LMNB1
lamin filament 1 LMNB1
alphav-beta3 integrin-HMGB1 complex 1 HMGB1
BAD-BCL-2 complex 1 BCL2
BMP receptor complex 1 BMP2
interleukin-28 receptor complex 1 IFNLR1


文献列表

  • Mark J Henderson, Kathleen A Trychta, Shyh-Ming Yang, Susanne Bäck, Adam Yasgar, Emily S Wires, Carina Danchik, Xiaokang Yan, Hideaki Yano, Lei Shi, Kuo-Jen Wu, Amy Q Wang, Dingyin Tao, Gergely Zahoránszky-Kőhalmi, Xin Hu, Xin Xu, David Maloney, Alexey V Zakharov, Ganesha Rai, Fumihiko Urano, Mikko Airavaara, Oksana Gavrilova, Ajit Jadhav, Yun Wang, Anton Simeonov, Brandon K Harvey. A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. Cell reports. 2021 04; 35(4):109040. doi: 10.1016/j.celrep.2021.109040. [PMID: 33910017]
  • Tobie D Lee, Olivia W Lee, Kyle R Brimacombe, Lu Chen, Rajarshi Guha, Sabrina Lusvarghi, Bethilehem G Tebase, Carleen Klumpp-Thomas, Robert W Robey, Suresh V Ambudkar, Min Shen, Michael M Gottesman, Matthew D Hall. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology. 2019 11; 96(5):629-640. doi: 10.1124/mol.119.115964. [PMID: 31515284]
  • Seung-Hyun Jeong, Ji-Hun Jang, Yong-Bok Lee. A novel and sensitive UPLC-MS/MS method to determine mequitazine in rat plasma and urine: Validation and its application to pharmacokinetic studies. Biomedical chromatography : BMC. 2019 Oct; 33(10):e4627. doi: 10.1002/bmc.4627. [PMID: 31222787]
  • Sung-Hoon Ahn, Han-Joo Maeng. Quantification of mequitazine in human plasma by gas chromatography- quadrupole mass spectrometry and its application to a human pharmacokinetic study. Biomedical chromatography : BMC. 2016 Apr; 30(4):574-8. doi: 10.1002/bmc.3585. [PMID: 26268745]
  • Hironori Sagara, Tatsuo Yukawa, Ryuichi Kashima, Takenori Okada, Takeshi Fukuda. Effects of pranlukast hydrate on airway hyperresponsiveness in non-asthmatic patients with Japanese cedar pollinosis. Allergology international : official journal of the Japanese Society of Allergology. 2009 Jun; 58(2):277-87. doi: 10.2332/allergolint.08-oa-0058. [PMID: 19390239]
  • Oh-Seung Kwon, Hye-Jung Kim, Heesoo Pyo, Suk-Jae Chung, Youn Bok Chung. Determination of mequitazine in human plasma by gas-chromatography/mass spectrometry with ion-trap detector and its pharmacokinetics after oral administration to volunteers. Archives of pharmacal research. 2005 Oct; 28(10):1190-5. doi: 10.1007/bf02972985. [PMID: 16276978]
  • P Casha, O Bernard, M C Galland, P Pisano, I Koné-Paut, R Vialet, A Durand, J L Bernard. [Status epilepticus in an asthmatic child]. Archives de pediatrie : organe officiel de la Societe francaise de pediatrie. 1994 Sep; 1(9):816-8. doi: . [PMID: 7842125]
  • K Tasaka, M Akagi, M Mio, K Izushi, I Aoki. Anti-platelet activating factor, anti-leukotriene D4 and some other antiallergic activities of mequitazine. Arzneimittel-Forschung. 1990 Oct; 40(10):1092-7. doi: . [PMID: 1705425]
  • T Hasegawa, K Takagi, T Kuzuya, M Nadai, R Apichartpichean, I Muraoka. Effect of mequitazine on the pharmacokinetics of theophylline in asthmatic patients. European journal of clinical pharmacology. 1990; 38(3):255-8. doi: 10.1007/bf00315026. [PMID: 2340844]
  • A Malet i Casajuana, J Ruiz de León, A Valero Santiago, J Sanosa Valls, M Zamorano Calderón, P A García Calderón. "In vivo" and "in vitro" evaluation of four antihistamines (astemizole, azatadine, mequitazine, terfenadine). Allergologia et immunopathologia. 1989 Mar; 17(2):85-93. doi: . [PMID: 2476015]
  • P Ylitalo, K Nieminen, G Wilén-Rosenqvist, J B Fourtillan, J Girault, L Ylitalo, J S Pukander, P H Karma. Serum levels and urinary excretion of mequitazine after a single oral dose. International journal of clinical pharmacology research. 1989; 9(5):305-8. doi: . [PMID: 2576245]
  • J B Fourtillan, J Girault, S Bouquet, M A Lefèbvre. Determination of mequitazin in human plasma and urine by capillary column gas-liquid chromatography-mass spectrometry. Journal of chromatography. 1984 Aug; 309(2):391-6. doi: 10.1016/0378-4347(84)80048-1. [PMID: 6148351]
  • J Demaubeuge, D Tennstedt, R Broux. Does mast cell protection plus mediator antagonism surpass the effect of a classic antihistaminic in the treatment of chronic urticaria? A double-blind comparison of oxatomide and mequitazine. Dermatologica. 1982 Jun; 164(6):386-94. doi: 10.1159/000250123. [PMID: 6126399]
  • J Yano, H Igo, K Shiraiwa, M Miura, H Watanabe, T Morino, K Matsumoto, K Hayano. [Subacute toxicity and recovery tests of mequitazine in beagle dogs (author's transl)]. The Journal of toxicological sciences. 1981 May; 6(2):129-57. doi: 10.2131/jts.6.129. [PMID: 6115947]
  • A Uzan, C Gueremy, G Le Fur. [Biotransformation of 10-(3-quinuclidinylmethyl)phenothiazine (LM 209), a new anti-allergy agent and the distribution and excretion of its metabolites]. Xenobiotica; the fate of foreign compounds in biological systems. 1976 Nov; 6(11):649-65. doi: 10.3109/00498257609151678. [PMID: 997584]