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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/05/24 19:23:19」(JST)
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Linsidomine
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| Systematic (IUPAC) name |
| 5-imino-3-morpholin-4-yl-5H-1,2,3-oxadiazol-3-ium-2-ide |
| Clinical data |
| AHFS/Drugs.com |
International Drug Names |
| Legal status |
? |
| Identifiers |
| ATC code |
C01DX18 |
| PubChem |
CID 5219 |
| UNII |
5O5U71P6VQ Y |
| KEGG |
D07161 Y |
| Synonyms |
SIN-1 |
| Chemical data |
| Formula |
C6H10N4O2 |
| Mol. mass |
170.17 g/mol |
| Y (what is this?) (verify) |
Linsidomine (3-morpholinosydnonimine or SIN-1[1]) is a vasodilator. It is a metabolite of the antianginal drug molsidomine and acts by releasing NO from the endothelial cells nonenzymatically. It also hyperpolarizes the cell membrane through influencing the sodium-potassium pump and thereby rendering it less responsive to adrenergic stimulation. Linsidomine injection at a dose of 1 mg produces usable erection[2] in about 70% of patients and full erection in up to 50% of patients. Linsidomine does not appear to be associated with priapism.[citation needed]
Linsidomine is neurotoxic and promotes oxidative stress on neurons.[3] Linsidomine is a peroxynitrite-generating compound involved in the pathogenesis of neurodegenerative diseases.[4]
References
- ^ Wen, TC.; Rogido, MR.; Moore, JE.; Genetta, T.; Peng, H.; Sola, A. (Oct 2005). "Cardiotrophin-1 protects cortical neuronal cells against free radical-induced injuries in vitro.". Neurosci Lett 387 (1): 38–42. doi:10.1016/j.neulet.2005.07.018. PMID 16084018.
- ^ Lemaire, A.; Buvat, J. (1998). "Erectile response to intracavernous injection of linsidomine in 38 impotent patients. Comparison with prostaglandin E1". Progres en urologie : journal de l'Association francaise d'urologie et de la Societe francaise d'urologie 8 (3): 388–391. PMID 9689672. edit
- ^ Wallace, DR.; Dodson, S.; Nath, A.; Booze, RM. (Jan 2006). "Estrogen attenuates gp120- and tat1-72-induced oxidative stress and prevents loss of dopamine transporter function.". Synapse 59 (1): 51–60. doi:10.1002/syn.20214. PMID 16237680.
- ^ Jang, JH.; Aruoma, OI.; Jen, LS.; Chung, HY.; Surh, YJ. (Feb 2004). "Ergothioneine rescues PC12 cells from beta-amyloid-induced apoptotic death.". Free Radic Biol Med 36 (3): 288–99. doi:10.1016/j.freeradbiomed.2003.11.005. PMID 15036348.
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Vasodilators used in cardiac diseases (C01D)
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| Nitrovasodilators |
- Glyceryl trinitrate #
- Isosorbide dinitrate #
- Isosorbide mononitrate
- Linsidomine
- Molsidomine
- Nicorandil
- Pentaerythritol tetranitrate
- Propatylnitrate
- Tenitramine
- Trolnitrate
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| Quinolone vasodilators |
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| Others |
- Benziodarone
- Carbocromen
- Cinepazet
- Cloridarol
- Dilazep
- Efloxate
- Etafenone
- Gapicomine
- Heptaminol
- Hexobendine
- Imolamine
- Itramin tosilate
- Levosimendan
- Nesiritide
- Nicorandil
- Oxyfedrine
- Pimobendan
- Prenylamine
- Serelaxin
- Trapidil
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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noco/cong/tumr, sysi/epon, injr
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proc, drug (C1A/1B/1C/1D), blte
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English Journal
- S-nitrosoglutathione reduces tau hyper-phosphorylation and provides neuroprotection in rat model of chronic cerebral hypoperfusion.
- Won JS1, Annamalai B1, Choi S2, Singh I2, Singh AK3.
- Brain research.Brain Res.2015 Oct 22;1624:359-69. doi: 10.1016/j.brainres.2015.07.057. Epub 2015 Aug 10.
- We have previously reported that treatment of rats subjected to permanent bilateral common carotid artery occlusion (pBCCAO), a model of chronic cerebral hypoperfusion (CCH), with S-nitrosoglutathione (GSNO), an endogenous nitric oxide carrier, improved cognitive functions and decreased amyloid-β a
- PMID 26271717
- Male Rat Germ Cells Display Age-Dependent and Cell-Specific Susceptibility in Response to Oxidative Stress Challenges.
- Selvaratnam J1, Paul C1, Robaire B2.
- Biology of reproduction.Biol Reprod.2015 Sep;93(3):72. doi: 10.1095/biolreprod.115.131318. Epub 2015 Jul 29.
- For decades male germ cells were considered unaffected by aging, due to the fact that males continue to generate sperm into old age; however, evidence indicates that germ cells from aged males are of lower quality than those of young males. The current study examines the effects of aging on pachyten
- PMID 26224006
- Beneficial effect of a nitric oxide donor in an ex vivo model of pig-to-human pulmonary xenotransplantation.
- Park HS1, Kim JE1,2, You HJ1,2, Gu J1,2, Yoo B3, Lee S2, Lee HJ2,3, Hwang HY2,3, Hwang Y2,3, Kim HK1,2, Kim YT2,3.
- Xenotransplantation.Xenotransplantation.2015 Sep;22(5):391-8. doi: 10.1111/xen.12195.
- BACKGROUND: Nitric oxide (NO) can reduce platelet adhesion and vascular resistance. Tempol can scavenge the reactive oxygen species (ROS) that induce tissue injury. As xenograft rejection attenuates endogenous NO production and generates ROS, we evaluated the potential effect of an NO donor (SIN-1,
- PMID 26381495
Japanese Journal
- Neoechinulin A Imparts Resistance to Acute Nitrosative Stress in PC12 Cells: A Potential Link of an Elevated Cellular Reserve Capacity for Pyridine Nucleotide Redox Turnover with Cytoprotection
- Geniposide Induces the Expression of Heme Oxygenase-1 via PI3K/Nrf2-Signaling to Enhance the Antioxidant Capacity in Primary Hippocampal Neurons
- Inhibitory Effects of Nitrative Stress on the Sulfation of 17.BETA.-Estradiol and 4-Methoxyestradiol by Human MCF 10A Mammary Epithelial Cells
★リンクテーブル★
[★]
- 英
- 3-morpholinosydnonimine
[★]
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