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Chemical Compound Review:

AC1O5PMW but-2-enedioic acid; (8S,10R,13S,14S,16R...

Synonyms: U-75412E, U75412E, U 75412E, 130590-09-9

This record was replaced with 3035460.

Huang, S.H. et al., Wang, S. et al., Wang, S. et al., Choi, M. et al., Dyess, D.L. et al., et al.

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Disease relevance of (8S,10S,13S,14S,16R,17S)-17-[2-[4-(3-ethylamino-2-pyridyl)piperazin-1-yl]acetyl]-10,13,16-trimethyl-6,7,8,12,14,15,16,17-octahydrocyclopenta[a]phenanthren-3-one

U75412E prevented progressive burn ischemia and the expansion of tissue loss [1].
In a simulated fire-related smoke exposure protocol, New Zealand white rabbits were utilized to investigate the potential effects of the 21-aminosteroid (lazaroid) analog U75412E on the early events of acute lung injury [2].
Retinal toxicity of intravitreal lazaroid (21-aminosteroid U75412E) [3].
Histopathology indicated that 16 mM U75412E pretreatment attenuated increases in wet lung/body weight ratios, inflammatory focus, and interstitial oedema associated with smoke insult [4].
Inhalation of total of 4.6 mg U75412E aerosolized at a rate of 1.53 mg/min for 3 min before or after smoke significantly prevented or limited the extent of alveolar hypoventilation, interstitial edema, and tumor necrosis factor-alpha (TNF-alpha) by pulmonary alveolar macrophages (PAM) ex vivo observed at 2 h [5].

High impact information on (8S,10S,13S,14S,16R,17S)-17-[2-[4-(3-ethylamino-2-pyridyl)piperazin-1-yl]acetyl]-10,13,16-trimethyl-6,7,8,12,14,15,16,17-octahydrocyclopenta[a]phenanthren-3-one

U75412E, a lipid peroxidation inhibitor, preserved vascular patency, restored blood flow, prevented a rise in tissue conjugated dienes, and maintained tissue viability in the interspaces [1].
Antioxidant activity of lazaroid (U-75412E) and its protective effects against crystalline silica-induced cytotoxicity [6].
Lazaroid (U-75412E) scavenges .OH radicals generated by crystalline silica-mediated reaction from H2O2 and inhibits lipid peroxidation in macrophages induced by these particles [6].
LDH release was significantly attenuated at a dose of 1 x 10(-5) M for the U75412E treated myocytes and at 1 x 10(-5) and 1 x 10(-6) M for the U74500E treated myocytes compared to the myocytes not pretreated with a lazaroid and exposed to free radicals [7].
Cytotoxicity of lazaroid U-75412E in human epithelial cell line (Wish) [8].

Biological context of (8S,10S,13S,14S,16R,17S)-17-[2-[4-(3-ethylamino-2-pyridyl)piperazin-1-yl]acetyl]-10,13,16-trimethyl-6,7,8,12,14,15,16,17-octahydrocyclopenta[a]phenanthren-3-one

Alveolar macrophages treated with lazaroid (U-75412E) before crystalline silica exposure were protected against cell injury and lipid peroxidation as demonstrated by those indicators [6].
However, U75412E did not attenuate smoke-induced changes in BAL concentration of tumor necrosis factor-alpha, total cell count, and granulocyte percentage [2].
U75412E administered before the injury was effective in limiting the alterations in microvascular permeability [9].

Anatomical context of (8S,10S,13S,14S,16R,17S)-17-[2-[4-(3-ethylamino-2-pyridyl)piperazin-1-yl]acetyl]-10,13,16-trimethyl-6,7,8,12,14,15,16,17-octahydrocyclopenta[a]phenanthren-3-one

In this study, 21-aminosteroid U75412E was injected into the vitreous body of rabbit eyes to evaluate its suitability for intraocular injection and its toxicity on intraocular tissues [3].
In this paper, we show that a novel antioxidant (lazaroid U75412E, a free radical scavenger) suppressed mitogen-induced T cell proliferation in vitro [10].

Associations of (8S,10S,13S,14S,16R,17S)-17-[2-[4-(3-ethylamino-2-pyridyl)piperazin-1-yl]acetyl]-10,13,16-trimethyl-6,7,8,12,14,15,16,17-octahydrocyclopenta[a]phenanthren-3-one with other chemical compounds

We evaluated the effects of two lazaroid compounds (U74389F and U75412E) on alterations in microvascular permeability that resulted from burn injuries [9].

References

U75412E, a lazaroid, prevents progressive burn ischemia in a rat burn model. Choi, M., Ehrlich, H.P. Am. J. Pathol. (1993) [Pubmed]
Early alterations of lung injury following acute smoke exposure and 21-aminosteroid treatment. Wang, S., Lantz, R.C., Robledo, R.F., Breceda, V., Hays, A.M., Witten, M.L. Toxicologic pathology. (1999) [Pubmed]
Retinal toxicity of intravitreal lazaroid (21-aminosteroid U75412E). Cruz, S.A., Karaçorlu, M., Peyman, G.A. International ophthalmology. (1992) [Pubmed]
The prophylactic effects of U75412E pretreatment in a smoke-induced lung injury rabbit model. Wang, S., Lantz, R.C., Chen, G.J., Breceda, V., Rider, E., Hays, A.M., Parliman, G., Tollinger, B.J., Robledo, R.F., Kunke, K., Tinajero, J., Witten, M.L. Pharmacol. Toxicol. (1996) [Pubmed]
A free radical scavenger (Lazaroid U75412E) attenuates tumor necrosis factor-alpha generation in a rabbit model of smoke-induced lung injury. Wang, S., Lantz, R.C., Rider, E.D., Chen, G.J., Breceda, V., Hays, A.M., Robledo, R.F., Tollinger, B.J., Dinesh, S.V., Witten, M.L. Respiration; international review of thoracic diseases. (1997) [Pubmed]
Antioxidant activity of lazaroid (U-75412E) and its protective effects against crystalline silica-induced cytotoxicity. Huang, S.H., Leonard, S., Shi, X., Goins, M.R., Vallyathan, V. Free Radic. Biol. Med. (1998) [Pubmed]
Effects of 21-aminosteroids in neonatal rat cardiac myocyte cell cultures exposed to free radicals. Burton, K.P. Cardiovasc. Res. (1994) [Pubmed]
Cytotoxicity of lazaroid U-75412E in human epithelial cell line (Wish). Mattana, A., Bennardini, F., Juliano, C., Picci, V., Marceddu, S., Sciola, L., Pippia, P., Franconi, F. Biochem. Pharmacol. (1994) [Pubmed]
Modulation of microvascular permeability by 21-aminosteroids after burn injuries. Dyess, D.L., Collins, J.N., Ardell, J.L., Townsley, M.I., Taylor, A.E., Ferrara, J.J. The Journal of burn care & rehabilitation. (2000) [Pubmed]
Suppressive effects of a novel antioxidant compound on human T cell functions in vitro. Kalsi, J.K., Clay, K., Rickard, D., Hall, N.D. Agents Actions (1993) [Pubmed]

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