Literature summary for 7.1.1.2 extracted from

Radeke, H.; Hanson, K.; Yalamanchili, P.; Hayes, M.; Zhang, Z.Q.; Azure, M.; Yu, M.; Guaraldi, M.; Kagan, M.; Robinson, S.; Casebier, D.
Synthesis and biological evaluation of the mitochondrial complex 1 inhibitor 2-[4-(4-fluorobutyl)benzylsulfanyl]-3-methylchromene-4-one as a potential cardiac positron emission tomography tracer (2007), J. Med. Chem., 50, 4304-4315.

Search for more literature for 7.1.1.2

Application

Application	Comment	Organism
medicine	radiolabeled MC-I inhibitors as potential myocardial perfusion imaging agents	Rattus norvegicus

Inhibitors

Inhibitors	Comment	Organism	Structure
2-(4-butylbenzylamino)-3-methylchromen-4-one	-	Rattus norvegicus
2-(4-butylbenzyloxy)-3-methylchromen-4-one	-	Rattus norvegicus
2-[(4-butylbenzyl)sulfanyl]-3-methyl-4H-chromen-4-one	-	Rattus norvegicus
2-[4-(4-fluorobutyl)benzylamino]-3-methylchromen-4-one	-	Rattus norvegicus
2-[4-(4-fluorobutyl)benzyloxy]-3-methylchromen-4-one	-	Rattus norvegicus
2-[4-(4-fluorobutyl)benzylsulfanyl]-3-methylchromen-4-one	most potent inhibitor. 30 min after high uptake of the radiotracer from the blood pool into the myocardium, kidney, and liver. After 2 h about 66% of the activity in the myocardium at 30 min has been retained, whereas ca. 70% has been cleared from the liver and kidney	Rattus norvegicus
fenazaquin	-	Rattus norvegicus
pyridaben	-	Rattus norvegicus
rotenone	-	Rattus norvegicus
[2-(4-butyl)benzylsulfanyl]-3-methylchromen-4-one	-	Rattus norvegicus

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
mitochondrion	-	Rattus norvegicus	5739	-

Organism

Organism	UniProt	Comment	Textmining
Rattus norvegicus	-	Sprague-Dawley rats	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
kidney	-	Rattus norvegicus	-
liver	-	Rattus norvegicus	-
myocardium	-	Rattus norvegicus	-

Synonyms

Synonyms	Comment	Organism
complex I	-	Rattus norvegicus
MC-I	-	Rattus norvegicus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.008	-	-	Rattus norvegicus	pyridaben
0.009	-	-	Rattus norvegicus	2-[4-(4-fluorobutyl)benzylsulfanyl]-3-methylchromen-4-one
0.016	-	-	Rattus norvegicus	rotenone
0.033	-	-	Rattus norvegicus	2-[4-(4-fluorobutyl)benzyloxy]-3-methylchromen-4-one
0.052	-	-	Rattus norvegicus	[2-(4-butyl)benzylsulfanyl]-3-methylchromen-4-one
0.052	-	-	Rattus norvegicus	2-[(4-butylbenzyl)sulfanyl]-3-methyl-4H-chromen-4-one
0.057	-	-	Rattus norvegicus	2-(4-butylbenzylamino)-3-methylchromen-4-one
0.06	-	-	Rattus norvegicus	2-(4-butylbenzyloxy)-3-methylchromen-4-one
0.09	-	-	Rattus norvegicus	fenazaquin
0.133	-	-	Rattus norvegicus	2-[4-(4-fluorobutyl)benzylamino]-3-methylchromen-4-one

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Release 2023.1 (January 2023)