202401-38-5Relevant academic research and scientific papers
Inhibition of tumor growth
-
Page/Page column 35, (2015/09/22)
The present invention provides a cytotoxic 7 to 25 mer peptide with three or more cationic residues which has one or more non-genetic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of p
Production of new amilorides as potent inhibitors of mitochondrial respiratory complex I
Murai, Masatoshi,Habu, Sayako,Murakami, Sonomi,Ito, Takeshi,Miyoshi, Hideto
, p. 1061 - 1066 (2015/10/05)
Amilorides, well-known inhibitors of Na+/H+ antiporters, have also shown to inhibit bacterial and mitochondrial NADH-quinone oxidoreductase (complex I). Since the membrane subunits ND2, ND4, and ND5 of bovine mitochondrial complex I
WEIGHT REDUCING COMPOUNDS
-
Page/Page column 17, (2009/09/04)
The present invention relates to compounds which find use as weight reducing agents, and find use in treating obesity and/or excess adiposity.
Radiolabeled phenethylguanidines: Novel imaging agents for cardiac sympathetic neurons and adrenergic tumors
Raffel, David M.,Jung, Yong-Woon,Gildersleeve, David L.,Sherman, Phillip S.,Moskwa, James J.,Tluczek, Louis J.,Chen, Wei
, p. 2078 - 2088 (2008/02/02)
The norepinephrine transporter (NET) substrates [123I]-m- iodobenzylguanidine (MIBG) and [11C]-m-hydroxyephedrine (HED) are used as markers of cardiac sympathetic neurons and adrenergic tumors (pheochromocytoma, neuroblastoma). However, their rapid NET transport rates limit their ability to provide accurate measurements of cardiac nerve density. [11C]Phenethylguanidine ([11C]1a) and 12 analogues ([ 11C]-1b-m) were synthesized and evaluated as radiotracers with improved kinetics for quantifying cardiac nerve density. In isolated rat hearts, neuronal uptake rates of [11C]1a-m ranged from 0.24 to 1.96 mL min-1 (g wet wt)-1, and six compounds had extremely long neuronal retention times (clearance T1/2 > 20 h) due to efficient vesicular storage. Positron emission tomography (PET) studies in nonhuman primates with [11C]-1e, N-[11C]guanyl-m-octopamine, which has a slow NET transport rate, showed improved myocardial kinetics compared to HED. Compound [11C]1c, [11C]-p-hydroxyphenethylguanidine, which has a rapid NET transport rate, avidly accumulated into rat pheochromocytoma xenograft tumors in mice. These encouraging findings demonstrate that radiolabeled phenethylguanidines deserve further investigation as radiotracers of cardiac sympathetic innervation and adrenergic tumors.
