5685-72-3Relevant articles and documents
3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α2-adrenoceptor compared to the imidazoline I1 receptor
Sczewski, Franciszek,Kornicka, Anita,Hudson, Alan L.,Laird, Shayna,Scheinin, Mika,Laurila, Jonne M.,Rybczyńska, Apolonia,Boblewski, Konrad,Lehmann, Artur,Gdaniec, Maria
scheme or table, p. 321 - 329 (2011/02/26)
A series of 3-[(4,5-dihydroimidazolidin-2-yl)imino]indazoles has been synthesized as positional analogues of marsanidine, a highly selective α2-adrenoceptor ligand. Parent compound 4a and its 4-chloro (4c) and 4-methyl (4d) derivatives display α2-adrenoceptor affinity at nanomolar concentrations (Ki = 39.4, 15.9 and 22.6 nM, respectively) and relatively high α2/I1 selectivity ratios of 82, 115 and 690, respectively. Evidence was obtained that these compounds act as partial agonists at α2A-adrenoceptors. Compound 4d with intrinsic activity comparable with that of marsanidine, but lower than that of clonidine, elicited pronounced cardiovascular effects in anesthetized rats at doses as low as 0.01 mg/kg iv.
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists
Vasudevan, Anil,Souers, Andrew J.,Freeman, Jennifer C.,Verzal, Mary K.,Gao, Ju,Mulhern, Mathew M.,Wodka, Derek,Lynch, John K.,Engstrom, Kenneth M.,Wagaw, Seble H.,Brodjian, Sevan,Dayton, Brian,Falls, Doug H.,Bush, Eugene,Brune, Michael,Shapiro, Robin D.,Marsh, Kennan C.,Hernandez, Lisa E.,Collins, Christine A.,Kym, Philip R.
, p. 5293 - 5297 (2007/10/03)
The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100 nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.
