151917-39-4Relevant articles and documents
Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator
Ritzen, Andreas,Sindet, Rikke,Hentzer, Morten,Svendsen, Nannette,Brodbeck, Robbin M.,Bundgaard, Christoffer
supporting information; experimental part, p. 3275 - 3278 (2010/03/24)
This Letter describes the discovery of a novel series of mGluR5 positive allosteric modulators (PAMs). The lead compound, 11c, exhibits excellent potency (EC50 = 30 nM) in vitro, and reaches high brain levels in both rats and mice after oral ad
Evaluation of radiolabeled (Hetero)aromatic analogues of N-(2-diethylaminoethyl)-4-iodobenzamide for imaging and targeted radionuclide therapy of melanoma
Chezal, Jean-Michel,Papon, Janine,Labarre, Pierre,Lartigue, Claire,Galmier, Marie-Josephe,Decombat, Caroline,Chavignon, Olivier,Maublant, Jean,Teulade, Jean-Claude,Madelmont, Jean-Claude,Moins, Nicole
experimental part, p. 3133 - 3144 (2009/04/07)
Targeted radionuclide therapy using radioiodinated compounds with a specific affinity for melanoma tissue is a promising treatment for disseminated melanoma, but the candidate with the ideal kinetic profile remains to be discovered. Targeted radionuclide therapy concentrates the effects on tumor cells, thereby increasing the efficacy and decreasing the morbidity of radiotherapy. In this context, analogues of N-(2-diethylaminoethyl)-4- iodobenzamide (BZA) are of interest. Various (hetero)aromatic analogues 5 of BZA were synthesized and radioiodinated with 125I, and their biodistribution in melanoma-bearing mice was studied after i.v. administration. Most [125I]5-labeled compounds appeared to bind specifically and with moderate-to-high affinity to melanoma tumor. Two compounds, 5h and 5k, stood out with high specific and long-lasting uptake in the tumor, with a 7- and 16-fold higher value than BZA at 72 h, respectively, and kinetic profiles that makes them promising agents for internal targeted radionuclide therapy of melanoma.
Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity
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Page column 18, (2010/01/30)
Compounds of the formula where R1and R2, independently are alkyl groups having 2 to 8 carbons; R3is hydrogen or lower alkyl; X is S, O or N—R4where R4is hydrogen or lower alkyl; Y is phenyl or pyridyl