3612-14-4Relevant articles and documents
Fentanyl family at the mu-opioid receptor: Uniform assessment of binding and computational analysis
Lipiński, Piotr F.J.,Kosson, Piotr,Matalińska, Joanna,Roszkowski, Piotr,Czarnocki, Zbigniew,Jarończyk, Ma?gorzata,Misicka, Aleksandra,Dobrowolski, Jan Cz.,Sadlej, Joanna
, (2019/02/26)
Interactions of 21 fentanyl derivatives with μ-opioid receptor (μOR) were studied using experimental and theoretical methods. Their binding to μOR was assessed with radioligand competitive binding assay. A uniform set of binding affinity data contains val
New antihistaminic N-heterocyclic 4-piperidinamines. 1. Synthesis and antihistaminic activity of N-(4-piperidinyl)-1H-benzimidazol-2-amines
Janssens,Torremans,Janssen,Stokbroekx,Luyckx
, p. 1925 - 1933 (2007/10/02)
The synthesis of a series N-(4-piperidinyl)-1H-benzimidazol-2-amines and the preliminary evaluation of their in vitro and in vivo antihistaminic activity are described. Cyclodesulfurization of (2-aminophenyl) thioureas with mercury(II) oxide resulted in 2-aminobenzimidazole intermediates, which were monoalkylated on the endo-nitrogen atom. After deprotection of the piperideine nitrogen atom with 48% aqueous hydrobromic acid solution, the title compounds were obtained by three different methods, viz. alkylation, reductive amination, or oxirane ring-opening reactions. The in vivo antihistaminic activity was evaluated by the compound 48/80 induced lethality test in rats and histamine-induced lethality test in guinea pigs after oral and/or subcutaneous administration. The duration of action, for a selected number of compounds, was studied in the guinea pig. The phenylethyl derivatives showed the most potent antihistamine properties after oral administration in both animal species.