221121-29-5Relevant academic research and scientific papers
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (σ2) receptor ligands
Banister, Samuel D.,Rendina, Louis M.,Kassiou, Michael
supporting information; experimental part, p. 4059 - 4063 (2012/07/03)
A series of N-substituted 7-azabicyclo[2.2.1]heptanes (12-17 and 22-25) and similarly substituted pyrrolidines (32-36 and 41-44) were synthesized as sterically-reduced, achiral analogs of adamantane- and trishomocubane-derived σ ligands. In vitro competition binding assays against σ receptors revealed that arylalkyl N-substituents conferred selectivity for the σ2 subtype, while alicyclic or polycarbocyclic substituents imparted high affinity for both subtypes. The σ2 binding and subtype selectivities of N-arylalkyl-7-azanorbornanes was generally greater than the analogously-substituted pyrrolidines, indicating that steric bulk and conformational restriction around the nitrogen atom are likely important for subtype discrimination.
New Tetracyclic Derivatives of Imidazobenzodiazepines and of Imidazothienodiazepines
Gerecke, Max,Kyburz, Emilio,Borer, Rene,Gassner, Walter
, p. 693 - 722 (2007/10/02)
The synthesis of new tetracyclic 1,4-diazepine derivatives is described.In these compounds, an additional five-membered heterocycle is fused on the known tricyclic ring systems imidazobenzodiazepine and imidazothienodiazepine.Many of these new compounds display a very high affinity to the benzodiazepine receptor in mammals.
