- Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for central σ1 receptors and comparison with fluoroalkyl homologs
-
The spirocyclic σ1 receptor ligand 1 (1′-benzyl-3- (fluoromethyl)-3H-spiro[[2]benzofuran-1,4′-piperidine]) was prepared in four steps starting from methoxy derivative 5. Due to its high σ1 affinity (Ki = 0.74 nM) and selec
- Maisonial, Aurélie,Gro?e Maestrup, Eva,Wiese, Christian,Hiller, Achim,Schepmann, Dirk,Fischer, Steffen,Deuther-Conrad, Winnie,Steinbach, J?rg,Brust, Peter,Wünsch, Bernhard
-
p. 257 - 269
(2012/03/26)
-
- SPIRO-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENES
-
The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
- -
-
Page/Page column 25
(2010/06/11)
-