185507-79-3Relevant academic research and scientific papers
Spiro[1,2,4-benzotriazine-3(4H),4′-(1′-substituted)piperidines] and related compounds as ligands for sigma receptors
Novelli, Federica,Sparatore, Fabio
, p. 871 - 882 (2007/10/03)
As analogues of some conformationally restricted spiropiperidine derivatives which are endowed with high affinity for σ1 receptor, a set of 16 spiro[1,2,4-benzotriazine-3(4H),4′-(1′-substituted)piperidines] and congeneric compounds was prepared and tested for affinity to σ1 receptor subtype. All N-arylalkyl substituted derivatives exhibited high affinity for the relevant receptor, with Ki in the low nanomolar range. Affinity for σ2 subtype (assayed only for a few representative compounds) was from one to three order of magnitude lower. Spiro[1,2,4-benzotriazine-3(4H),4′-(1′-benzyl)piperidine] (2), with a ratio Kiσ2/Kiσ1=7000 should represent the most selective σ1 ligand so far described.
Preparation and pharmacological activities of spiro[3,4-dihydro-6/7-R-1,2,4-benzotriazine-3,4'-(1'-substituted)piper idines]
Novelli,Sparatore
, p. 541 - 550 (2007/10/03)
A set of spiro[3,4-dihydro-1,2,4-benzotriazines-3,4'-piperidine] derivatives was prepared and subjected to a broad pharmacological screening. Many of these compounds are characterized by a 3-(4-fluorobenzoyl)propyl substituent on the piperidine nitrogen, thus resembling the p-fluorobutyrophenone antipsychotics. Modest dopamine antagonism was observed for the tested compounds, which however were mainly endowed with analgesic and antihypertensive activities. Antihypercholesterolemic activity was also seen in compound 5, which represents an interesting new lead, being completely structurally unrelated to the known agents in this field.
