1160004-82-9Relevant academic research and scientific papers
Tricyclic Triazoles as σ1Receptor Antagonists for Treating Pain
Díaz, José Luis,Cuevas, Félix,Oliva, Ana I.,Font, Daniel,Sarmentero, M. ángeles,álvarez-Bercedo, Paula,López-Valbuena, José M.,Pericàs, Miquel A.,Enrech, Raquel,Montero, Ana,Yeste, Sandra,Vidal-Torres, Alba,álvarez, Inés,Pérez, Pilar,Cendán, Cruz Miguel,Cobos, Enrique J.,Vela, José Miguel,Almansa, Carmen
, p. 5157 - 5170 (2021)
The synthesis and pharmacological activity of a new series of 5a,7,8,8a-tetrahydro-4H,6H-pyrrolo[3,4-b][1,2,3]triazolo[1,5-d][1,4]oxazine derivatives as potent sigma-1 receptor (σ1R) ligands are reported. A lead optimization program aimed at improving the aqueous solubility of parent racemic nonpolar derivatives led to the identification of several σ1R antagonists with a good absorption, distribution, metabolism, and excretion in vitro profile, no off-target affinities, and characterized by a low basic pKa (around 5) that correlates with high exposure levels in rodents. Two compounds displaying a differential brain-to-plasma ratio distribution profile, 12lR and 12qS, exhibited a good analgesic profile and were selected as preclinical candidates for the treatment of pain.
Tricyclic triazolic compounds
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Page/Page column 50, (2009/07/10)
The present invention relates to new tricyclic triazolic compounds having a high affinity for sigma-1 receptor as well as to the process for the preparation thereof, to composition comprising them and to their use as medicaments according to compounds of
