105310-50-7Relevant academic research and scientific papers
Non-Peptide Ligands for Opioid Receptors. Design of κ-Specific Agonists
Ronsisvalle, G.,Pasquinucci, L.,Pappalardo, M. S.,Vittorio, F.,Fronza, G.,et al.
, p. 1860 - 1865 (1993)
A series of phenyl carboxy esters 5a-d derived from N-(cyclopropylmethyl)normetazocine was synthesized and evaluated for its selectivity at μ, κ, and δ opioid receptors.Compound 5a, although 43 times less potent than the reference compound U50488, was spe
1-Aryl-2-(aminomethyl)cyclopropanecarboxylic Acid Derivatives. A New Series of Potential Antidepressants
Bonnaud, Bernard,Cousse, Henri,Mouzin, Gilbert,Briley, Mike,Stenger, Antoine,et al.
, p. 318 - 325 (2007/10/02)
A series of 1-aryl-2-(aminomethyl)cyclopropanecarboxylic acid derivatives were synthesized and evaluated as potential antidepressants.Compounds with the Z configuration were synthesized from 1-aryl-2-oxo-3-oxabicyclohexane and those with E configuration from (E)-1-phenyl-2-(hydroxymethyl)cyclopropanecarboxylic acid.The compounds were evaluated in animal tests designed to reveal potential antidepressant activity and the existence of undesirable side effects.Several derivatives were more active than imipramine and desipramine.On the basis of its activity in pharmacological animal tests of antidepressant activity and its potential lack of side effects, 1-phenyl-1--2-(aminomethyl)cyclopropane hydrochloride, midalcipran (INN), was selected for further development.This compound is currently in phase III clinical evaluation.
