Synthesis and pharmacological characterization of ABT-200: a putative novel antidepressant combining potent α-2 antagonism with moderate NE uptake inhibition

• Published in: Bioorganic & medicinal chemistry letters Vol. 4; no. 11; pp. 1319 - 1322
• Main Authors: Zelle, Robert E., Hancock, Arthur A., Buckner, Steven A., Basha, Fatima Z., Tietje, Karin, DeBernardis, John F., Meyer, Michael D.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 09.06.1994; Elsevier
• Subjects: Biological and medical sciences; Medical sciences; Neuropharmacology; Pharmacology. Drug treatments; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease); Psychology. Psychoanalysis. Psychiatry; Psychopharmacology; α2-Adrenergic receptor; Psychotropic; Antidepressant agent; Norepinephrine; Antagonist; Reuptake inhibitor; Chemical synthesis; Biological activity; Pyrrolidine derivatives
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(01)80353-X

ABT-200, (±)-(1′R*, 3R*)-3-phenyl-1-[(1′,2′,3′,4′-tetrahydro-5′,6′-methylenedioxy-1′-naphthalenyl)methyl]pyrrolidine, ( 1a/b) represents the first example of a new structural class of potent α-2 antagonists which possess the additional property of norepinephrine (NE) uptake inhibition. This profile of combined activities is expected to have utility in the treatment of depression. ABT-200, (±)-(1′R*, 3R*)-3-phenyl-1-[(1′,2′,3′,4′-tetrahydro-5′,6′-methylenedioxy-1′-naphthalenyl)methyl]pyrrolidine represents the first example of a new structural class of potent α-2 antagonists which possess the additional property of norepinephrine (NE) uptake inhibition. This profile of combined activities is expected to have utility in the treatment of depression.