Radioiodinated benzovesamicol analogs for cholinergic nerve mapping

US5077035A · kind A · utility

Assignee

• THE REGENTS OF THE UNIVERSITY OF MICHIGAN · US

Inventors

• Donald M. Wieland · Ann Arbor, US
• Yong-Woon Jung · Ann Arbor, US
• Marcian Van Dort · Ann Arbor, US
• David L. Gildersleeve · Ypsilanti, US

Key dates

• Filing date: May 14, 1990
• Grant date: Dec 31, 1991
• Expiry date: May 14, 2010

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K2123/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Radioiodinated benzovesamicol analogs which selectively localize in presynaptic cholinergic neurons of the general formula: ##STR1## where X is selected from the group consisting of H, OH, NH.sub.2, NHCO-3-[I]-Ph, and a radioactive isotope of iodine, and Y is selected from the group of H and a radioactive isotope of iodine, Y being H is X contains iodine. Illustrative examples include: (.+-.)-trans-2-hydroxy-5-iodo-3-(4-phenylpiperidino)tetralin; (.+-.)-trans-3-hydroxy-5-iodo-2-(4-phenylpiperidino)tetralin; (.+-.)-trans-5-amino-2-hydroxy-8-iodo-3-(4-phenylpiperidino)tetralin; and (.+-.)-trans-2-hydroxy-5-(3-iodobenzamido)-3-(4-phenylpiperidino)tetralin. The novel radioiodinated benzovesamicol analogs may be used as radiopharmaceuticals to visualize cholinergic neurons with conventional imaging devices which are typically found in most nuclear medicine or radiology clinics.