Pharmacopsychiatry 2004; 37: 214-220
DOI: 10.1055/s-2004-832680
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

Clinical Trials with Sigma Ligands

H.-P. Volz1 , K. D. Stoll2
  • 1Krankenhaus für Psychiatrie und Psychotherapie Schloss Werneck, Werneck, Germany
  • 2Novartis Pharma GmbH Nürnberg, Germany
Further Information

Publication History

Publication Date:
17 November 2004 (online)

So far, sigma-ligands have been investigated for several indications in human studies in functional diarrhea as a model of somatoform disorder (igmesine), depression (igmesine, opipramol), anxiety (opipramol and - in animal models - siramisine), schizophrenia (panamasine, SL 82.0715, rimcazole, DuP 734, BMY 14 802), and somatoform disorders (opipramol). Results for schizophrenia failed to be clear cut and so investigations have apparently stopped for the time being. The Sigma-1-selective igmesine (200 mg) showed good results in a phase-1-model of functional diarrhea and some promising results in depressed patients. However, further development has been stopped due to marketing reasons, which is also true for siramasine, a selective sigma-2-ligand with anxiolytic properties. Opipramol, which, apart from a sigma-1- and 2-receptor liability, also possesses histamine-H1-antagonistic properties in connection with lower affinities for D2 and 5-HT2A showed broad efficacy in generalized anxiety disorder and somatoform disorders. The receptor profile of opipramol and the results of studies of the selective sigma site ligands siramisine and igmesine suggest that opipramol acts pharmacologically and clinically via sigma receptors.

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Prof. Dr. Hans-Peter Volz

Krankenhaus für Psychiatrie und Psychotherapie Schloss Werneck

Balthasar-Neumann-Platz 1

D-97440 Werneck

Phone: +49/9722/21-1280

Fax: +49/9722/21-1465

Email: hans-peter.volz@kh-schloss-werneck.de

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