Substituted guanidines and derivatives thereof as modulators of neurotransmitter release and novel methodology for identifying neurotransmitter release blockers

US5403861A · kind A · utility

Assignee

• Cambridge NeuroScience, Inc. · US

Inventors

• Stanley M. Goldin · Lexington, US
• Subbarao Katragadda · Belmont, US
• Lain-Yen Hu · Ann Arbor, US
• N. Laxma Reddy · Solon, US
• James B. Fischer · Cambridge, US
• Andrew Gannett Knapp · Salem, US
• Lee David Margolin · Belmont, US

Key dates

• Filing date: Feb 10, 1992
• Grant date: Apr 4, 1995
• Expiry date: Feb 10, 2012

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.