Technology Bundle ID
TAB-3566

Deuterated alpha5 Subunit-selective Negative Allosteric Modulators of Gamma-Aminobutyric Acid Type A Receptors as Fast Acting Treatments for Depression and Mood Disorders

Applications
Linked ID
E-232-2017-0
Lead Inventors
Scott Thompson (University of Maryland)
Co-Inventors
Adam Van Dyke (University of Maryland)
Craig Thomas (NCATS)
Patrick Morris (NCATS)
ICs
This technology includes GABAa a5 Negative Allosteric modulators (GABAa a5 NAMs) which have been recently discovered to act as fast-acting antidepressants in a variety of mouse models of depression. These NAMs are actively metabolized in vivo. This invention involves the conceptualization and synthesis of GABAa a5 NAM molecules with a deuterium in the active metabolic position. This significantly increased the metabolic stability, while still retaining the antidepressant activity.
Commercial Applications
Treatment for depression or other neurological disorders.
Competitive Advantages
These molecules have similar activity as GABAa a5 NAMs to the current molecules in clinical trials, while having significantly improved metabolic stability, and likely longer half lives in vivo.

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