Rational Design of Anxiolytic and Anticonvulsant Drugs

The balance between neuronal excitation and inhibition is critical for information processing in the brain. When this balance is disrupted, epilepsy and anxiety disorders may result. This balance depends on inhibitory neurotransmission mediated primarily through GABAA receptors. These receptors can be potently modified by endogenous neurosteroids. However, existing drugs have serious side effects because they are relatively indiscriminate, affecting many GABAA receptor subtypes. A subtype-selective drug would avoid this difficulty, and therefore provide a more effective therapy. Dr. Bamber and colleague at the University of Utah have identified novel subunits on the GABAA receptors that are modulated by neurosteroids. Thus providing a family of potential molecular targets for compounds that could specifically affect small subsets of GABAA receptors.

This technology would be used by pharmaceutical companies that are developing or marketing drugs that target GABAA receptors. The target compounds could be used to treat anxiety disorders, enhance cognition, as anticonvulsants and as sleep inducing agents for insomnia. This represents a very significant patient population.

Stage of Development
A PCT patent application has been filed with the USPTO and is pending. This technology is part of an active and ongoing research program and has been demonstrated to work in proof of concept experiments. It is available for licensing under either exclusive or non-exclusive terms.

Additional Info
*Wardell B, Marik PS, Piper D, Rutar T, Jorgensen EM, Bamber BA. (2006) Residues in the first transmembrane domain of the Caenorhabditis elegans GABA(A) receptor confer sensitivity to the neurosteroid pregnenolone sulfate. Br J Pharmacol.

Inventor(s): Bruce Bamber, Bryan Wardell

Type of Offer: Licensing

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