Small Molecule for Treatment of Epilepsy, Pain, and Other Neurological Disorders
- Technology Benefits
- • Selective antagonist for kainite receptor • No other commercially available molecule with similar activity
- Detailed Technology Description
- A new class of small molecules that may be used to targetspecific AMPA* receptors #therapeutics #smallmolecules #pain #neurology
- *Abstract
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Over-activation of AMPA receptors contributes to the pathology of a number of neurological diseases, particularly epilepsy, neuropathic pain, and stroke. A new group of heterotricyclic molecules called "IKM" analogs have been determined to act pharmacologically as AMPA receptor antagonists. Northwestern researchers have discovered a new class of small molecules that may be used to target specific AMPA receptors. A small molecule, 2,4-epi-neodysiherbaine (2,4-epi-NDH), has been determined to act as a selective kainate receptor antagonist. 2,4-epi-NDH is a synthetic analog of a natural molecule, dysiherbaine, which is itself a rigid analog of the excitatory amino acid neurotransmitter L-glutamate. The novelty of 2,4-epi-NDH is structural in that it has altered stereochemistry at the C2 and C4 positions and thus is not strictly considered an L-glutamate congener. The molecular also exhibits a novel pharmacological profile. There currently is no commercially available small molecule with similar pharmacological activity, making 2,4-epi-neodysiherbaine a desirable candidate for therapeutic use.
- *Inventors
- Leanne Lash Geoffrey Swanson* Ryuichi Sakai
- Country/Region
- USA
