Kainate receptor-selective epimeric analogs of dysiherbaine

Geoffrey Swanson (Inventor)

Research output: Patent

Abstract

Small Molecule for Treatment of Epilepsy, Pain, and Other Neurological Disorders NU 2007-036 Inventors Leanne Lash Geoffrey Swanson* Ryuichi Sakai Abstract 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. Applications o Small molecule therapy for epilepsy, pain, and stroke Advantages o Selective antagonist for kainite receptor o No other commercially available molecule with similar activity IP Status Issued US Patent No. 7,973,075 Marketing Contact Michael Moore, PhD Invention Manager (e) michaelmoore@northwestern.edu (p) 847.491.4645
Original languageEnglish
Patent number7973075
StatePublished - Jul 5 2011

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