Bearsden Bio, Inc.

Transgenomic, Inc.

Other

Maria-Luisa Maccecchini

Xue-Feng Pei

Baoqing Li

Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neuropsychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.

Sulfur containing dihydrophthalazine antagonists of excitatory amino acid receptors

Substituted benzodiazepine compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compounds are generally 7- or 8-mono substituted 5H-2,3-benzodiazepines. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.

5H-2,3-benzodiazepine antagonists of excitatory amino acid receptors

Novel compounds and compositions for modulating NMDA receptor function comprising Conantokin-G and derivatives thereof; methods for modulating NMDA receptor function and methods for treating neuropsychopharmacological disorders, using the novel compounds and compositions of the invention; and a method for screening compounds capable of binding to a novel allosteric modulatory site, are described.

Allosteric modulators of the NMDA receptor and their use in the treatment of CNS disorders and enhancement of CNS function

Allosteric modulators of the NMDA receptor and their use in the

Novel compounds and compositions for modulating NMDA receptor function comprising Conantokin-G and derivatives thereof; methods for modulating NMDA receptor function and methods for treating neuropsychopharmacological disorders, using the novel compounds and compositions of the invention; and a method for screening compounds capable of binding to a novel allosteric modulatory site are described.

This invention concerns inhibitors of the tolerance and dependence induced by opiate analgesics. Excitatory amino acids control the action of the NMDA receptor through allosteric binding sites. Early studies showed that channel blockers and allosteric site antagonists of the NMDA receptor inhibited the development of tolerance to and dependence on opiate analgesics, but also produced their own undesirable side effects. Partial agonists of the NMDA allosteric sites tend to normalize NMDA receptor function and do not produce strong undesirable side effects. It has been discovered that partial agonists inhibit the development of tolerance to opiate analgesics, and it is taught that partial agonists also inhibit development of dependence on opiate analgesics. ACPC, 1-aminocyclopropanecarboxylic acid, in particular, is an exemplary partial agonist at the glysine site useful to treat opiate addiction. Compounds containing an opiate analgesic and a partial agonist, produce analgesia without inducing tolerance or dependence.

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West Chester, PA, United States of America

Maria-Luisa Maccecchini