CoCensys Begins Preclinical Development of NMDA Antagonist

CoCensys Inc. (Irvine, CA) announced today that Parke-Davis, a division of Warner-Lambert Co. (Morris Plains, NJ), has advanced its lead compound into preclinical development for the treatment of neurological disorders. This compound is an antagonist to N-methyl-D-aspartate (NMDA) receptors in the brain.

NMDA receptors have long been recognized as promising molecular targets for the treatment of neurological disorders such as stroke, traumatic brain injury, epilepsy, Parkinson's disease, and chronic pain states. The first generation of NMDA receptor antagonists that blocked the receptor channel directly produced unacceptable side effects, such as induction of psychotomimetic (PCP-like) behaviors and neurotoxicity. Subsequent studies at the molecular level demonstrated the heterogeneity of NMDA receptors, which consist of subtypes with distinct biophysical and pharmacologic properties and different patterns of distribution in the brain.

While the first generation of NMDA receptor antagonists were non-selective, the collaboration between CoCensys and Parke-Davis sought to design drugs that interact selectively with specific subtypes of NMDA receptors. The intent was to retain the potential therapeutic utility of an NMDA receptor antagonist while greatly improving the side-effect profile.

"The subtype-selective antagonists appear to have therapeutic potential for a variety of neurological disorders," said Richard Woodward, senior director of drug discovery at CoCensys. "We believe from our animal studies that these types of compounds have superior behavioral and side effect profiles to channel blockers such as dizocilpine (MK-801) and competitive antagonists such as selfotel (CGS 19755)."

CoCensys is a biopharmaceutical company that discovers and develops products for the treatment of neurological and psychiatric disorders.

For more information: Richard Woodward, Senior Director of Drug Discovery, CoCensys Inc., 201 Technology Dr., Irvine, CA 92618. Tel: 949-753-6100. Fax: 949-753-6161.