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NOVEL NEUROPROTECTIVE AGENTS

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
16782
Program Year/Program:
1991 / SBIR
Agency Tracking Number:
16782
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
NEUROTHERAPEUTICS, L.P.
2515 N CLARK ST, STE 800 CHICAGO, IL 60614
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 1991
Title: NOVEL NEUROPROTECTIVE AGENTS
Agency: HHS
Contract: N/A
Award Amount: $50,000.00
 

Abstract:

ACUTE NEUROLOGIC DISORDERS SUCH AS STROKE AND HEAD TRAUMA ARE PRESENTLY UNTREATABLE. RECENT BREAKTHROUGHS IN THE UNDERSTANDING OF HOW NEURAL TISSUE DEGENERATES, POST-ISCHEMIA, HAVE MADE POSSIBLE SEVERAL AVENUES OF THERAPEUTIC INTERVENTION FOR THESE DEVASTATING DISORDERS WHICH HOLD THE PROMISE OF SALVAGING MUCH OF THE BRAIN TISSUETHAT IS DESTROYED IN THE HOURS FOLLOWING STROKE OR HEAD TRAUMA. IT HAS BEEN SHOWN THAT EXCITATORY AMINO ACID (EAA) NEUROTRANSMITTERS, GLUTAMATE AND ASPARTATE ARE OVER RELEASED AFTER A STROKE AND THAT THIS ACTUALLY STIMULATES NERVE CELLS TO DEATH. THIS PROCESS IS CALLED EXCITOTOXICITYAND HAS LEAD TO THE DEVELOPMENT OF EAA RECEPTOR BLOCKERS AS A THERAPEUTIC STRATEGY. THESE AGENTS, ALTHOUGH EFFECTIVE, HAVE PROVEN TO HAVE UNACCEPTABLE SIDE EFFECTS. THE NEUROTHERAPEUTICS APPROACH IS TO INHIBIT THE RELEASE OF EAAS PRESYNAPTICALLY VIA BLOCKING THE N-TYPE CALCIUM CHANNELTHAT REGULATES EAA RELEASE. WE HAVE IDENTIFIED A GROUP OF AGENTS THAT ACTS AT N-TYPE CHANNELS. DURING PHASE I, WE WILL DEMONSTRATE EFFICACY OF THESE AGENTS IN AN IN VITRO AND IN VIVO MODEL SYSTEM OF NEUROPROTECTION. AN ATTEMPT TO OBTAIN SOME STRUCTURE ACTIVITY RELATIONSHIPS WILL ALSO BE MADE. IN PHASE II, WE WILL LAUNCH A MEDICINAL CHEMISTRY EFFORT TO DERIVATIZE THE AGENT CHARACTERIZED IN PHASE I. THE GOALS HERE ARE TO GENERATE AGENTS WITH GREATER POTENCY AT THE N-TYPE CALCIUM CHANNEL. ACUTE NEUROLOGIC DISORDERS SUCH AS STROKE AND HEAD TRAUMA ARE PRESENTLY UNTREATABLE. RECENT BREAKTHROUGHS IN THE UNDERSTANDING OF HOW NEURAL TISSUE DEGENERATES, POST-ISCHEMIA, HAVE MADE POSSIBLE SEVERAL AVENUES OF THERAPEUTIC INTERVENTION FOR THESE DEVASTATING DISORDERS WHICH HOLD THE PROMISE OF SALVAGING MUCH OF THE BRAIN TISSUETHAT IS DESTROYED IN THE HOURS FOLLOWING STROKE OR HEAD TRAUMA. IT HAS BEEN SHOWN THAT EXCITATORY AMINO ACID (EAA) NEUROTRANSMITTERS, GLUTAMATE AND ASPARTATE ARE OVER RELEASED AFTER A STROKE AND THAT THIS ACTUALLY STIMULATES NERVE CELLS TO DEATH. THIS PROCESS IS CALLED EXCITOTOXICITYAND HAS LEAD TO THE DEVELOPMENT OF EAA RECEPTOR BLOCKERS AS A THERAPEUTIC STRATEGY. THESE AGENTS, ALTHOUGH EFFECTIVE, HAVE PROVEN TO HAVE UNACCEPTABLE SIDE EFFECTS. THE NEUROTHERAPEUTICS APPROACH IS TO INHIBIT THE RELEASE OF EAAS PRESYNAPTICALLY VIA BLOCKING THE N-TYPE CALCIUM CHANNELTHAT REGULATES EAA RELEASE. WE HAVE IDENTIFIED A GROUP OF AGENTS THAT ACTS AT N-TYPE CHANNELS. DURING PHASE I, WE WILL DEMONSTRATE EFFICACY OF THESE AGENTS IN AN IN VITRO AND IN VIVO MODEL SYSTEM OF NEUROPROTECTION. AN ATTEMPT TO OBTAIN SOME STRUCTURE ACTIVITY RELATIONSHIPS WILL ALSO BE MADE. IN PHASE II, WE WILL LAUNCH A MEDICINAL CHEMISTRY EFFORT TO DERIVATIZE THE AGENT CHARACTERIZED IN PHASE I. THE GOALS HERE ARE TO GENERATE AGENTS WITH GREATER POTENCY AT THE N-TYPE CALCIUM CHANNEL.

Principal Investigator:

Paul Marangos
6194556093

Business Contact:

Small Business Information at Submission:

Neurotherapeutics Corp
11211 Sorrento Valley Rd #h San Diego, CA 92121

EIN/Tax ID:
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No