IDENTIFICATION OF SIGMA ANTAGONISTS

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$49,911.00
Award Year:
1991
Program:
SBIR
Phase:
Phase I
Contract:
n/a
Award Id:
16836
Agency Tracking Number:
16836
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
6200 Freeport Ctr, Baltimore, MD, 21224
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
Edward Carbon Jr
(301) 558-7000
Business Contact:
() -
Research Institution:
n/a
Abstract
DOPAMINE (D2) RECEPTOR ANTAGONISTS SUCH AS HALOPERIDOL AND CHLORPROMAZINE ARE MOST COMMONLY USED TO TREAT SCHIZOPHRENIA. HOWEVER, BOTH ACUTE AND CHRONIC ADMINISTRATION OF THESE DRUGS CAN RESULT IN THE APPEARANCE OF EXTRAPYRAMIDAL SIDE EFFECTS (EPS) WHICH, LIKE THE THERAPEUTIC EFFECTS OF THESE DRUGS, RESULTS FROM BLOCKADE OFD2 RECEPTORS. THEREFORE, ANTIPSYCHOTIC DRUGS WHOSE MECHANISM OF ACTION DOES NOT INVOLVE D2 RECEPTOR ANTAGONISM WILL BE VALUABLE THERAPEUTIC AGENTS. A NOVEL APPROACH TO THE TREATMENT OF SCHIZOPHRENIA IS THE DEVELOPMENT OF SIGMA ANTAGONISTS. NOVA HAS IDENTIFIED POTENT AND SELECTIVE, ORALLY ACTIVE SIGMA AGENTS HAVING ANTIPSYCHOTIC PROPERTIES. THE SPECIFIC AIMS OF THE PHASE I STUDY ARE TO IDENTIFY POTENT AND SELECTIVE COMPOUNDS EXHIBITING ORAL EFFICACY USING TWO BEHAVIORAL PARADIGMS THOUGHT TO PREDICT ANTIPSYCHOTIC POTENTIAL, AND TO OBTAIN A STRUCTURE-ACTIVITY PROFILE ON WHICH TO BASE FUTURE MEDICINALCHEMISTRY EFFORTS. THE ULTIMATE GOAL OF THIS RESEARCH IS TOIDENTIFY AN ANTIPSYCHOTIC AGENT(S), DEVOID OF EPS LIABILITY,THAT IS THERAPEUTICALLY SUPERIOR TO CURRENTLY AVAILABLE ANTIPSYCHOTICS. GIVEN THE EXISTING LACK OF SUITABLE TREATMENTS FOR SCHIZOPHRENIA, THE IDENTIFICATION AND DEVELOPMENT OF AN ANTIPSYCHOTIC DRUG THAT IS BOTH EFFICACIOUS AND SAFE WILL RESULT IN BOTH THERAPEUTIC AND COMMERCIAL SUCCESS. DOPAMINE (D2) RECEPTOR ANTAGONISTS SUCH AS HALOPERIDOL AND CHLORPROMAZINE ARE MOST COMMONLY USED TO TREAT SCHIZOPHRENIA. HOWEVER, BOTH ACUTE AND CHRONIC ADMINISTRATION OF THESE DRUGS CAN RESULT IN THE APPEARANCE OF EXTRAPYRAMIDAL SIDE EFFECTS (EPS) WHICH, LIKE THE THERAPEUTIC EFFECTS OF THESE DRUGS, RESULTS FROM BLOCKADE OFD2 RECEPTORS. THEREFORE, ANTIPSYCHOTIC DRUGS WHOSE MECHANISM OF ACTION DOES NOT INVOLVE D2 RECEPTOR ANTAGONISM WILL BE VALUABLE THERAPEUTIC AGENTS. A NOVEL APPROACH TO THE TREATMENT OF SCHIZOPHRENIA IS THE DEVELOPMENT OF SIGMA ANTAGONISTS. NOVA HAS IDENTIFIED POTENT AND SELECTIVE, ORALLY ACTIVE SIGMA AGENTS HAVING ANTIPSYCHOTIC PROPERTIES. THE SPECIFIC AIMS OF THE PHASE I STUDY ARE TO IDENTIFY POTENT AND SELECTIVE COMPOUNDS EXHIBITING ORAL EFFICACY USING TWO BEHAVIORAL PARADIGMS THOUGHT TO PREDICT ANTIPSYCHOTIC POTENTIAL, AND TO OBTAIN A STRUCTURE-ACTIVITY PROFILE ON WHICH TO BASE FUTURE MEDICINALCHEMISTRY EFFORTS. THE ULTIMATE GOAL OF THIS RESEARCH IS TOIDENTIFY AN ANTIPSYCHOTIC AGENT(S), DEVOID OF EPS LIABILITY,THAT IS THERAPEUTICALLY SUPERIOR TO CURRENTLY AVAILABLE ANTIPSYCHOTICS. GIVEN THE EXISTING LACK OF SUITABLE TREATMENTS FOR SCHIZOPHRENIA, THE IDENTIFICATION AND DEVELOPMENT OF AN ANTIPSYCHOTIC DRUG THAT IS BOTH EFFICACIOUS AND SAFE WILL RESULT IN BOTH THERAPEUTIC AND COMMERCIAL SUCCESS.

* information listed above is at the time of submission.

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