USA flag logo/image

An Official Website of the United States Government

DEVELOPMENT OF ENDOTHELIN-1 ANTAGONISTS

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
16705
Program Year/Program:
1991 / SBIR
Agency Tracking Number:
16705
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
Nova Pharmaceutical Corp
6200 Freeport Ctr Baltimore, MD 21224
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 1991
Title: DEVELOPMENT OF ENDOTHELIN-1 ANTAGONISTS
Agency: HHS
Contract: N/A
Award Amount: $47,000.00
 

Abstract:

ENDOTHELIN-1 (ET-1), A 21 AMINO ACID PEPTIDE, ACTING AT SPECIFIC RECEPTORS IN VASCULAR TISSUES HAS BEEN DEMONSTRATED TO INITIATE SUCH PHYSIOLOGICAL RESPONSES AS: DECREASES/INCREASES IN SYSTEMIC ARTERIAL PRESSURE, ALTERATIONS IN LOCAL BLOOD DISTRIBUTION, RENAL FUNCTION (I. E. FORMATION AND COMPOSITION OF URINE, RELEASE OF CIRCULATING HORMONES), AND DILATION/CONTRACTION OF NONVASCULAR SMOOTH MUSCLE (I. E. RESPIRATORY, GASTROINTESTINAL). IN ADDITION TO THESE PHYSIOLOGICAL ROLES ET-1 MAY ALSO BE INVOLVED IN SUCH DIVERSE FUNCTIONS AS INFLAMMATORY AND NEUROMODULATORY ACTION. ET-1 REGULATION OF CARDIOVASCULAR FUNCTION MAY PLAY A SIGNIFICANT ROLE IN CORONARY ANGINA AND CEREBRAL VASOSPASM, HYPERTENSION, AND ATHEROSCLEROSIS. WE WILL PERFORM THE IDENTIFICATION AND EVALUATION OF SYSTEMICALLY ACTIVE NON-PEPTIDE ANTAGONISTS OF ET-1 TO BE DEVELOPED AS NOVEL THERAPEUTIC APPROACHES FOR TREATING ANY OF THE DISORDERS MENTIONED ABOVE. STARTING WITH AN INVENTORY OF APPROXIMATELY 20,000 COMPOUNDS, IN VITRO RADIOLIGAND BINDING AND CALCIUM MOBILIZATION ASSAYS WILL SERVE AS INITIAL SCREENING PROCEDURES FOR IDENTIFYING SELECTIVE ET-1 ANTAGONISTS. LEAD STRUCTURES WILL THEN BE EVALUATED FOR ET-1-ANTAGONIST ACTIVITY IN VIVO USING CARDIOVASCULAR MONITORING. COMPOUNDS IDENTIFIED DURING PHASE I STUDIES WILL PROVIDE POINTS OF DEPARTURE FOR SYNTHETIC CHEMICAL IMPROVEMENTS DURING PHASE II WORK WITH CONTINUED EVALUATION OF COMPOUNDS FOR A CARDIOVASCULAR ACTIVITY AS WELL AS THE DEVELOPMENT OF ANIMAL MODELS NECESSARY TO ASSESS OTHER POTENTIAL THERAPEUTIC USES FOR AN ET-1 ANTAGONIST.

Principal Investigator:

Sweetnam, Paul M
Principal Investigator
3015587000

Business Contact:

1 r43 hl46098-01
Small Business Information at Submission:

Nova Pharmaceutical Corpo
6200 Freeport Centre Baltimore, MD 21224

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