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THE NATURE OF THE ADENOSINE RECEPTOR WILL BE STUDIED USING ADENOSINE AGONISTS…

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
4894
Program Year/Program:
1986 / SBIR
Agency Tracking Number:
4894
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
Research Biochemicals,
1 STRATHMORE RD Natick, MA 01760
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 1986
Title: THE NATURE OF THE ADENOSINE RECEPTOR WILL BE STUDIED USING ADENOSINE AGONISTS AND ANTAGONISTS MODIFIED FOR SELECTIVITY AND POSSIBLE AFFINITY LABELING.
Agency: HHS
Contract: N/A
Award Amount: $50,000.00
 

Abstract:

THE NATURE OF THE ADENOSINE RECEPTOR WILL BE STUDIED USING ADENOSINE AGONISTS AND ANTAGONISTS MODIFIED FOR SELECTIVITY AND POSSIBLE AFFINITY LABELING. ADENOSINE PLAYS A KEY ROLE IN PHYSIOLOGICAL PROCESSES, AND CURRENTLY NO SELECTIVE A1 ORA2 ANTAGONISTS HAVE AS YET BEEN DEVELOPED. SELECTIVE AGONISTS AND ANTAGONISTS FOR ADENOSINE RECEPTORS COULD HAVE CLINICAL IMPORTANCE IN THE TREATMENT OF ASTHMA, AS DIURETICS, RESPIRATORY STIMULANTS, AND AS CENTRAL DEPRESSANTS OR STIMULANTS. A SERIES OF SELECTIVE A1- ADENOSINE ANTAGONISTS WILL BE SYNTHESIZED AND EVALUATED BASED ON THE PRESENCE OF: (1) ALKYL, ALKENYL, ALKYNYL, HYDROXYETHLY, OR AMINOALKYL SUBSTITUENTS AT THE 1-, 3-, AND 7-POSITIONS OF XANTHINE; (2) AN ORTHOHYDROXY OR ORTHOAMINO GROUP ON THE 8-PHENYL SUBSTITUENT; AND (3) AN APPROPRIATE POLAR PARA SUBSTITUENT ON THE 8-PHENYL SUBSTITUENT FOR INCREASED WATER SOLUBILITY. AS YET, NO XANTHINE DERIVATIVESWITH MORE THAN A MODEST SELECTIVITY FOR A2 ADENOSINE RECEPTORS HAVE BEEN DISCOVERED, AND OTHER HETEROCYCLIC SYSTEMS WILL BE INVESTIGATED AS ADENOSINE RECEPTOR ANTAGONISTS. A SERIES OF FUNCTIONAL CONGENERS OF ADENOSINE BASED ON THE POTENT A1 ADENOSINE RECEPTOR AGONIST ACTIVITY OF N6-PHENYLADENOSINE WILL ALSO BE SYNTHESIZED AND EVALUATED. SELECTIVE EXAMPLES OF ADENOSINE ANALOGS IN WHICHTHE RIBOSE MOIETY WILL BE REPLACED WITH A HYDROXYETHOXY SUBSTITUENT WILL ALSO BE PREPARED AND EVALUATED.

Principal Investigator:

John l neumeyer
PRINCIPAL INVESTIGATOR
6176518151

Business Contact:

Small Business Information at Submission:

Research Biochemicals Inc
9 Eric Drive Natick, MA 01760

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