THE NATURE OF THE ADENOSINE RECEPTOR WILL BE STUDIED USING ADENOSINE AGONISTS AND ANTAGONISTS MODIFIED FOR SELECTIVITY AND POSSIBLE AFFINITY LABELING.

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$50,000.00
Award Year:
1986
Program:
SBIR
Phase:
Phase I
Contract:
n/a
Award Id:
4894
Agency Tracking Number:
4894
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
Research Biochemicals Inc (Currently Research Biochemicals,)
9 Eric Drive, Natick, MA, 01760
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
JOHN L NEUMEYER
PRINCIPAL INVESTIGATOR
(617) 651-8151
Business Contact:
() -
Research Institution:
n/a
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.

* information listed above is at the time of submission.

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