HIGH AFFINITY LIGANDS FOR SPECIFIC DOPAMINE RECEPTORS

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: N/A
Agency Tracking Number: 3360
Amount: $264,000.00
Phase: Phase II
Program: SBIR
Awards Year: 1987
Solicitation Year: N/A
Solicitation Topic Code: N/A
Solicitation Number: N/A
Small Business Information
P.o. Box 181, Wayland, MA, 01778
DUNS: N/A
HUBZone Owned: N
Woman Owned: N
Socially and Economically Disadvantaged: N
Principal Investigator
 Richard A. Milius
 Principal Investigator
 (617) 358-4795
Business Contact
Phone: () -
Research Institution
N/A
Abstract
THE DEVELOPMENT OF SAFER AND MORE EFFECTIVE ANTIPSYCHOTIC DRUGS REQUIRES THE AVAILABILITY OF SENSITIVE PROBES OF THE DOPAMINE (DA) RECEPTOR, WHICH IS A SITE OF ACTION OF THESE AGENTS. RESEARCH BIOCHEMICALS PROPOSES A PROGRAM TO PREPARE NOVEL SUBSTANCES WITH SELECTIVE AGONIST OR ANTAGONIST ACTION AT SPECIFIC DA RECEPTORS FOR USE BY RESEARCHERS IN NEUROPHARMACOLOGY. THE OBJECTIVES OF PHASE I RESEARCH ARE: 1. THE SYNTHESIS OF NOVEL APORPHINES AND RELATED COMPOUNDS WITH IRREVERSIBLE BINDING ACTIVITY AT DA RECEPTOR SITES. STRUCTURES WILL BE FORMULATED WITH PARTICULAR EMPHASIS ON SELECTIVE ACTIVITY AT PRESYNAPTIC DA AUTORECEPTORS. IRREVERSIBLE BINDING WILL BE ACCOMPLISHED WITH ALKYLATING AND/OR PHOTOACTIVATED FUNCTIONAL GROUPS. 2.THE INCORPORATION OF HIGHLY SELECTIVE DA RECEPTOR LIGANDS INTO A PRACTICAL AFFINITY COLUMN. THE PROTOTYPE OF THIS PRODUCT WILL BE A CLEBOPRIDE-FUNCTIONALIZED SUPPORT FOR USE IN ISOLATING DA D2 RECEPTORS. 3.THE PREPARATION OF HITHERTO UNAVAILABLE ENANTIOMERICALLY PURE PAIRS OF KNOWN DA AGONISTS AND ANTAGONISTS TO PERMIT STEREOCHEMICAL EXPLORATION OF RECEPTOR SURFACES. THE NEW PRODUCTS GENERATED IN PHASE I STUDIES WILL BE EVALUATED FOR COMMERICAL INTRODUCTION TO THE EXPANDING NEUROSCIENTIFIC COMMUNITY.

* Information listed above is at the time of submission. *

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