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Abstract

Grant Number:	4R44NS043830-02
PI Name:	WANG-SMITH, LAURENE
PI Email:
PI Title:
Project Title:	Novel Pharmacotherapy for Parkinson's Disease

Abstract: DESCRIPTION (provided by applicant):This FastTrack Phase I/II application seeks to develop the first orally available, non-tolerance producing, dopamine D1 full agonist. There is substantial data that such a drug would have unsurpassed efficacy in Parkinson's disease, as well as the potential to help other difficult totreat conditions such as negative symptoms of schizophrenia. The Phase I application is designed to provide the preclinical data necessary to select a lead compound for development, and provide backup compounds in case they are needed later. The milestones to be achieved will include: 1. Conclude a broad-based receptor screening profile for DAR-201; 2. Perform functional characterization for any receptor or enzyme system for which DAR-201 is found to have significant affinity. 3 Prepare 50 mg quantities of at least five selected compounds as backups; 4. Complete binding and functional profile of the selected backup compounds at six dopamine receptors (i.e., D1, D2L. D2s, D3. D4, D5) and selected other monamine receptors; 5. Use the unilateral 6-OHDA model of Parkinson?s disease to collect dose-response and time-course data on the activity of selected compounds; and 6. Get complete receptor profiling to complement the data accumulated from Aims 3&4.

Thesaurus Terms:
Parkinson's disease, dopamine agonist, drug design /synthesis /production, neuropharmacologic agent, neuropharmacology, oral administration
6 hydroxydopamine, brain disorder chemotherapy, dopamine receptor, drug screening /evaluation, receptor expression
Callithricidae

Institution:	DARPHARMA, INC.
	215 CLOISTER CT
	CHAPEL HILL, NC 27514
Fiscal Year:	2003
Department:
Project Start:	01-AUG-2002
Project End:	31-JAN-2004
ICD:	NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE
IRG:	ZRG1

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