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DISCOVERY OF NOVEL PHARMACOTHERAPIES: COCAINE DEPENDENCE

Award Number: R01DA011542
ORGANIZATION: NATIONAL INSTITUTE ON DRUG ABUSE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 09/30/1997
PERIOD OF PERFORMANCE END DATE: 02/28/2009

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DISCOVERY OF NOVEL PHARMACOTHERAPIES: COCAINE DEPENDENCE - DESCRIPTION (provided by applicant): Cocaine dependence is a problem of national significance. In the past decade there has been a considerable advance in the understanding of the chemistry and pharmacology of cocaine dependence. Notwithstanding, no cocaine pharmacotherapy has yet been approved by the FDA. A number of lead compounds are undergoing pharmacological evaluation as potential therapeutic agents. Cocaine's reinforcing properties and stimulant effects are associated with its propensity to bind to monoamine transporters. The goal of this project is to design potential pharmacotherapies for cocaine dependence. We will focus on the development of an understanding of the interaction between ligand and monoamine neurotransmitter uptake systems. We propose to expand our search for compounds that bind to DAT and SERT mechanisms but disturb dopamine (DA) uptake minimally, for compounds with slow onset and long duration of action, and for mechanism-based inhibitors of cocaine binding. We will focus on three classes: 8-oxabicyclo[3,2,1]octanes (oxatropanes), 8-azabicyclo[3,2,1]octanes (tropanes) and pyrovalerone analogues. The Specific Aims are: Synthesis and evaluation of (i) non-nitrogen tropane analogs, (ii) 6- and 7 hydroxylated 8-azatropane prodrugs, (iii) 6- and 7-hydroxylated 8-oxatropan(en)es, (iv) dopamine sparing cocaine antagonists that bind irreversibly to the cocaine site, (v) 3-heterobiaryltropanes. (vi) analogues of pyrovalerone.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2008 ( Subtotal = $379,817 )
2008	2008	ORGANIX, INC	240 SALEM STREET	WOBURN	MA	01801	MIDDLESEX	USA	Drug Use and Addiction Research Programs	000	10	3/3/2008	NON-COMPETING CONTINUATION	$379,817
														Subtotal = $379,817

Issue Date FY: 2007 ( Subtotal = $387,569 )
2007	2007	ORGANIX, INC	240 SALEM STREET	WOBURN	MA	01801	MIDDLESEX	USA	Drug Use and Addiction Research Programs	000	9	3/7/2007	NON-COMPETING CONTINUATION	$387,569
														Subtotal = $387,569

Issue Date FY: 2006 ( Subtotal = $399,144 )
2006	2006	ORGANIX, INC	240 SALEM STREET	WOBURN	MA	01801	MIDDLESEX	USA	Drug Use and Addiction Research Programs	000	8	2/13/2006	NON-COMPETING CONTINUATION	$399,144
														Subtotal = $399,144

Issue Date FY: 2005 ( Subtotal = $408,750 )
2005	2005	ORGANIX, INC	240 SALEM STREET	WOBURN	MA	01801	MIDDLESEX	USA	Drug Use and Addiction Research Programs	000	7	3/25/2005	NON-COMPETING CONTINUATION	$408,750
														Subtotal = $408,750

Issue Date FY: 2004 ( Subtotal = $435,000 )
2004	2004	ORGANIX, INC	240 SALEM STREET	WOBURN	MA	01801	MIDDLESEX	USA	Drug Use and Addiction Research Programs	000	6	5/12/2004	COMPETING CONTINUATION	$435,000
														Subtotal = $435,000

Issue Date FY: 2001 ( Subtotal = $264,702 )
2001	2001	ORGANIX, INC	240 SALEM STREET	WOBURN	MA	01801	MIDDLESEX	USA	Drug Use and Addiction Research Programs	000	5	6/26/2001	NON-COMPETING CONTINUATION	$264,702
														Subtotal = $264,702

Issue Date FY: 2000 ( Subtotal = $256,992 )
2000	2000	ORGANIX, INC	240 SALEM STREET	WOBURN	MA	01801	MIDDLESEX	USA	Drug Use and Addiction Research Programs	000	4	6/22/2000	NON-COMPETING CONTINUATION	$256,992
														Subtotal = $256,992

Issue Date FY: 1999 ( Subtotal = $249,508 )
1999	1999	ORGANIX, INC	240 SALEM STREET	WOBURN	MA	01801	MIDDLESEX	USA	Drug Use and Addiction Research Programs	000	3	6/22/1999	NON-COMPETING CONTINUATION	$249,508
														Subtotal = $249,508

Issue Date FY: 1998 ( Subtotal = $242,237 )
1998	1998	ORGANIX, INC	240 SALEM STREET	WOBURN	MA	01801	MIDDLESEX	USA	Drug Use and Addiction Research Programs	000	2	7/27/1998	NON-COMPETING CONTINUATION	$242,237
														Subtotal = $242,237

Grand Total All Awards = $3,023,719

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DISCOVERY OF NOVEL PHARMACOTHERAPIES: COCAINE DEPENDENCE

Award Number: R01DA011542

ORGANIZATION: NATIONAL INSTITUTE ON DRUG ABUSE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 09/30/1997

PERIOD OF PERFORMANCE END DATE: 02/28/2009

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