Halopiperidines for imaging of monoamine transporters

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$190,643.00
Award Year:
2003
Program:
SBIR
Phase:
Phase I
Contract:
1R43NS046109-01
Award Id:
66716
Agency Tracking Number:
NS046109
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
MOLECULAR INSIGHT PHARMACEUTICALS, INC., 160 2ND ST, CAMBRIDGE, MA, 02142
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
MILES SMITH
(617) 492-5554
msmith@molecularinsight.com
Business Contact:
(617) 492-5554
Research Institution:
n/a
Abstract
DESCRIPTION (provided by applicant): The monoamine transporters are important targets for therapy, diagnosis and monitoring of a number of CNS disease states. It is expected that imaging agents that exhibit high affinity and selectivity for the dopamine transporter (DAT) would fulfill a number of unmet needs including use for Parkinson's disease (PD), ADD/ADHD, depression and cocaine abuse. Additionally, imaging agents that exhibit high affinity and selectivity for either the serotonin or norepinephrine transporters would similarly be of utility for the diagnosis and monitoring of depressive syndromes and related disorders. While, many studies have reported the design of radioligands for the DAT no agents have been disclosed that exhibit favorable imaging properties that are required for widespread utilization. Fewer reports are available on specific radioligands for the serotonin (5-HTT) and norepinephrine (NET) transporters. Herein, we propose the rational design and synthesis a series of halogenated piperidines as potential radio-tracers for imaging of the monoamine transporters utilizing PET and SPECT. These studies utilize our versatile and efficient piperidine pharmacophore for the facile preparation of highly selective monoamine transporter ligands exploiting the divergent structure activity relationships for the enantiomers/isomers of the piperidine. In this manner it is anticipated that this work will result in the identification of new radiopharmaceuticals that can be labeled with positron emitting elements for PET, or single photon emitting elements for SPECT. These radiopharmaceuticals would be of wide spread use for both the diagnosis of CNS disorders and the monitoring of therapeutic interventions.

* information listed above is at the time of submission.

Agency Micro-sites


SBA logo

Department of Agriculture logo

Department of Commerce logo

Department of Defense logo

Department of Education logo

Department of Energy logo

Department of Health and Human Services logo

Department of Homeland Security logo

Department of Transportation logo

Enviromental Protection Agency logo

National Aeronautics and Space Administration logo

National Science Foundation logo
US Flag An Official Website of the United States Government