SPECT diagnostic agents for Parkinson’s Disease and ADHD
The Harvard research team has over two decades of experience in the design and synthesis of molecules that target monoamine uptake potently and selectively. The class of compounds utilized for the design of the subject SPECT agents is the 8-azabicyclo[3.2.1]octanes (tropanes). Potency and selectivity has been engineered into this class by careful selection of three dimensional asymmetry of the parent molecules. Two lead compounds, Technepine and Fluoratec, have been demonstrated to label the dopamine transporter in dopamine neurons in non-human primates and have proved highly promising.
Applications
Certain neurological disease, such as Parkinson’s Disease (PD) and Attention Deficit Hyperactivity Disorder (ADHD), are characterized by the compromised status of dopamine producing neurons in the striatum of the brain. The progression of PD is accompanied by a decrease in dopamine neurons. ADHD has been demonstrated to be accompanied by an increase in dopamine transporter (DAT) levels located on dopamine neurons. Therefore, a measure of the status of dopamine neurons can provide a window on the quantitative diagnosis of both PD and ADHD.
The preferred modality for evaluation of neuronal activity at the receptor or transporter level is the ultra-sensitive technique of measuring a radio emitter localized at the actual region of interest. Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) are well-accepted techniques in clinical use around the world. Diagnostic PET and SPECT imaging agents for PD have been under evaluation for some time. Very recently, an iodinated SPECT imaging agent, 123iodine-DatScan, has been brought onto the US market by GE Healthcare for the diagnosis of PD.
The Harvard research team has over two decades of experience in the design and synthesis of molecules that target monoamine uptake potently and selectively. The class of compounds utilized for the design of the subject SPECT agents is the 8-azabicyclo[3.2.1]octanes (tropanes). Potency and selectivity has been engineered into this class by careful selection of three dimensional asymmetry of the parent molecules. Two lead compounds, Technepine and Fluoratec, have been demonstrated to label the dopamine transporter in dopamine neurons in non-human primates and have proved highly promising.
Certain neurological disease, such as Parkinson’s Disease (PD) and Attention Deficit Hyperactivity Disorder (ADHD), are characterized by the compromised status of dopamine producing neurons in the striatum of the brain. The progression of PD is accompanied by a decrease in dopamine neurons. ADHD has been demonstrated to be accompanied by an increase in dopamine transporter (DAT) levels located on dopamine neurons. Therefore, a measure of the status of dopamine neurons can provide a window on the quantitative diagnosis of both PD and ADHD.
The preferred modality for evaluation of neuronal activity at the receptor or transporter level is the ultra-sensitive technique of measuring a radio emitter localized at the actual region of interest. Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) are well-accepted techniques in clinical use around the world. Diagnostic PET and SPECT imaging agents for PD have been under evaluation for some time. Very recently, an iodinated SPECT imaging agent, 123iodine-DatScan, has been brought onto the US market by GE Healthcare for the diagnosis of PD.
Intellectual Property Status: Patent(s) Pending
Case Number: 1624