Fluorinated and iodinated dopamine agents

Details Fluorinated and iodinated dopamine agents Fluorinated and iodinated dopamine agents

1992-04-03

1995-08-29

Geist, Gary

Organic compounds -- part of the class 532-570 series

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

546124, 546224, 548567, C07D22316, C07D45102, C07D21156, C07D20708

Patent

active

054461472

ABSTRACT:
This invention relates to novel dopamine D-1 and D-2 imaginging agents which are both fluorinated and iodinated and can appropriately labelled for use in both PET and SPECT imaging. Compounds include S-(-)-2-fluoroethoxy-3-methyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-iodoben zamide and R(+)-2,3-dimethoxy-N-[(1-(4'-fluorobenzyl)-2-pyrrolidinyl)methyl]-5-iodobe nzamide.

REFERENCES:
patent: 5068326 (1991-11-01), Kung
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Billings, J. J., et al., "Characterization of Radioiodinated TISCH: A High-Affinity and Selective Ligand for Mapping CNS D.sub.1 Dopamine Receptor", J. Neurochem 58, No. 1: 227-236 (1992).
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Hogberg, T., et al., "Potential Antipsychotic Agents. 9. Synthesis and Stereoselective Dopamine D-2 Receptor Blockade of a Potent Class of Substituted (R)-N-[(1-Benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to Other Side Chain Congeners", J. Med. Chem. 34: 948-955 (1991).
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Murphy, R. A., et al., "Synthesis and Characterization of Iodobenzamide Analogues: Potential D-2 Dopamine Receptor Imaging Agents", J. Med. Chem. 33, No. 1:171-178 (1990).
Kung, H. F., et al., "Current and Future Radiopharmaceuticals for Brain Imaging With Single Photon Emission Computed Tomography", Seminars in Nuclear Medicine, vol. XX, No. 4: 290-302 (1990).
Kung, H. F., et al., "In Vitro and In Vivo Evaluation of [.sup.123 I]IBZM: A Potential CNS D-2 Dopamine Receptor Imaging Agent", J. Nucl. Med. 30, No. 1: 88-92 (1989).
Kung, H. F., et al., "In Vivo SPECT Imaging of CNS D-2 Dopamine Receptors: Initial Studies with Iodine-123-IBZM in Humans", J. Nucl. Med. 31: 573-579 (1990).
Kung, M-P., et al., "The Characterization of IBF as a New Selective Dopamine D-2 Receptor Imaging Agent", J. Nucl Med. 31: 648-654 (1990).
Kung, M-P., et al., "A Kit Formulation for Preparation of Iodine-123-IBZM: A New CNS D-2 Dopamine Receptor Imaging Agent", J. Nucl. Med. 32: 339-342 (1991).
Hoegberg et al., "Synthesis & Binding Properties of the New Fluorinated Benzamide NCQ616", Acta Pharm. Nord. 4(4), pp. 297-300, 1992. (abstract provided in action).

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