Contact

Porträt Prof. Dr. Brust, Peter; FWPN

Prof. Dr. Peter Brust
Head Neuroradiopharmaceuticals
p.brustAthzdr.de
Phone: +49 351 260 - 4610
Fax: +49 351 260 - 4699

[18F]NCFHEB/[18F]Flubatine a potential PET marker of early Alzheimer`s disease


The nicotinic α4β2 acetylcholine receptors are an important target for diagnostic neuroimaging and drug development because of their involvement in learning and memory processes, neuropsychiatric diseases such as Alzheimer´s disease, Parkinsons´s disease, Tourette´s syndrome, epilepsy, autism, attention-deficit hyperactivity disorder, schizophrenia, and depression, as well as drug addiction and pain. In our group, a highly affine and selective α4β2 nAChR targeting radiotracer has been developed which is related on the structure of the alkaloid epibatidine. The two radiolabeled stereoisomers of norchloro-fluoro-homoepibatidine, (+)-[18F]flubatine and (-)-[18F]flubatine, were investigated in piglets in dynamic PET studies. (-)-[18F]flubatine proofed to possess radiotracer properties superior to the clinically used 2-[18F]F-A85380, and is currently assessed in man to quantitatively image α4β2nAChR in the living brain.

Development of [18F]flubatine

Partner

  • Department of Nuclear Medicine and Department of Psychiatry, University of Leipzig

  • Central Institute for Electronics, Research Center Juelich

  • Advanced Biochemical Compounds ABX GmbH, Radeberg

Publications

  • 1. Meyer PM, Strecker K, Kendziorra K, Becker G, Hesse S, Woelpl D, Hensel A, Patt M, Sorger D, Wegner F, Lobsien D, Barthel H, Brust P, Gertz HJ, Sabri O, Schwarz J. Reduced alpha4beta2*-nicotinic acetylcholine receptor binding and its relationship to mild cognitive and depressive symptoms in Parkinson disease. Arch Gen Psychiatry. 2009,66(8):866-77.

  • 2. Brust P, Patt JT, Deuther-Conrad W, Becker G, Patt M, Schildan A, Sorger D, Kendziorra K, Meyer P, Steinbach J, Sabri O. In vivo measurement of nicotinic acetylcholine receptors with [18F]norchloro-fluoro-homoepibatidine. Synapse. 2008,62(3):205-18.
  • 3. Deuther-Conrad W, Patt JT, Lockman PR, Allen DD, Patt M, Schildan A, Ganapathy V, Steinbach J, Sabri O, Brust P. Norchloro-fluoro-homoepibatidine (NCFHEB) - a promising radioligand for neuroimaging nicotinic acetylcholine receptors with PET. Eur Neuropsychopharmacol. 2008,18(3):222-9.

Contact

Prof. Dr. Peter Brust
Head Neuroradiopharmaceuticals
p.brustAthzdr.de
Phone: +49 351 260 - 4610
Fax: +49 351 260 - 4699