Nuclear Medicine and Biology
Volume 33, Issue 5 , Pages 599-605 , July 2006

Imaging of aromatase distribution in rat and rhesus monkey brains with [11C]vorozole

  • Kayo Takahashi

      Affiliations

    • Division of Pharmacology, Department of Neuroscience, Uppsala University, Uppsala SE-75124, Sweden
    • Uppsala Imanet, Uppsala SE-75109, Sweden
    • Corresponding Author InformationCorresponding author. Uppsala Imanet, PO Box 967, Uppsala SE-75109, Sweden. Tel.: +46 18 666865; fax: +46 18 666819.
  • ,
  • Mats Bergström

      Affiliations

    • Uppsala Imanet, Uppsala SE-75109, Sweden
    • Department of Pharmaceutical Biosciences, Uppsala University, Uppsala SE-75124, Sweden
  • ,
  • Pernilla Frändberg

      Affiliations

    • Uppsala Imanet, Uppsala SE-75109, Sweden
  • ,
  • Eva-Lotta Vesström

      Affiliations

    • Uppsala Imanet, Uppsala SE-75109, Sweden
  • ,
  • Yasuyoshi Watanabe

      Affiliations

    • Department of Physiology, Osaka City University Graduate School of Medicine, Osaka 545-8585, Japan
  • ,
  • Bengt Långström

      Affiliations

    • Uppsala Imanet, Uppsala SE-75109, Sweden

Received 30 September 2005 ,Revised 12 March 2006 ,Accepted 17 March 2006.

References 

  1. Lephart ED. A review of brain aromatase cytochrome P450. Brain Res Brain Res Rev. 1996;22:1–26
  2. Roselli CE, Abdelgadir SE, Ronnekleiv OK, Klosterman SA. Anatomic distribution and regulation of aromatase gene expression in the rat brain. Biol Reprod. 1998;58:79–87
  3. Roselli CE. The effect of anabolic–androgenic steroids on aromatase activity and androgen receptor binding in the rat preoptic area. Brain Res. 1998;792:271–276
  4. Wagner CK, Morrell JI. Distribution and steroid hormone regulation of aromatase mRNA expression in the forebrain of adult male and female rats: a cellular-level analysis using in situ hybridization. J Comp Neurol. 1996;370:71–84
  5. Balthazart J, Foidart A. Brain aromatase and the control of male sexual behavior. J Steroid Biochem Mol Biol. 1993;44:521–540
  6. Abdelgadir SE, Resko JA, Ojeda SR, Lephart ED, McPhaul MJ, Roselli CE. Androgens regulate aromatase cytochrome P450 messenger ribonucleic acid in rat brain. Endocrinology. 1994;135:395–401
  7. Foidart A, Harada N, Balthazart J. Effects of steroidal and non steroidal aromatase inhibitors on sexual behavior and aromatase-immunoreactive cells and fibers in the quail brain. Brain Res. 1994;657:105–123
  8. Foidart A, Harada N, Balthazart J. Aromatase-immunoreactive cells are present in mouse brain areas that are known to express high levels of aromatase activity. Cell Tissue Res. 1995;280:561–574
  9. Rissman EF, Harada N, Roselli CE. Effect of vorozole, an aromatase enzyme inhibitor, on sexual behavior, aromatase activity and neural immunoreactivity. J Neuroendocrinol. 1996;8:199–210
  10. Brodie AMH. Inhibitors of steroid biosynthesis. In:  Sandler M,  Harold J editor. Design of enzyme inhibitors as drugs. Oxford: Oxford University Press; 1994;p. 503–522
  11. Wouters W, Snoeck E, De Coster R. Vorozole, a specific non-steroidal aromatase inhibitor. Breast Cancer Res Treat. 1994;30:89–94
  12. Plourde PV, Dyroff M, Dowsett M, Demers L, Yates R, Webster A. ARIMIDEX: a new oral, once-a-day aromatase inhibitor. J Steroid Biochem Mol Biol. 1995;53:175–179
  13. Dowsett M, Jones A, Johnston SR, Jacobs S, Trunet P, Smith IE. In vivo measurement of aromatase inhibition by letrozole (CGS 20267) in postmenopausal patients with breast cancer. Clin Cancer Res. 1995;1:1511–1515
  14. Lidström P, Bonasera TA, Kirilovas D, Lindblom B, Lu L, Bergström E, et al. Synthesis, in vivo rhesus monkey biodistribution and in vitro evaluation of a 11C-labelled potent aromatase inhibitor: [N-methyl-11C]vorozole. Nucl Med Biol. 1998;25:497–501
  15. Azcoitia I, Sierra A, Veiga S, Honda S, Harada N, Garcia-Segura LM. Brain aromatase is neuroprotective. J Neurobiol. 2001;47:318–329
  16. Iivonen S, Corder E, Lehtovirta M, Helisalmi S, Mannermaa A, Vepsäläinen S, et al. Polymorphisms in the CYP19 gene confer increased risk for Alzheimer disease. Neurology. 2004;62:1170–1176
  17. Ishunina TA, van Beurden D, van der Meulen G, Unmehopa UA, Hol EM, Huitinga I, et al. Diminished aromatase immunoreactivity in the hypothalamus, but not in the basal forebrain nuclei in Alzheimer's disease. Neurobiol Aging. 2005;26:173–194
  18. Sihver S, Sihver W, Bergström M, Höglund AU, Sjöberg P, Långström B, et al. Quantitative autoradiography with short-lived positron emission tomography tracers: a study on muscarinic acetylcholine receptors with N-[(11)C]methyl-4-piperidylbenzilate. J Pharmacol Exp Ther. 1999;290:917–922
  19. Sihver W, Sihver S, Bergström M, Murata T, Matsumura K, Onoe H, et al. Methodological aspects for in vitro characterization of receptor binding using 11C-labeled receptor ligands: a detailed study with the benzodiazepine receptor antagonist [11C]Ro 15-1788. Nucl Med Biol. 1997;24:723–731
  20. Wagner CK, Morrell JI. Neuroanatomical distribution of aromatase mRNA in the rat brain: indications of regional regulation. J Steroid Biochem Mol Biol. 1997;61:307–314
  21. Roselli CE, Horton LE, Resko JA. Distribution and regulation of aromatase activity in the rat hypothalamus and limbic system. Endocrinology. 1985;117:2471–2477
  22. Roselli CE, Ellinwood WE, Resko JA. Regulation of brain aromatase activity in rats. Endocrinology. 1984;114:192–200
  23. Roselli CE, Resko JA. The distribution and regulation of aromatase activity in the central nervous system. Steroids. 1987;50:495–508
  24. Roselli CE. Sex differences in androgen receptors and aromatase activity in microdissected regions of the rat brain. Endocrinology. 1991;128:1310–1316
  25. Roselli CE, Abdelgadir SE, Resko JA. Regulation of aromatase gene expression in the adult rat brain. Brain Res Bull. 1997;44:351–357
  26. Koymans LM, Moereels H, Vanden Bossche H. A molecular model for the interaction between vorozole and other non-steroidal inhibitors and human cytochrome P450 19 (P450 aromatase). J Steroid Biochem Mol Biol. 1995;53:191–197
  27. Krekels MD, Wouters W, De Coster R. Aromatase inhibition by R 76 713: a kinetic analysis in rat ovarian homogenates. Steroids. 1990;55:69–73
  28. Krekels MD, Wouters W, De Coster R, Van Ginckel R, Leonaers A, Janssen PA. Aromatase in the human choriocarcinoma JEG-3: inhibition by R 76 713 in cultured cells and in tumors grown in nude mice. J Steroid Biochem Mol Biol. 1991;38:415–422
  29. Vanden Bossche H, Willemsens G, Roels I, Bellens D, Moereels H, Coene MC, et al. R 76713 and enantiomers: selective, nonsteroidal inhibitors of the cytochrome P450-dependent oestrogen synthesis. Biochem Pharmacol. 1990;40:1707–1718
  30. Wouters W, De Coster R, Beerens D, Doolaege R, Gruwez JA, Van Camp K, et al. Potency and selectivity of the aromatase inhibitor R 76,713. A study in human ovarian, adipose stromal, testicular and adrenal cells. J Steroid Biochem. 1990;36:57–65
  31. Abdelgadir SE, Roselli CE, Choate JV, Resko JA. Distribution of aromatase cytochrome P450 messenger ribonucleic acid in adult rhesus monkey brains. Biol Reprod. 1997;57:772–777
  32. Roselli CE, Resko JA. Aromatase activity in the rat brain: hormonal regulation and sex differences. J Steroid Biochem Mol Biol. 1993;44:499–508
  33. Roselli CE, Salisbury RL, Resko JA. Genetic evidence for androgen-dependent and independent control of aromatase activity in the rat brain. Endocrinology. 1987;121:2205–2210

PII: S0969-8051(06)00063-1

doi: 10.1016/j.nucmedbio.2006.03.009

Nuclear Medicine and Biology
Volume 33, Issue 5 , Pages 599-605 , July 2006