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Autoradiographic evaluation of [.sup.3H]CUMI-101, a novel, selective 5-HT.sub.1AR ligand in human and baboon brain.(Report)

Brain Research, April 24, 2013, Vol.1507, p.11(8) [Tạp chí có phản biện]

ISSN: 0006-8993

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  • Nhan đề:
    Autoradiographic evaluation of [.sup.3H]CUMI-101, a novel, selective 5-HT.sub.1AR ligand in human and baboon brain.(Report)
  • Chủ đề: Prazosin -- Evaluation
  • Là 1 phần của: Brain Research, April 24, 2013, Vol.1507, p.11(8)
  • Mô tả: To link to full-text access for this article, visit this link: http://dx.doi.org/10.1016/j.brainres.2013.02.035 Byline: J.S. Dileep Kumar (a)(b), Ramin V. Parsey (c), Suham A. Kassir (a), Vattoly J. Majo (b), Matthew S. Milak (a)(b), Jaya Prabhakaran (b), Norman R. Simpson (a), Mark D. Underwood (a)(b), J. John Mann (a)(b)(d), Victoria Arango (a)(b) Keywords: Autoradiography; 5-HT.sub.1AR; Brain; Serotonin Agonist Abstract: [.sup.11C]CUMI-101 is the first selective serotonin receptor (5-HT.sub.1AR) partial agonist radiotracer for positron emission tomography (PET) tested in vivo in nonhuman primates and humans. We evaluated specific binding of [.sup.3H]CUMI-101 by quantitative autoradiography studies in postmortem baboon and human brain sections using the 5-HT.sub.1AR antagonist WAY-100635 as a displacer. The regional and laminar distributions of [.sup.3H]CUMI-101 binding in baboon and human brain sections matched the known distribution of [.sup.3H]8-OH-DPAT and [.sup.3H]WAY-100635. Prazosin did not measurably displace [.sup.3H]CUMI-101 binding in baboon or human brain sections, thereby ruling out [.sup.3H]CUMI-101 binding to [alpha]1-adrenergic receptors. This study demonstrates that [.sup.11C]CUMI-101 is a selective 5-HT.sub.1AR ligand for in vivo and in vitro studies in baboon and human brain. Author Affiliation: (a) Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, USA (b) Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, USA (c) Department of Psychiatry and Behavioral Sciences, Stony Brook University, Stony Brook, NY, USA (d) Department of Radiology, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA Article History: Accepted 20 February 2013
  • Ngôn ngữ: English
  • Số nhận dạng: ISSN: 0006-8993

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