Autoradiographic evaluation of [3H]CUMI-101, a novel, selective 5-HT1AR ligand in human and baboon brain

被引：10

作者：

Kumar, J. S. Dileep ^{[1
,2
]}

Parsey, Ramin V. ^{[3
]}

Kassir, Suham A. ^{[1
]}

Majo, Vattoly J. ^{[2
]}

Milak, Matthew S. ^{[1
,2
]}

Prabhakaran, Jaya ^{[2
]}

Simpson, Norman R. ^{[1
]}

Underwood, Mark D. ^{[1
,2
]}

Mann, J. John ^{[1
,2
,4
]}

Arango, Victoria ^{[1
,2
]}

机构：

[1] New York State Psychiat Inst & Hosp, Div Mol Imaging & Neuropathol, New York, NY 10032 USA

[2] Columbia Univ, Dept Psychiat, Coll Phys & Surg, New York, NY 10032 USA

[3] SUNY Stony Brook, Dept Psychiat & Behav Sci, Stony Brook, NY 11794 USA

[4] Columbia Univ, Dept Radiol, Coll Phys & Surg, New York, NY 10032 USA

来源：

BRAIN RESEARCH | 2013年 / 1507卷

关键词：

Autoradiography; 5-HT1AR; Brain; Serotonin Agonist; IN-VIVO; RECEPTOR AGONIST; PREFRONTAL CORTEX; INCREASED BINDING; H-3; WAY-100635; RAT; 8-OH-DPAT; PET; RADIOLIGAND; ANTAGONIST;

D O I：

10.1016/j.brainres.2013.02.035

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

[C-11]CUMI-101 is the first selective serotonin receptor (5-HT1AR) partial agonist radiotracer for positron emission tomography (PET) tested in vivo in nonhuman primates and humans. We evaluated specific binding of [H-3]CUMI-101 by quantitative autoradiography studies in postmortem baboon and human brain sections using the 5-HT1AR antagonist WAY-100635 as a displacer. The regional and laminar distributions of [H-3]CUMI-101 binding in baboon and human brain sections matched the known distribution of [H-3]8-OH-DPAT and [H-3]WAY-100635. Prazosin did not measurably displace [H-3]CUMI-101 binding in baboon or human brain. sections, thereby ruling out [H-3]CUMI-101 binding to alpha 1-adrenergic receptors. This study demonstrates that [C-11]CUMI-101 is a selective 5-HT1AR ligand for in vivo and in vitro studies in baboon and human brain. (C) 2013 Elsevier B.V. All rights reserved.

引用

页码：11 / 18

页数：8

共 43 条

[31] The 5HT1A receptor ligand, S15535, antagonises G-protein activation:: a [35S]GTPγS and [3H]S15535 autoradiography study [J].

Newman-Tancredi, A ;

Rivet, JM ;

Chaput, C ;

Touzard, M ;

Verrièle, L ;

Millan, MJ .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1999, 384 (2-3) :111-121

[32] Preliminary evaluation of 2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-3-methyl-6-methoxy-4(3H)-quinazolinone ([±]HX-CH 44) as a selective β1-adrenoceptor ligand for PET [J].

Valette, H ;

Dollé, F ;

Guenther, I ;

Demphel, S ;

Rasetti, C ;

Hinnen, F ;

Fuseau, C ;

Crouzel, C .

NUCLEAR MEDICINE AND BIOLOGY, 1999, 26 (01) :105-109

[33] Characterization of [3H]-N-[R-(2-benzothiazolyl)thio-2-propyl]-2-chloroadenosine ([3H]-NNC 21-0136) binding to rat brain:: Profile of a novel selective agonist for adenosine A1 receptors [J].

Thomsen, C ;

Valsborg, JS ;

Foged, C ;

Knutsen, L .

DRUG DEVELOPMENT RESEARCH, 1997, 42 (02) :86-97

[34] Antidepressant-like activity and safety profile evaluation of 1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione derivatives as 5-HT1Areceptor partial agonists [J].

Partyka, Anna ;

Zagorska, Agnieszka ;

Kotanska, Magdalena ;

Walczak, Maria ;

Jastrzebska-Wiesek, Magdalena ;

Knutelska, Joanna ;

Bednarski, Marek ;

Gluch-Lutwin, Monika ;

Mordyl, Barbara ;

Janiszewska, Paulina ;

Wesolowska, Anna .

PLOS ONE, 2020, 15 (08)

[35] Efficacy of antipsychotic agents at human 5-HT1A receptors determined by [3H]WAY100,635 binding affinity ratios:: Relationship to efficacy for G-protein activation [J].

Newman-Tancredi, A ;

Verrièle, L ;

Touzard, M ;

Millan, MJ .

EUROPEAN JOURNAL OF PHARMACOLOGY, 2001, 428 (02) :177-184

[36] AUTORADIOGRAPHIC IDENTIFICATION AND CHARACTERIZATION OF SIGMA RECEPTORS IN GUINEA-PIG BRAIN USING [H-3] 1(CYCLOPROPYLMETHYL)-4-(2'-(4''-FLUOROPHENYL)-2'-OXOETHYL) PIPERIDINE ([H-3]DUP 734), A NOVEL SIGMA RECEPTOR LIGAND [J].

HEROUX, JA ;

TAM, SW ;

DESOUZA, EB .

BRAIN RESEARCH, 1992, 598 (1-2) :76-86

[37] Synthesis and biological evaluation of novel 3-(5-substituted-1H-indol-3-yl) pyrrolidine-2,5-dione derivatives with a dual affinity for serotonin 5-HT1A receptor and SERT [J].

Wrobel, Martyna Z. ;

Chodkowski, Andrzej ;

Dawidowski, Maciej ;

Siwek, Agata ;

Stachowicz, Katarzyna ;

Szewczyk, Bernadeta ;

Nowak, Gabriel ;

Satala, Grzegorz ;

Bojarski, Andrzej J. ;

Turlo, Jadwiga .

BIOORGANIC CHEMISTRY, 2023, 141

[38] AUTORADIOGRAPHIC DISTRIBUTION OF BRAIN NEUROKININ-1 SUBSTANCE-P RECEPTORS USING A HIGHLY SELECTIVE LIGAND [H3]-[SAR9,MET(O-2)11]-SUBSTANCE-P [J].

DAM, TV ;

MARTINELLI, B ;

QUIRION, R .

BRAIN RESEARCH, 1990, 531 (1-2) :333-337

[39] Syntheses and structure-activity relationships of novel, potent, and selective trans-2-[3-oxospiro[isobenzofuran-1(3H),1′-cyclohexan]-4′-yl]benzimidazole NPYY5 receptor antagonists [J].

Ogino, Yoshio ;

Ohtake, Norikazu ;

Nagae, Yoshikazu ;

Matsuda, Kenji ;

Ishikawa, Makoto ;

Moriya, Minoru ;

Kanesaka, Maki ;

Mitobe, Yuko ;

Ito, Junko ;

Kanno, Tetsuya ;

Ishihara, Akane ;

Iwaasa, Hisashi ;

Ohe, Tomoyuki ;

Kanatani, Akio ;

Fukami, Takehiro .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (18) :4997-5001

[40] Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl-11C]2-(4-(4-(2-methoxyphenyl) piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3, 5(2H,4H)dione in nonhuman primates [J].

Kumar, J. S. Dileep ;

Prabhakaran, Jaya ;

Majo, Vattoly J. ;

Milak, Matthew S. ;

Hsiung, Shu-Chi ;

Tamir, Hadassah ;

Simpson, Norman R. ;

Van Heertum, Ronald L. ;

Mann, J. John ;

Parsey, Ramin V. .

EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2007, 34 (07) :1050-1060

← 1 2 3 4 5 →