Radiofluorinated histamine H3 receptor antagonist as a potential probe for in vivo PET imaging: Radiosynthesis and pharmacological evaluation

Svetlana V. Selivanova; Michael Honer; Francine Combe; Kathleen Isensee; Holger Stark; Stefanie D. Krämer; P. August Schubiger; Simon M. Ametamey

doi:10.1016/j.bmc.2012.03.024

Radiofluorinated histamine H3 receptor antagonist as a potential probe for in vivo PET imaging: Radiosynthesis and pharmacological evaluation

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2012.03.024 ◽

2012 ◽

Vol 20 (9) ◽

pp. 2889-2896 ◽

Cited By ~ 8

Author(s):

Svetlana V. Selivanova ◽

Michael Honer ◽

Francine Combe ◽

Kathleen Isensee ◽

Holger Stark ◽

...

Keyword(s):

Receptor Antagonist ◽

Pet Imaging ◽

Histamine H3 Receptor ◽

Pharmacological Evaluation ◽

H3 Receptor ◽

Histamine H3

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4-Hydroxypiperidines and Their Flexible 3-(Amino)propyloxy Analogues as Non-Imidazole Histamine H3 Receptor Antagonist: Further Structure–Activity Relationship Exploration and In Vitro and In Vivo Pharmacological Evaluation

International Journal of Molecular Sciences ◽

10.3390/ijms19041243 ◽

2018 ◽

Vol 19 (4) ◽

pp. 1243

Author(s):

Beata Olszewska ◽

Anna Stasiak ◽

Daniel McNaught Flores ◽

Wiesława Fogel ◽

Rob Leurs ◽

...

Keyword(s):

Receptor Antagonist ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Histamine H3 Receptor ◽

Pharmacological Evaluation ◽

Structure Activity ◽

H3 Receptor ◽

Histamine H3

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A Novel Potent and Selective Histamine H3 Receptor Antagonist Enerisant: In Vitro Profiles, In Vivo Receptor Occupancy, and Wake-Promoting and Procognitive Effects in Rodents

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.120.000185 ◽

2020 ◽

Vol 375 (2) ◽

pp. 276-285

Author(s):

Noriko Hino ◽

Toshiyuki Marumo ◽

Makiko Kotani ◽

Toshiharu Shimazaki ◽

Ayaka Kaku-Fukumoto ◽

...

Keyword(s):

Receptor Antagonist ◽

Receptor Occupancy ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Histamine H3

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ChemInform Abstract: Development of FUB 181, a Selective Histamine H3-Receptor Antagonist of High Oral in vivo Potency with 4-(ω-(Arylalkyloxy)alkyl)-1H-imidazole Structure.

ChemInform ◽

10.1002/chin.199844130 ◽

2010 ◽

Vol 29 (44) ◽

pp. no-no

Author(s):

H. STARK ◽

A. HUELS ◽

X. LIGNEAU ◽

K. PURAND ◽

H. PERTZ ◽

...

Keyword(s):

Receptor Antagonist ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Histamine H3

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ChemInform Abstract: Diphenylmethyl Ethers: Synthesis and Histamine H3-Receptor Antagonist in vitro and in vivo Activity.

ChemInform ◽

10.1002/chin.199652144 ◽

2010 ◽

Vol 27 (52) ◽

pp. no-no

Author(s):

A. HUELS ◽

K. PURAND ◽

H. STARK ◽

X. LIGNEAU ◽

J.-M. ARRANG ◽

...

Keyword(s):

Receptor Antagonist ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Histamine H3

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In vivo receptor occupancy assay of histamine H3 receptor antagonist in rats using non-radiolabeled tracer

Journal of Pharmacological and Toxicological Methods ◽

10.1016/j.vascn.2012.03.003 ◽

2012 ◽

Vol 65 (3) ◽

pp. 115-121 ◽

Cited By ~ 10

Author(s):

Ramakrishna Nirogi ◽

Vishwottam Kandikere ◽

Gopinadh Bhyrapuneni ◽

Nageswararao Muddana ◽

Ramanatha Saralaya ◽

...

Keyword(s):

Receptor Antagonist ◽

Receptor Occupancy ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Histamine H3

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Diphenylmethyl ethers: synthesis and histamine H3-receptor antagonist in vitro and in vivo activity

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/0960-894x(96)00361-7 ◽

1996 ◽

Vol 6 (16) ◽

pp. 2013-2018 ◽

Cited By ~ 15

Author(s):

A Hüls ◽

K Purand ◽

H Stark ◽

X Ligneau ◽

J.-M Arrang ◽

...

Keyword(s):

Receptor Antagonist ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Histamine H3

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Search for multifunctional agents against Alzheimer’s disease among non-imidazole histamine H3 receptor ligands. In vitro and in vivo pharmacological evaluation and computational studies of piperazine derivatives

Bioorganic Chemistry ◽

10.1016/j.bioorg.2019.103084 ◽

2019 ◽

Vol 90 ◽

pp. 103084 ◽

Cited By ~ 1

Author(s):

Jakub Jończyk ◽

Krzysztof Lodarski ◽

Marek Staszewski ◽

Justyna Godyń ◽

Paula Zaręba ◽

...

Keyword(s):

Computational Studies ◽

Receptor Ligands ◽

Histamine H3 Receptor ◽

Pharmacological Evaluation ◽

Piperazine Derivatives ◽

H3 Receptor ◽

Multifunctional Agents ◽

Histamine H3

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Radiosynthesis of a Histamine H3 receptor antagonist: In vitro and in vivo evaluation

NeuroImage ◽

10.1016/j.neuroimage.2006.04.037 ◽

2006 ◽

Vol 31 ◽

pp. T46

Author(s):

Anu J. Airaksinen ◽

J.A. Jablonowski ◽

M. van der Mey ◽

A.J. Barbier ◽

R.P. Klok ◽

...

Keyword(s):

Receptor Antagonist ◽

In Vivo Evaluation ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Histamine H3

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Effect of histamine H3-receptor antagonist, clobenpropit on the induction of diarrhea by endotoxin:Continuous monitoring of monoamine and its metabolites concentrations in the blood by in viVo microdialysis system

The Japanese Journal of Pharmacology ◽

10.1016/s0021-5198(19)44820-8 ◽

1997 ◽

Vol 73 ◽

pp. 78

Author(s):

Jun Yamakami ◽

Eiichi Sakurai ◽

Tomoya Sakurada ◽

Akio Nomura ◽

Noboru Hikichi

Keyword(s):

Receptor Antagonist ◽

In Vivo Microdialysis ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Histamine H3

Download Full-text

Ameliorating effects of histamine H3 receptor antagonist E177 on acute pentylenetetrazole-induced memory impairments in rats

Behavioural Brain Research ◽

10.1016/j.bbr.2021.113193 ◽

2021 ◽

Vol 405 ◽

pp. 113193

Author(s):

Alaa Alachkar ◽

Mohamed Lotfy ◽

Ernest Adeghate ◽

Dorota Łażewska ◽

Katarzyna Kieć-Kononowicz ◽

...

Keyword(s):

Receptor Antagonist ◽

Histamine H3 Receptor ◽

Memory Impairments ◽

H3 Receptor ◽

Histamine H3

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