New Histamine H3-Receptor Ligands of the Proxifan Series:  Imoproxifan and Other Selective Antagonists with High Oral in Vivo Potency†

Astrid Sasse; Bassem Sadek; Xavier Ligneau; Sigurd Elz; Heinz H. Pertz; Peter Luger; C. Robin Ganellin; Jean-Michel Arrang; Jean-Charles Schwartz; Walter Schunack; Holger Stark

doi:10.1021/jm000971p

New Histamine H3-Receptor Ligands of the Proxifan Series: Imoproxifan and Other Selective Antagonists with High Oral in Vivo Potency†

Journal of Medicinal Chemistry ◽

10.1021/jm000971p ◽

2000 ◽

Vol 43 (17) ◽

pp. 3335-3343 ◽

Cited By ~ 19

Author(s):

Astrid Sasse ◽

Bassem Sadek ◽

Xavier Ligneau ◽

Sigurd Elz ◽

Heinz H. Pertz ◽

...

Keyword(s):

Receptor Ligands ◽

Histamine H3 Receptor ◽

Selective Antagonists ◽

H3 Receptor ◽

Histamine H3

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ChemInform Abstract: New Histamine H3-Receptor Ligands of the Proxifan Series: Imoproxifan and Other Selective Antagonists with High Oral in vivo Potency.

ChemInform ◽

10.1002/chin.200051123 ◽

2000 ◽

Vol 31 (51) ◽

pp. no-no

Author(s):

Holger Stark ◽

et al. et al.

Keyword(s):

Receptor Ligands ◽

Histamine H3 Receptor ◽

Selective Antagonists ◽

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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In vivo modulation of rat hypothalamic histamine release by the histamine H3 receptor ligands, immepip and clobenpropit. Effects of intrahypothalamic and peripheral application

European Journal of Pharmacology ◽

10.1016/s0014-2999(98)00739-0 ◽

1998 ◽

Vol 362 (2-3) ◽

pp. 149-155 ◽

Cited By ~ 30

Author(s):

Frank P Jansen ◽

Takatoshi Mochizuki ◽

Yumiko Yamamoto ◽

Hendrik Timmerman ◽

Atsushi Yamatodani

Keyword(s):

Histamine Release ◽

Receptor Ligands ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Hypothalamic Histamine ◽

Histamine H3

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Diether (substituted) piperidine derivatives as novel, histamine H3 receptor ligands

Inflammation Research ◽

10.1007/s00011-009-2002-6 ◽

2009 ◽

Vol 58 (S1) ◽

pp. 47-48

Author(s):

K. J. Kuder ◽

X. Ligneau ◽

J.-C. Camelin ◽

D. Łażewska ◽

J.-C. Schwartz ◽

...

Keyword(s):

Receptor Ligands ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Histamine H3

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Metabolic benefits of novel histamine H3 receptor ligands in the model of excessive eating: The importance of intrinsic activity and pharmacokinetic properties

Biomedicine & Pharmacotherapy ◽

10.1016/j.biopha.2021.111952 ◽

2021 ◽

Vol 142 ◽

pp. 111952

Author(s):

Kamil Mika ◽

Małgorzata Szafarz ◽

Marek Bednarski ◽

Kamil Kuder ◽

Katarzyna Szczepańska ◽

...

Keyword(s):

Intrinsic Activity ◽

Receptor Ligands ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Pharmacokinetic Properties ◽

Histamine H3

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ChemInform Abstract: Substituted N-Phenylcarbamates as Histamine H3 Receptor Antagonists with Improved in vivo Potency.

ChemInform ◽

10.1002/chin.200024119 ◽

2010 ◽

Vol 31 (24) ◽

pp. no-no

Author(s):

S. Reidemeister ◽

H. Stark ◽

X. Ligneau ◽

C. R. Ganellin ◽

J.-C. Schwartz ◽

...

Keyword(s):

Receptor Antagonists ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Histamine H3

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Corrigendum to “Waking selective neurons in the posterior hypothalamus and their response to histamine H3-receptor ligands: an electrophsiological study in freely moving cats” [Behav. Brain Res. 144 (2003) 227–241]

Behavioural Brain Research ◽

10.1016/j.bbr.2004.02.004 ◽

2004 ◽

Vol 152 (1) ◽

pp. 163

Author(s):

G. Vanni-Mercier ◽

S. Gigout ◽

G. Debilly ◽

J.S. Lin

Keyword(s):

Posterior Hypothalamus ◽

Receptor Ligands ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Freely Moving ◽

Freely Moving Cats ◽

Histamine H3

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In-vivo histamine H3 receptor antagonism activates cellular signaling suggestive of symptomatic and disease modifying efficacy in Alzheimer’s disease

Neuropharmacology ◽

10.1016/j.neuropharm.2010.10.026 ◽

2011 ◽

Vol 60 (2-3) ◽

pp. 460-466 ◽

Cited By ~ 42

Author(s):

R. Scott Bitner ◽

Stella Markosyan ◽

Arthur L. Nikkel ◽

Jorge D. Brioni

Keyword(s):

Alzheimer’S Disease ◽

Alzheimer's Disease ◽

Cellular Signaling ◽

Receptor Antagonism ◽

Histamine H3 Receptor ◽

H3 Receptor ◽

Disease Modifying ◽

Histamine H3

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Corrigendum to “Search for new multi-target compounds against Alzheimer’s disease among histamine H3 receptor ligands” [Eur. J. Med. Chem. 185 (2020) 111785]

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2020.112611 ◽

2020 ◽

Vol 205 ◽

pp. 112611

Author(s):

Marek Bajda ◽

Dorota Łażewska ◽

Justyna Godyń ◽

Paula Zaręba ◽

Kamil Kuder ◽

...

Keyword(s):

Alzheimer’S Disease ◽

Alzheimer's Disease ◽

Receptor Ligands ◽

Histamine H3 Receptor ◽

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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