The medicinal chemistry and therapeutic potentials of ligands of the histamine H3 receptor

1995 ◽  
pp. 107-165 ◽  
Author(s):  
R. Leurs ◽  
R. C. Vollinga ◽  
H. Timmerman
Keyword(s):  
Medicinal Chemistry ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3

5 Recent Medicinal Chemistry of the Histamine H3 Receptor

2006 ◽  
pp. 181-206 ◽  
Author(s):  
Michael A. Letavic ◽  
Ann J. Barbier ◽  
Curt A. Dvorak ◽  
Nicholas I. Carruthers
Keyword(s):  
Medicinal Chemistry ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3

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

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

scholarly journals Purification of a histamine H3 receptor negatively coupled to phosphoinositide turnover in the human gastric cell line HGT1.

1992 ◽  
Vol 267 (35) ◽  
pp. 25315-25320
Author(s):  
Y Cherifi ◽  
C Pigeon ◽  
M Le Romancer ◽  
A Bado ◽  
F Reyl-Desmars ◽  
...  
Keyword(s):  
Cell Line ◽  
Histamine H3 Receptor ◽  
Gastric Cell ◽  
Phosphoinositide Turnover ◽  
H3 Receptor ◽  
Histamine H3

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

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

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

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

005 Samelisant (SUVN-G3031), a histamine H3 receptor inverse agonist in animal models of sleep disorders

SLEEP ◽  
2021 ◽  
Vol 44 (Supplement_2) ◽  
pp. A2-A2
Author(s):  
Saivishal Daripelli ◽  
Parusharamulu Molgara ◽  
Nageswararao Muddana ◽  
Pradeep Jayarajan ◽  
Venkat Reddy Mekala ◽  
...  
Keyword(s):  
Knockout Mice ◽  
Radioligand Binding ◽  
Research Work ◽  
Brain Regions ◽  
Inverse Agonist ◽  
Abuse Liability ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3

Abstract Introduction Narcolepsy is a chronic sleep disorder characterized by overwhelming daytime drowsiness, sudden attacks of sleep and sometimes accompanied by cataplexy. Although the orexin deficiency is considered to be the primary cause of this disorder, lot of attention has been diverted on targeting histaminergic neurotransmission by blockade of histamine H3 receptor (H3R). Samelisant (SUVN-G3031) is one of the potent and selective H3R inverse agonist currently being evaluated in a Phase 2 study as monotherapy for the treatment of narcolepsy with and without cataplexy (ClinicalTrials.gov Identifier: NCT04072380). In the current research work, Samelisant was evaluated for neurotransmitter changes in rats and sleep EEG in orexin knockout mice, a reliable proof-of-concept study for treatment of excessive daytime sleepiness and cataplexy in narcolepsy. Methods Binding affinity of Samelisant towards human and rat histamine H3R was evaluated in in-vitro radioligand binding assay and functionality in GTP□S assay. Effect of Samelisant was studied in (R)-α-methyl histamine induced dipsogenia. In rat brain microdialysis, Samelisant was evaluated for its effects on modulation of neurotransmitters like histamine, dopamine and norepinephrine. Male orexin knockout mice were implanted with telemetric device for simultaneous monitoring of electroencephalography (EEG) and electromyography. Effects of Samelisant (3 and 10 mg/kg, p.o.) were evaluated during active period of animals. Results Samelisant is an inverse agonist at histamine H3 receptors with hKi of 8.7 nM and showed minimal binding against over 70 target sites. Samelisant produced significant increase in histamine, dopamine and norepinephrine levels in cortex. Samelisant produced no change in the striatal and accumbal dopamine levels in rats, suggesting no propensity to induce abuse liability. Samelisant blocked R-α-methyl histamine induced water intake and produced dose dependent increase in tele-methylhistamine levels in various brain regions and in cerebrospinal fluid of male Wistar rats. Samelisant produced significant increase in wakefulness with concomitant decrease in non-rapid eye movement sleep in orexin knockout mice. Samelisant also significantly decreased number of cataplectic episodes in orexin knockout mice. Conclusion Samelisant is an inverse agonist at histamine H3 receptor and results from the preclinical studies presented here provide a strong evidence for the potential utility of Samelisant in the treatment of narcolepsy with and without cataplexy. Support (if any):

Chronic administration of the histamine H3 receptor agonist immepip decreases l-Dopa-induced dyskinesias in 6-hydroxydopamine-lesioned rats

2019 ◽  
Vol 236 (6) ◽  
pp. 1937-1948 ◽  
Author(s):  
Alberto Avila-Luna ◽  
Camilo Ríos ◽  
Arturo Gálvez-Rosas ◽  
Sergio Montes ◽  
José-Antonio Arias-Montaño ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Chronic Administration ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
6 Hydroxydopamine ◽  
Histamine H3

Anxiolytic-like profiles of histamine H3 receptor agonists in animal models of anxiety: a comparative study with antidepressants and benzodiazepine anxiolytic

2009 ◽  
Vol 205 (2) ◽  
pp. 177-187 ◽  
Author(s):  
Fumikazu Yokoyama ◽  
Miki Yamauchi ◽  
Masayo Oyama ◽  
Kunihiro Okuma ◽  
Kaname Onozawa ◽  
...  
Keyword(s):  
Animal Models ◽  
Comparative Study ◽  
Histamine H3 Receptor ◽  
Receptor Agonists ◽  
H3 Receptor ◽  
Animal Models Of Anxiety ◽  
Histamine H3
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