scholarly journals Determination of in vitro metabolism of new non-imidazole histamine H3 receptor antagonist 1-[3-(4-tert-butylphenoxy)propyl]piperidine

2019 ◽  
Vol 76 (5) ◽  
pp. 877-884
Author(s):  
Agata Kryczyk-Poprawa ◽  
Małgorzata Szafarz ◽  
Aneta Palak Palak ◽  
Dorota Łażewska ◽  
Kamil Kuś ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
In Vitro Metabolism ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3

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

ChemInform ◽  
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

scholarly journals Determination of Histamine H3-Receptor Antagonist Conessine in Wistar Rat Plasma by a Rapid and Sensitive RP-UFLC Method: Application to a Pharmacokinetic Study

2020 ◽  
Vol 12 (1) ◽  
pp. 55-62
Author(s):  
Nilesh Sudhakar Ambhore ◽  
Rama Satyanarayana Raju Kalidhindi ◽  
Shubhashri Mohire ◽  
Karthik Yamjala ◽  
Shashank Mulukutla ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Pharmacokinetic Study ◽  
Wistar Rat ◽  
Rat Plasma ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3

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

1996 ◽  
Vol 6 (16) ◽  
pp. 2013-2018 ◽  
Author(s):  
A Hüls ◽  
K Purand ◽  
H Stark ◽  
X Ligneau ◽  
J.-M Arrang ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3

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

NeuroImage ◽  
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

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):

P1-235: Effects of the novel histamine H3 receptor antagonist S 38093 in a non-human primate model of cognitive dysfunction

2009 ◽  
Vol 5 (4S_Part_8) ◽  
pp. P245-P245
Author(s):  
Jay S. Schneider ◽  
Emmanuel Decamp ◽  
Michael Hill ◽  
Erwan Bezard ◽  
Alan Crossman ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Cognitive Dysfunction ◽  
The Novel ◽  
Primate Model ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Human Primate ◽  
Histamine H3

scholarly journals Influence of a selective histamine H3 receptor antagonist on hypothalamic neural activity, food intake and body weight

2005 ◽  
Vol 29 (12) ◽  
pp. 1402-1412 ◽  
Author(s):  
K Malmlöf ◽  
F Zaragoza ◽  
V Golozoubova ◽  
H H F Refsgaard ◽  
T Cremers ◽  
...  
Keyword(s):  
Body Weight ◽  
Food Intake ◽  
Receptor Antagonist ◽  
Neural Activity ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3
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