Penbutolol: Pharmacokinetics, effect on exercise tachycardia, and in vitro inhibition of radioligand binding

1988 ◽  
Vol 35 (6) ◽  
pp. 613-623 ◽  
Author(s):  
D. Brockmeier ◽  
P. Hajd� ◽  
W. Henke ◽  
E. Mutschler ◽  
D. Palm ◽  
...  
Keyword(s):  
Radioligand Binding ◽  
Exercise Tachycardia ◽  
In Vitro Inhibition

Effekte von Substanz P und Neurotensin auf die Kontraktilität des Ileums der Maus in vitro: Inhibition durch STW 5

2007 ◽  
Vol 45 (08) ◽  
Author(s):  
D Hagelauer ◽  
O Kelber ◽  
D Weiser ◽  
S Laufer ◽  
H Heinle
Keyword(s):  
Substanz P ◽  
In Vitro Inhibition

In vitro Inhibition of Pancreatic Enzyme Activities by Dietary Fiber

Digestion ◽  
1982 ◽  
Vol 24 (1) ◽  
pp. 54-59 ◽  
Author(s):  
G. Isaksson ◽  
I. Lundquist ◽  
I. Ihse
Keyword(s):  
Dietary Fiber ◽  
Enzyme Activities ◽  
Pancreatic Enzyme ◽  
In Vitro Inhibition

scholarly journals In Vitro Inhibition of Alphaviruses by Lycorine

2021 ◽  
Author(s):  
Na Li ◽  
Zhen Wang ◽  
Rui Wang ◽  
Zhe-Rui Zhang ◽  
Ya-Nan Zhang ◽  
...  
Keyword(s):  
In Vitro Inhibition

scholarly journals IN VITRO INHIBITION OF HELICOBACTER PYLORI UREASE WITH NON AND SEMI FERMENTED CAMELLIA SINENSIS

2009 ◽  
Vol 27 (1) ◽  
pp. 30-34
Author(s):  
AR Shoae Hassani ◽  
N Ordouzadeh ◽  
A Ghaemi ◽  
N Amirmozafari ◽  
K Hamdi ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Camellia Sinensis ◽  
In Vitro Inhibition

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):

In vitro inhibition of prostaglandin H synthase by compounds from the exocrine secretions of lace bugs

1989 ◽  
Vol 93 (2) ◽  
pp. 253-255 ◽  
Author(s):  
Russell A. Jurenka ◽  
John W. Neal ◽  
Ralph W. Howard ◽  
James E. Oliver ◽  
Gary J. Blomquist
Keyword(s):  
Prostaglandin H Synthase ◽  
Exocrine Secretions ◽  
Lace Bugs ◽  
In Vitro Inhibition ◽  
Prostaglandin H
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