Brain histamine H3 receptors in rats with portacaval anastomosis: in vitro and in vivo studies

1998 ◽  
Vol 358 (5) ◽  
pp. 574-581 ◽  
Author(s):  
V. Lozeva ◽  
Martti Attila ◽  
Eeva Anttila ◽  
Kirsti Laitinen ◽  
Mikko Hippeläinen ◽  
...  
Keyword(s):  
In Vivo Studies ◽  
Portacaval Anastomosis ◽  
Brain Histamine ◽  
Histamine H3 Receptors ◽  
H3 Receptors ◽  
Histamine H3

scholarly journals Protean agonism at histamine H3 receptors in vitro and in vivo

2003 ◽  
Vol 100 (19) ◽  
pp. 11086-11091 ◽  
Author(s):  
F. Gbahou ◽  
A. Rouleau ◽  
S. Morisset ◽  
R. Parmentier ◽  
S. Crochet ◽  
...  
Keyword(s):  
Histamine H3 Receptors ◽  
H3 Receptors ◽  
Histamine H3

The histamine analogue impentamine discriminates between peripheral and brain histamine H3 receptors

1995 ◽  
Vol 31 ◽  
pp. 272-272
Author(s):  
R LEURS ◽  
M KATHMANN ◽  
R VOLLINGA ◽  
W MENGE ◽  
E SCHLICKER ◽  
...  
Keyword(s):  
Brain Histamine ◽  
Histamine H3 Receptors ◽  
H3 Receptors ◽  
Histamine H3

In vitro pharmacology at human histamine H3 receptors and brain access of non-imidazole alkylpiperidine derivatives

2007 ◽  
Vol 55 (2) ◽  
pp. 111-116 ◽  
Author(s):  
S BERTONI ◽  
L FLAMMINI ◽  
V MANENTI ◽  
V BALLABENI ◽  
G MORINI ◽  
...  
Keyword(s):  
Histamine H3 Receptors ◽  
H3 Receptors ◽  
In Vitro Pharmacology ◽  
Human Histamine ◽  
Histamine H3

scholarly journals Biphenylalkoxyamine Derivatives–Histamine H3 Receptor Ligands with Butyrylcholinesterase Inhibitory Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3580
Author(s):  
Dorota Łażewska ◽  
Paula Zaręba ◽  
Justyna Godyń ◽  
Agata Doroz-Płonka ◽  
Annika Frank ◽  
...  
Keyword(s):  
Neurodegenerative Diseases ◽  
Inhibitory Activity ◽  
Symptomatic Treatment ◽  
In Vivo Studies ◽  
Avoidance Task ◽  
Receptor Ligands ◽  
Mao B ◽  
Histamine H3

Neurodegenerative diseases, e.g., Alzheimer’s disease (AD), are a key health problem in the aging population. The lack of effective therapy and diagnostics does not help to improve this situation. It is thought that ligands influencing multiple but interconnected targets can contribute to a desired pharmacological effect in these complex illnesses. Histamine H3 receptors (H3Rs) play an important role in the brain, influencing the release of important neurotransmitters, such as acetylcholine. Compounds blocking their activity can increase the level of these neurotransmitters. Cholinesterases (acetyl- and butyrylcholinesterase) are responsible for the hydrolysis of acetylcholine and inactivation of the neurotransmitter. Increased activity of these enzymes, especially butyrylcholinesterase (BuChE), is observed in neurodegenerative diseases. Currently, cholinesterase inhibitors: donepezil, rivastigmine and galantamine are used in the symptomatic treatment of AD. Thus, compounds simultaneously blocking H3R and inhibiting cholinesterases could be a promising treatment for AD. Herein, we describe the BuChE inhibitory activity of H3R ligands. Most of these compounds show high affinity for human H3R (Ki < 150 nM) and submicromolar inhibition of BuChE (IC50 < 1 µM). Among all the tested compounds, 19 (E153, 1-(5-([1,1′-biphenyl]-4-yloxy)pentyl)azepane) exhibited the most promising in vitro affinity for human H3R, with a Ki value of 33.9 nM, and for equine serum BuChE, with an IC50 of 590 nM. Moreover, 19 (E153) showed inhibitory activity towards human MAO B with an IC50 of 243 nM. Furthermore, in vivo studies using the Passive Avoidance Task showed that compound 19 (E153) effectively alleviated memory deficits caused by scopolamine. Taken together, these findings suggest that compound 19 can be a lead structure for developing new anti-AD agents.

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