Discovery of a potent, selective, and orally bioavailable histamine H3 receptor antagonist SAR110068 for the treatment of sleep

Discovery of a potent, selective, and orally bioavailable histamine H3 receptor antagonist SAR110068 for the treatment of sleep–wake disorders

Published:2013-11 Issue:22 Volume:23 Page:6141-6145
ISSN:0960-894X
Container-title:Bioorganic & Medicinal Chemistry Letters
language:en
Short-container-title:Bioorganic & Medicinal Chemistry Letters

Author:

Gao Zhongli,Hurst William J.,Czechtizky Werngard,Francon Dominique,Griebel Guy,Nagorny Raisa,Pichat Philippe,Schwink Lothar,Stengelin Siegfried,Hendrix James A.,George Pascal G.

Publisher

Elsevier BV

Subject

Organic Chemistry,Clinical Biochemistry,Drug Discovery,Pharmaceutical Science,Molecular Biology,Molecular Medicine,Biochemistry

Reference22 articles.

1. Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor

2. Computational analysis of novel drugs designed for use as acetylcholinesterase inhibitors and histamine H3 receptor antagonists for Alzheimer's disease by docking, scoring and de novo evolution

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

4. BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, Hydrochloride], a Nonimidazole Inverse Agonist/Antagonist at the Human Histamine H3 Receptor: Preclinical Pharmacology

5. The brain H3-receptor as a novel therapeutic target for vigilance and sleep–wake disorders

Cited by 7 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Targeting Microglia in Neuroinflammation: H3 Receptor Antagonists as a Novel Therapeutic Approach for Alzheimer’s Disease, Parkinson’s Disease, and Autism Spectrum Disorder;Pharmaceuticals;2024-06-25

2. Revisiting Preclinical Observations of Several Histamine H3 Receptor Antagonists/Inverse Agonists in Cognitive Impairment, Anxiety, Depression, and Sleep–Wake Cycle Disorder;Frontiers in Pharmacology;2022-06-01

3. Stimulation of dorsal hippocampal histaminergic transmission mitigates the expression of ethanol withdrawal-induced despair in mice;Alcohol;2021-11

4. The Histamine H3 Receptor: Structure, Pharmacology, and Function;Molecular Pharmacology;2016-08-25

5. Histamine H3R Antagonists: From Scaffold Hopping to Clinical Candidates;Histamine Receptors;2016