Abstract：
:S 38093, a novel histamine H3 receptor inverse agonist, was tested in a series of neurochemical and behavioral paradigms designed to evaluate its procognitive and arousal properties. In intracerebral microdialysis studies performed in rats, S 38093 dose-dependently increased histamine extracellular levels in the prefrontal cortex and facilitated cholinergic transmission in the prefrontal cortex and hippocampus of rats after acute and chronic administration (10mg/kg i.p.). Acute oral administration of S 38093 at 0.1mg/kg significantly improved spatial working memory in rats in the Morris water maze test. The compound also displayed cognition enhancing properties in the two-trial object recognition task in rats, in a natural forgetting paradigm at 0.3 and 1mg/kg p.o. and in a scopolamine-induced memory deficit situation at 3mg/kg p.o. The property of S 38093 to promote episodic memory was confirmed in a social recognition test in rats at 0.3 and 1mg/kg i.p. Arousal properties of S 38093 were assessed in freely moving rats by using electroencephalographic recordings: at 3 and 10mg/kg i.p., S 38093 significantly reduced slow wave sleep delta power and induced at the highest dose a delay in sleep latency. S 38093 at 10mg/kg p.o. also decreased the barbital-induced sleeping time in rats. Taken together these data indicate that S 38093, a novel H3 inverse agonist, displays cognition enhancing at low doses and arousal properties at higher doses in rodents.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Panayi F,Sors A,Bert L,Martin B,Rollin-Jego G,Billiras R,Carrié I,Albinet K,Danober L,Rogez N,Thomas JY,Pira L,Bertaina-Anglade V,Lestage Pdoi
10.1016/j.ejphar.2017.03.008subject
Has Abstractpub_date
2017-05-15 00:00:00pages
1-10eissn
0014-2999issn
1879-0712pii
S0014-2999(17)30159-0journal_volume
803pub_type
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