Awakening properties of newly discovered highly selective H₃ receptor antagonists in rats

Behavioural Brain Research
Guy GriebelSandra Beeské

Abstract

The objective of the present study was to compare the awakening effects of two newly discovered H₃ receptor antagonists (i.e. SAR110894 and SAR110068) with those of reference H₃ receptor ligands (i.e. ciproxifan, ABT-0239 and GSK189254) and classical psychostimulants (i.e. amphetamine and modafinil) by using EEG recording in rats during their light phase. Results showed that SAR110068 (10 and 30 mg/kg, p.o.) increased wakefulness and decreased slow wave sleep to a similar degree than ciproxifan (10 mg/kg, i.p.), ABT-0239 (10 mg/kg, p.o.) and GSK189254 (10 mg/kg, p.o.), while SAR110894 (3-30 mg/kg, p.o.) did not modify significantly any of the sleep/wakefulness parameters. Time-course analysis revealed that the awakening effects of GSK189254 lasted for about 1h, while ciproxifan, ABT-0239 and SAR110068 produced such effects for 3-4 h. The magnitude of the awakening effects of the psychostimulants, amphetamine (3 mg/kg, i.p.) and modafinil (300 mg/kg, i.p.), was dramatically higher than with the H₃ compounds, and they lasted for 5 and 6 h, respectively. However, unlike the H₃ receptor antagonists, both psychostimulants produced a strong increase in theta (θ) rhythm, which is indicative of CNS side effects, such as hyperactivity o...Continue Reading

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Citations

Oct 18, 2013·Expert Opinion on Therapeutic Patents·Dorota Łażewska, Katarzyna Kieć-Kononowicz
Jun 14, 2013·Biomedical Chromatography : BMC·Ramakrishna NirogiHimabindu Vurimindi
Aug 19, 2015·Neuropharmacology·Maximiliano Rapanelli, Christopher Pittenger
May 28, 2013·Current Opinion in Neurobiology·Jason Rihel, Alexander F Schier
Oct 23, 2018·Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova·O V YakovlevaM G Poluektov
Jan 18, 2018·Expert Opinion on Therapeutic Patents·Dorota Łażewska, Katarzyna Kieć-Kononowicz
Oct 11, 2016·Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova·O V BabkinaO S Levin
Oct 4, 2017·Pharmacology Research & Perspectives·Daniel S WhittakerChristopher S Colwell

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