Effect of a kynurenic acid analog on home-cage activity and body temperature in rats.

Abstract

BACKGROUND:

N-(2-N,N-Dimethylaminoethyl)-4-oxo-1H-quinoline-2-carboxamide hydrochloride (SzR-72) is a kynurenic acid (KYNA) amide analog that displays neuroprotective action. Whereas its brain penetration ability and its solubility limit the therapeutic use of KYNA: the corresponding properties of the analog exceed those of the parent compound. Although SzR-72 has been extensively studied, its exact mechanism of action has not yet been fully clarified. As KYNA induces hypothermia in laboratory rodents, it may be hypothesized that SzR-72 may have a similar effect. This would be of major importance, since the hypothermia generated by external cooling is neuroprotective, thus a putative hypothermic effect of SzR-72 could contribute to its neuroprotective action.

METHODS:

The effects of SzR-72 on the body temperature and home-cage activity of rats were studied by using a telemetry system. In order to follow the longitudinal changes in the effects of the compound, subchronic drug administration was applied.

RESULTS:

The initial administration of the compound induced substantial hypothermia and reduced the home-cage activity. During the 5 days of SzR-72 administration, partial tolerance developed to the hypothermic effect, while the inhibition of home-cage activity detected after the acute administration was completely tolerated.

CONCLUSIONS:

On the basis of these results, it cannot be excluded that the hypothermic effect of SzR-72 contributes to its neuroprotective action.

• Authors: Ferenc Kassai, Rita Kedves, István Gyertyán, Bernadett Tuka, Ferenc Fülöp, József Toldi, Balázs Lendvai, László Vécsei
• Journal: Pharmacological reports : PR (Pharmacol Rep) Vol. 67 Issue 6 Pg. 1188-92 (Dec 2015) ISSN: 2299-5684 [Electronic] Switzerland
• PMID: 26481540 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2015 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.

Chemical References

• Neuroprotective Agents
• SZR 72
• Kynurenic Acid

Topics

• Animals
• Body Temperature (drug effects)
• Drug Tolerance
• Kynurenic Acid (analogs & derivatives, pharmacology)
• Male
• Motor Activity (drug effects)
• Neuroprotective Agents (pharmacology)
• Rats