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.
| Original language | English |
|---|---|
| Pages (from-to) | 1188-1192 |
| Number of pages | 5 |
| Journal | Pharmacological Reports |
| Volume | 67 |
| Issue number | 6 |
| DOIs | |
| Publication status | Published - dec. 1 2015 |
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ASJC Scopus subject areas
- Pharmacology
Cite this
Effect of a kynurenic acid analog on home-cage activity and body temperature in rats. / Kassai, Ferenc; Kedves, Rita; Gyertyán, István; Tuka, Bernadett; Fülöp, F.; Toldi, J.; Lendvai, Balázs; Vécsei, L.
In: Pharmacological Reports, Vol. 67, No. 6, 01.12.2015, p. 1188-1192.Research output: Article
}
TY - JOUR
T1 - Effect of a kynurenic acid analog on home-cage activity and body temperature in rats
AU - Kassai, Ferenc
AU - Kedves, Rita
AU - Gyertyán, István
AU - Tuka, Bernadett
AU - Fülöp, F.
AU - Toldi, J.
AU - Lendvai, Balázs
AU - Vécsei, L.
PY - 2015/12/1
Y1 - 2015/12/1
N2 - 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.
AB - 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.
KW - Home-cage activity
KW - Hypothermia
KW - Kynurenic acid
KW - Kynurenic acid analog
KW - Telemetry
UR - http://www.scopus.com/inward/record.url?scp=84941657155&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84941657155&partnerID=8YFLogxK
U2 - 10.1016/j.pharep.2015.04.015
DO - 10.1016/j.pharep.2015.04.015
M3 - Article
C2 - 26481540
AN - SCOPUS:84941657155
VL - 67
SP - 1188
EP - 1192
JO - Pharmacological Reports
JF - Pharmacological Reports
SN - 1734-1140
IS - 6
ER -