13 research outputs found
Anxiolytic-like effect of etazolate, a type 4 phosphodiesterase inhibitor in experimental models of anxiety
444-449Etazolate is a selective inhibitor of type 4 phosphodiesterase (PDE4) class enzyme. Antidepressant-like
effect of etazolate has been previously demonstrated in the rodent models of
depression. The present study was designed to investigate the anxiolytic-like
activity of etazolate in experimental mouse models of anxiety. The putative
anxiolytic effect of etazolate (0.25-1 mg/kg, ip) was studied in mice by using
a battery of behavioural tests of anxiety such as elevated plus maze (EPM),
light/dark (L/D) aversion, hole board (HB) and open field (OFT) with diazepam
(2 mg/kg, ip) as reference anxiolytic. Like diazepam (2 mg/kg, ip), etazolate
(0.5 and 1 mg/kg, ip) significantly increased the percentage of both time spent
and entries into open arms in the EPM test. In the L/D test etazolate (0.5 and
1 mg/kg, ip) increased the both total time spent in and latency time to leave
the light compartment. Etazolate (0.5 and 1 mg/kg, ip) also significantly
increased head dipping scores and time spent in head dipping, whereas
significantly decreased the head dipping latency in HB test.
In addition, etazolate (0.5 and 1 mg/kg, ip) significantly increased the
ambulation scores (square crossed) and number of rearing in OFT. In conclusion,
these findings indicated that etazolate exhibited an anxiolytic-like effect in
experimental models of anxiety and may be considered an alternative approach
for the management of anxiety disorder
Anti-depressant like activity of <i>N</i>-n-butyl-3-methoxyquinoxaline-2-carboxamide (<b>6o</b>) a 5-HT<sub>3 </sub>receptor antagonist
435-443<span style="font-size:11.0pt;font-family:
" times="" new="" roman";mso-fareast-font-family:"times="" roman";mso-bidi-font-family:="" mangal;mso-ansi-language:en-gb;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-GB">The compound 6o (at 0.5, 1 and 2
mg/kg, ip) with optimum log P and pA2
value, was subjected to forced swim test (FST) and tail suspension test (TST).
The compound 6o significantly
reduced the duration of immobility in mice without affecting the base line
locomotion in actophotometer. Moreover, 6o
(2 mg/kg, ip), potentiated the 5-hydroxytryptophan
(5-HTP)-induced head twitch responses in mice and at 1 and 2 mg/kg, ip
antagonized the reserpine-induced hypothermia (RIH) in rats. In interaction
studies with various standard drugs/ligands using FST, <b style="mso-bidi-font-weight:
normal">6o (1 and 2 mg/kg, ip) potentiated the anti-depressant effect
fluoxetine (5 mg/kg, ip) and reversed the depressant effect of parthenolide (1
mg/kg, ip) by reducing the duration of immobility. Furthermore, 6o (1 and 2 mg/kg, ip) potentiated the
effect of bupropion (10 mg/kg, ip) in TST. The behavioural anomalies of the
olfactory bulbectomised (OBX) rats were augmented by chronic 6o (1 and 2 mg/kg) treatment as
observed from the modified open field test (parameters: ambulation, rearing,
fecal pellet). The results suggest that compound <b style="mso-bidi-font-weight:
normal">6o exhibited anti-depressant like effect in rodent models of
depression.</span
Anxiolytic-like effect of <i style="mso-bidi-font-style:normal">N</i>-n-butyl-3-methoxyquinoxaline-2-carboxamide (<b>6o</b>) in experimental mouse models of anxiety
510-514The present research was designed to
explore the anxiolytic-like activity of a novel 5-HT3 receptor antagonist (6o)
in
experimental mouse models of anxiety. The anxiolytic activity of '6o' at
(1 and 2 mg/kg, ip) was evaluated in mice by using a battery of behavioural
tests of anxiety such as elevated plus maze (EPM), light/dark aversion test,
hole board (HB) and open field test (OFT) with diazepam (2 mg/kg, ip) as a
standard anxiolytic. None of the tested doses of '6o' affected the base
line locomotion. Compound '6o' (2 mg/kg, ip) and diazepam (2mg/kg, ip)
significantly increased the percentage of both time spent and open arm entries
in the EPM test. Compound '6o' in (1 mg/kg, ip) dose was only able to
affect the percentage time spent in open arm significantly in the EPM test. In
the light and dark test, compound '6o' (2 mg/kg, ip) and diazepam
(2mg/kg, ip) significantly increased the total time spent in light compartment
as well as number of transitions from one compartment to other and number of
square crossed. Compound '6o' (1 and 2 mg/kg, ip) and diazepam (2 mg/kg,
ip) also significantly increased number of head dips and number of squares
crossed, whereas significantly decreased the head
dipping latency in HB test as compared to vehicle control group. In addition, '6o'
in both the doses and diazepam
(2mg/kg, ip) significantly increased the ambulation scores (squares crossed) in
OFT however, there was no significant effect of '6o' (1 and 2 mg/kg, ip)
and diazepam (2 mg/kg, ip) on rearing scores. To conclude compound '6o'
exhibited an
anxiolytic-like effect in animal models of anxiety
<span style="font-size:11.0pt;mso-bidi-font-size:10.0pt; font-family:"Times New Roman";mso-fareast-font-family:"Times New Roman"; mso-ansi-language:EN-IN;mso-fareast-language:EN-IN;mso-bidi-language:AR-SA">Antidepressant and anxiolytic-like effects of<span style="font-size:11.0pt; mso-bidi-font-size:10.0pt;font-family:"Times New Roman";mso-fareast-font-family: "Times New Roman";mso-ansi-language:EN-GB;mso-fareast-language:EN-US; mso-bidi-language:AR-SA" lang="EN-GB"> 4n, a novel 5-HT<sub>3</sub> receptor antagonist using behaviour based rodent models</span></span>
625-632The present study was designed to investigate the putative antidepressant and
anxiolytic-like effects of <span style="mso-bidi-font-weight:
bold">N-n-Butylquinoxalin-2-carboxamide
(4n), a novel 5-HT3
receptor antagonist, with an optimal log P (2.01) and p<i style="mso-bidi-font-style:
normal">A2 value (7.3) greater than ondansetron (6.9) using
rodent behavioural models of depression and anxiety.
Acute treatment of 4n
(1-4 mg/kg, ip) in mice produced antidepressant-like effect in forced swim test
(FST) without affecting the baseline locomotion in actophotometer test in mice.
4n (2-4 mg/kg, ip) treatment also
potentiated the 5-hydroxytryptophan (5-HTP) induced head twitch response in
mice. Further, 4n (1-4 mg/kg, ip)
treatment antagonized reserpine induced hypothermia in rats. Chronic treatment
(14 days) with 4n (1-4 mg/kg) and
paroxetine (10 mg/kg) significantly attenuated the behavioural anomalies
induced by bilateral olfactory bulbectomy in rats in modified open field paradigm. <span style="mso-ansi-language:EN-IN;mso-fareast-language:
EN-IN">An anxiogenic-like behaviour was induced by light alone as the stimulus
using light-dark aversion test. 4n
(2-4 mg/kg, ip) treatment significantly increased no. of transitions between
dark and lit area and the time spent in the lit area. In
conclusion, these preliminary investigations confirm that <b style="mso-bidi-font-weight:
normal">4n exhibited antidepressant and <span style="mso-ansi-language:
EN-IN;mso-fareast-language:EN-IN">anxiolytic-like effects in rodent models of depression and anxiety.
</span
Anti-depressant-like activity of a novel serotonin type-3 (5-HT<sub>3</sub>) receptor antagonist in rodent models of depression
619-626N-Cyclohexyl-3-methoxyquinoxalin-2-carboxamide (QCM-13), a novel 5-HT3
antagonist identified from a series of compounds with higher pA2
(7.6) and good log P (2.91) value was screened in rodent models of depression
such as forced swim test (FST), tail suspension test (TST), interaction studies
with standard anti-depressants and confirmatory studies such as reversal of
parthenolide induced depression and reserpine induced hypothermia. In FST (2
and 4 mg/kg) and TST (2 and 4 mg/kg), QCM-13 significantly reduced the duration
of immobility in mice without affecting the base line locomotion. QCM-13 (2 and
4 mg/kg) was also found to have significant interaction with standard
anti-depressants (fluoxetine and bupropion in FST and TST respectively).
Further, reversal of parthenolide induced depression in mice and reserpine
induced hypothermia in rat models indicate the serotonergic influence of QCM-13
for anti-depressant potential