Investigation of the effects of tianeptine and fluoxetine on pentylenetetrazole-induced seizures in rats

Ceyhan, Mustafa Nuri; Kayır, Hakan; Uzbay, I.T.

doi:10.1016/j.jpsychires.2004.06.002

Cited by 33 publications

(23 citation statements)

References 38 publications

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“…Our findings on the delaying effects of tianeptine on PTZinduced seizures support the results of Ceyhan et al (2005) who observed that tianeptine inhibited PTZ-induced seizures in rats. In the present study, we have confirmed those results with tianeptine in mice and extended those results by using adenosine receptor antagonists.…”

Section: Discussionsupporting

confidence: 92%

“…Previous studies performed in rodents indicated that tianeptine was effective at lower doses as compared with those using in the present study. For example, it had an anticonvulsant activity in rats at dose of 10 mg/kg (Ceyhan et al, 2005). In contrast to rats, we did not observe any significant effect on PTZ-induced seizures by tianeptine treatment in mice up to dose of 40 mg/kg.…”

Section: Discussioncontrasting

confidence: 78%

“…In addition, in a recent study from our laboratory (Ceyhan et al, 2005) indicated that tianeptine but not fluoxetine, an SSRI, have a beneficial inhibitory effect on PTZ-induced seizures in rats. In another study from our laboratory indicated that tianeptine has an inhibitory effect on audiogenic seizure in ethanol-withdrawn rats (Uzbay et al, 2006).…”

Section: Introductionmentioning

confidence: 94%

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Effects of Tianeptine on Onset Time of Pentylenetetrazole-Induced Seizures in Mice: Possible Role of Adenosine A1 Receptors

Uzbay

Kayır

Ceyhan

2006

Neuropsychopharmacol

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Depression is a common psychiatric problem in epileptic patients. Thus, it is important that an antidepressant agent has anticonvulsant activity. This study was organized to investigate the effects of tianeptine, an atypical antidepressant, on pentylenetetrazole (PTZ)-induced seizure in mice. A possible contribution of adenosine receptors was also evaluated. Adult male Swiss-Webster mice (25-35 g) were subjects. PTZ (80 mg/kg, i.p.) was injected to mice 30 min after tianeptine (2.5-80 mg/kg, i.p.) or saline administration. The onset times of 'first myoclonic jerk' (FMJ) and 'generalized clonic seizures' (GCS) were recorded. Duration of 600 s was taken as a cutoff time in calculation of the onset time of the seizures. To evaluate the contribution of adenosine receptors in the effect of tianeptine, a nonspecific adenosine receptor antagonist caffeine, a specific A 1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), a specific A2 A receptor antagonist 8-(3-chlorostyryl) caffeine (CSC) or their vehicles were administered to the mice 15 min before tianeptine (80 mg/kg) or saline treatments. Tianeptine (40 and 80 mg/kg) pretreatment significantly delayed the onset time of FMJ and GCS. Caffeine (10-60 mg/kg, i.p.) dose-dependently blocked the retarding effect of tianeptine (80 mg/kg) on the onset times of FMJ and GCS. DPCPX (20 mg/kg) but not CSC (1-8 mg/kg) blocked the effect of tianeptine (80 mg/kg) on FMJ. Our results suggest that tianeptine delayed the onset time of PTZ-induced seizures via adenosine A 1 receptors in mice. Thus, this drug may be a useful choice for epileptic patients with depression.

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Section: Discussionsupporting

confidence: 92%

Section: Discussioncontrasting

confidence: 78%

Section: Introductionmentioning

confidence: 94%

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Effects of Tianeptine on Onset Time of Pentylenetetrazole-Induced Seizures in Mice: Possible Role of Adenosine A1 Receptors

Uzbay

Kayır

Ceyhan

2006

Neuropsychopharmacol

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“…Firstly, antidepressants mentioned are not effective in all experimental models of epilepsy. Fluoxetine (Ceyhan et al 2005) and mirtazapine (Yilmaz et al 2007) did not affect PTZ-induced convulsions. Moreover, mirtazapine was found ineffective in the maximal electroshock test in mice (Yilmaz et al 2007).…”

Section: Discussionmentioning

confidence: 82%

“…Moreover, mirtazapine was found ineffective in the maximal electroshock test in mice (Yilmaz et al 2007). Secondly, tianeptine, the drug decreasing serotonin concentration in the synaptic cleft, inhibited clonic PTZ convulsions (Ceyhan et al 2005), which indicates that some other mechanisms may contribute to the anticonvulsant action of antidepressant drugs. Uzbay (2008) suggests that adenosinergic, glutamatergic, and nitrergic systems may be crucial in this respect.…”

Section: Discussionmentioning

confidence: 95%

Effect of acute and chronic treatment with milnacipran potentiates the anticonvulsant activity of conventional antiepileptic drugs in the maximal electroshock-induced seizures in mice

et al. 2009

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Pharmacokinetic study of tianeptine and its active metabolite MC5 in rats following different routes of administration using a novel liquid chromatography tandem mass spectrometry analytical method

Szafarz

Wencel

Pociecha

et al. 2017

Naunyn-Schmiedeberg's Arch Pharmacol

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Tianeptine is an atypical antidepressant with a unique mechanism of action and recently it has been also reported that its major metabolite, compound MC5, possesses pharmacological activity similar to that of the parent drug. The current study aims to investigate the pharmacokinetics (PK) of both tianeptine and MC5 after intravenous or intraperitoneal administration of the parent drug as well as the metabolic ratio of MC5 in rats. To achieve these goals an LC-MS/MS method using the small sample volume for the quantitation of tianeptine and its active metabolite MC5 in rat plasma and liver perfusate has been developed and validated. Following an intravenous administration of tianeptine pharmacokinetic parameters were calculated by non-compartmental analysis. The average tianeptine volume of distribution at steady state was 2.03 L/kg and the systemic clearance equaled 1.84 L/h/kg. The mean elimination half-lives of tianeptine and MC5 metabolite were 1.16 and 7.53 h, respectively. The hepatic clearance of tianeptine determined in the isolated rat liver perfusion studies was similar to the perfusate flow rate despite the low metabolic ratio of MC5. Mass spectrometric analysis of rat bile indicated that tianeptine and MC5 metabolite are eliminated with bile as glucuronide and glutamine conjugates. Bioavailability of tianeptine after its intraperitoneal administration was 69%. The PK model with a metabolite compartment developed in this study for both tianeptine and MC5 metabolite after two routes of administration may facilitate tianeptine dosage selection for the prospective pharmacological experiments.

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Investigation of the effects of tianeptine and fluoxetine on pentylenetetrazole-induced seizures in rats

Cited by 33 publications

References 38 publications

Effects of Tianeptine on Onset Time of Pentylenetetrazole-Induced Seizures in Mice: Possible Role of Adenosine A1 Receptors

Effects of Tianeptine on Onset Time of Pentylenetetrazole-Induced Seizures in Mice: Possible Role of Adenosine A1 Receptors

Effect of acute and chronic treatment with milnacipran potentiates the anticonvulsant activity of conventional antiepileptic drugs in the maximal electroshock-induced seizures in mice

Pharmacokinetic study of tianeptine and its active metabolite MC5 in rats following different routes of administration using a novel liquid chromatography tandem mass spectrometry analytical method

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