Effects of sildenafil treatment on the development of tolerance to diazepam-induced motor impairment and sedation in mice

Talarek, Sylwia; Orzelska, Jolanta; Listos, Joanna; Fidecka, Sylwia

doi:10.1016/s1734-1140(10)70320-0

Cited by 20 publications

(20 citation statements)

References 36 publications

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“…It is worth emphasizing that the doses of drugs modifying l -arginine:NO:cGMP pathway used in the present experiments were chosen on the base of our previous experiments and both acute and chronic administration of NO modulators did not affect the motor performance in mice (Talarek et al 2008; Talarek et al 2010). Therefore, the results of the present study seem not to be associated with motor-impairing effect of these compounds per se.…”

Section: Discussionmentioning

confidence: 99%

“…FNZ was injected subcutaneously (sc). The doses of drugs modifying l -arginine:NO:cGMP pathway were tested in our previous experiments (Talarek et al 2008; Talarek et al 2010), and those which did not affect the motor performance in mice were used in the present studies. All the substances were administered in a volume of 10 ml/kg body weight.…”

Section: Methodsmentioning

confidence: 99%

“…Moreover, there is behavioural data indicating that inhibition of NOS prolongs the sleeping time induced by BZ (Talarek and Fidecka 2004) and enhances the anticonvulsant (Talarek and Fidecka 2003), antinociceptive (Talarek and Fidecka 2002) and anxiolytic (Quock and Nguyen 1992) effects of BZ. In addition, there are findings suggesting some role of l -arginine:NO:cGMP pathway in the development of diazepam-induced tolerance to its motor-impairing effect in mice (Talarek et al 2008). …”

Section: Introductionmentioning

confidence: 99%

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The Importance of l-Arginine:NO:cGMP Pathway in Tolerance to Flunitrazepam in Mice

et al. 2016

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The goal of the study was to investigate the effects of drugs modifying l-arginine:NO:cGMP pathway on the development of tolerance to flunitrazepam (FNZ)-induced motor impairment in mice. FNZ-induced motor incoordination was assessed on the 1st and 8th days of experiment, using the rotarod and chimney tests. It was found that (a) both a non-selective nitric oxide synthase (NOS) inhibitor: N G-nitro-l-arginine methyl ester (l-NAME) and an unselective neuronal NOS inhibitor: 7-nitroindazole (7-NI) inhibited the development of tolerance to the motor-impairing effects of FNZ in the rotarod and the chimney tests and (b) both a NO precursor: l-arginine and a selective inhibitor of phosphodiesterase 5 (PDE5): sildenafil did not affect the development of tolerance to FNZ-induced motor impairment in mice. Those findings provided behavioural evidence that NO could contribute an important role in the development of tolerance to FNZ in mice.

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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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The Importance of l-Arginine:NO:cGMP Pathway in Tolerance to Flunitrazepam in Mice

et al. 2016

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“…The QUAN-0808 had positive effects in both electrical and chemical tests. These animal models are usually considered suitable for identifying anticonvulsant 1,9 activity againsta variety of seizures. The chemical models of seizure, such as PTZinduced seizures, represent models of'myoclonic seizure' that produce clonic and tonic seizures.…”

Section: Anticonvulsant Activitymentioning

confidence: 99%

A Mini Review on Biological Activities of 6-(4-Chlorophenyoxy)-Tetrazolo [5,1-A] Phthalazine (Quan-0808) Compound

Asif¹

2017

Journal of Pharmaceutical Research

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Abstract:Purpose: Approaches:Findings: Conclusions:Key words:QUAN-0808 (6-(4-chlorophenoxy)-tetrazolo[5,1-a]phthalazine) was tested for the anticonvulsant, anti-inflammatory, analgesic, anticoagulant, antithrombotic and antidepressant effects.Anticonvulsant activity was testedby electroshock seizure model and neurotoxicity was tested by the rotarod neurotoxicity test in mice. In chemically induced models of seizure like pentylenetetrazole, isoniazid, thiosemicarbazide and 3-mercaptopropionic acid were further tested for the anticonvulsant activity.QUAN-0808 caused significant anticonvulsant activity against all types of seizures. It appreciably reduced xylene-induced ear edema, reduced the prostaglandin E2 and nitric oxide levels on the edema and reduced acetic acid-induced capillary permeability hyperactivity and reduced acetic acid-induced writhing response. It exhibited anti-inflammatory and antinociceptiveeffect in a dose-dependent manner.The peripheral effect mechanisms of QUAN-0808 may be related to a reduced in the formation of PGE2, NO, bradykinin and additional inflammatory mediators. The anticoagulant and antithrombotic effects of Q808 delayed bleeding and clotting time in mice. QUAN-0808 exerts anticoagulant, antithrombotic and antidepressant effect, exhibited a significant reduction in immobility as antidepressant. anticonvulsant, antidepressive, antinociceptive, antithrombotic. Tetrazolo

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“…In contrast, low NO concentrations may affect GABAergic transmission as an inhibitory effect. [31] A decrease in NO amounts is followed by a corresponding decrease in the GABA levels via an increase in the GABA transaminase activity. [32] Naziroglu et al [21] showed no differences in the NO levels in the brain cortex of rats when seizures were induced with PTZ.…”

Section: Mda Determinationmentioning

confidence: 99%

The Effects of Pregabalin on Cerebral Cortical Oxidative Stress of Rats on Pentylenetetrazole Induced Epileptic Seizure

Tüfekçi¹,

Koyuncuoğlu²,

Kırbaş³

et al. 2013

Epilepsi

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SummaryObjectives: In this experimental model of epileptic seizure induced by pentylenetetrazole (PTZ), we aimed to investigate the effect of pregabalin, (PGB), (Lyrica(R)) in the brain cortex tissues and on superoxide dismutase (SOD) and catalase (CAT) activities as well as nitric oxide (NO) and malondialdehyde (MDA) levels, which are indicators of oxidative stress. Methods:Forty male Wistar rats were randomly divided into four equal groups. The first group was used as a control group. The second group received a single dose administration of PTZ. Third and fourth groups were given, via gastric gavage, doses of 100 mg/kg body weight/day of PGB, divided into two, for two days. Seizure is obtained by applying intraperitoneally (ip) 50 mg/kg body weight of PTZ to groups II and IV. After one hour of PTZ administration, all rats were sacrificed and brain cortex tissues were taken. SOD and CAT activities and NO and MDA levels were studied in the brain cortex tissues.Results: MDA levels and SOD activity of the PGB and PGB+PTZ groups were significantly lower than the control group ( p=0.005, p=0.001 and p=0.005, p=0.004, respectively), and NO level of the PGB and PGB+PTZ groups were significantly higher than the control group (p=0.001, p=0.001, respectively). CAT levels between the groups were similar. Conclusion:Our study results indicate that PGB prevents oxidative stress and increases NO levels in the rat brain cortical tissues during epileptic seizure. Increased NO may contribute to PGB's antiepileptic effect.Key words: Epilepsy; oxidative stress; pregabalin; pentylenetetrazole. ÖzetAmaç: Pentilentetrazol (PTZ) ile epileptik nöbet oluşturulan bu deneysel modelde, beyin korteksinde, oksidatif stresin göstergeleri olan sü-peroksit dismutaz (SOD), katalaz (CAT) aktiviteleri, nitrikoksit (NO) ve malondialdehit (MDA) düzeyleri üzerine pregabalinin (PGB) etkilerini araştırmayı amaçladık. Gereç ve Yöntem:Wistar cinsi 40 adet erkek sıçan rastgele 4 eşit gruba ayrıldı. İlk grup kontrol grubu olarak kullanıldı ve tek doz PTZ uygulanan grup, ikinci grup olarak kabul edildi. Üçüncü ve dördüncü gruba 100 mg/kg vücut ağırlığı/gün PGB ikiye bölünmüş dozlarda intragastrik yolla iki gün verildi. Grup II ve grup IV'e intraperitoneal (i.p.) (50 mg/kg vücut ağırlığı) PTZ uygulanarak nöbet oluşturuldu. PTZ uygulamasından bir saat sonra tüm sıçanlar sakrifiye edildi ve beyin korteksleri alındı. Beyin korteks dokularında SOD ve CAT aktiviteleri ile NO ve MDA düzeyleri çalışıldı.Bulgular: PGB ve PGB+PTZ gruplarında MDA düzeyi ve SOD aktivitesi, kontrol grubundan istatistiksel olarak daha düşük saptandı (sırasıyla p=0.005, p=0.001 ve p=0.005, p=0.004). PGB ve PGB+PTZ gruplarının NO düzeyi, kontrol grubundan istatistiksel olarak daha yüksekti (sırasıyla p=0.001, p=0.001). Gruplar arasındaki CAT düzeyleri benzerdi.Sonuç: Çalışmamızın sonuçları, PGB'nin oksidatif stresi önlediğini ve epileptik nöbet sırasında sıçan beyin korteks dokularında NO düzeylerini arttırdığını göstermiştir. Artmış olan NO düzeyinin PGB'in antiepileptik etkisine katkı ...

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Effects of sildenafil treatment on the development of tolerance to diazepam-induced motor impairment and sedation in mice

Cited by 20 publications

References 36 publications

The Importance of l-Arginine:NO:cGMP Pathway in Tolerance to Flunitrazepam in Mice

The Importance of l-Arginine:NO:cGMP Pathway in Tolerance to Flunitrazepam in Mice

A Mini Review on Biological Activities of 6-(4-Chlorophenyoxy)-Tetrazolo [5,1-A] Phthalazine (Quan-0808) Compound

The Effects of Pregabalin on Cerebral Cortical Oxidative Stress of Rats on Pentylenetetrazole Induced Epileptic Seizure

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