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Piracetam, Levetiracetam, and cycloprolylglycine


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#1 stellar

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Posted 03 January 2005 - 04:13 AM


1: J Affect Disord. 1979 Dec;1(4):227-35. Related Articles, Links

Evidence that piracetam has an anxiolytic action.

File SE, Hyde JR.

In the social interaction test of anxiety Piracetam (100 mg/kg) had an anxiolytic profile very similar to that seen after 5 days of administration of chlordiazepoxide (5 mg/kg). Piracetam (50-300 mg/kg) produced no signs of sedation and it was therefore suggested that it might be a non-sedative anxiolytic drug. Piracetam (100 mg/kg) produced significantly higher cortical concentrations of 5-hydroxytryptamine and lower concentrations of 5-hydroxyindoleacetic acid, indicating a reduced 5-HT turnover. There were no drug-induced changes in noradrenaline or dopamine in any brain region, either with or without pretreatment with alpha-methylparatyrosine. The cortical concentrations of 7 amino acids were measured and were unchanged by treatment with Piracetam.

PMID: 95599 [PubMed - indexed for MEDLINE]



Anxiolytic profile of the antiepileptic drug levetiracetam
in the Vogel conflict test in the rat
by
Lamberty Y, Falter U, Gower AJ, Klitgaard H.
UCB S.A. Pharma Sector,
Preclinical CNS Research, Chemin du Foriest,
B-1420 Braine l'Alleud, Belgium.
yves.lamberty@ucb-group.com
Eur J Pharmacol. 2003 May 23;469(1-3):97-102

ABSTRACT

The novel antiepileptic drug levetiracetam has been shown to reverse anxiogenic effects of benzodiazepine withdrawal in mice tested in an elevated plus-maze without altering the behaviour of normal mice in this model. This could suggest that the effect of levetiracetam is dependent upon the level of stress/anxiety of the animals. Levetiracetam was therefore further examined in another widely used animal model of anxiety, the Vogel conflict test. In the first experiment, water-deprived rats were submitted to a free drinking period (habituation) in a chamber equipped with a bottle of water. Twenty-four hours later, animals were returned to the same chamber but the licks to the water bottle were then punished with a foot shock (0.5 mA, 90 ms). In the second experiment, the procedure was modified by administering a foot shock at the end of the habituation period in order to induce a state of stress/anxiety (conditioned fear/ anticipatory anxiety) for subsequent testing. Levetiracetam (17 and 54 mg/kg) and chlordiazepoxide (5 mg/kg) were administered via the intraperitoneal route. The results indicated that in the first experiment only chlordiazepoxide showed a statistically significant anxiolytic effect. In contrast, in the second experiment, where the shock was given at the end of the habituation period, levetiracetam (54 mg/kg) revealed significant anxiolytic activity similar to chlordiazepoxide. This suggests that levetiracetam may have potential anxiolytic effects and may provide therapeutic benefits to individual with anxiety spectrum disorders.




1: Bull Exp Biol Med. 2001 May;131(5):464-6. Related Articles, Links

Anxiolytic activity of endogenous nootropic dipeptide cycloprolylglycine in elevated plus-maze test.

Gudasheva TA, Konstantinopol'skii MA, Ostrovskaya RU, Seredenin SB.

Institute of Pharmacology, Russian Academy of Medical Sciences, Moscow. uusolari@solaris.msk.ru

Testing in an elevated plus-maze revealed dose-dependent anxiolytic activity of piracetam analog cycloprolylglycine. Intraperitoneal injection of this agent (0.05 mg/kg) 9-fold prolonged the time spent in open arms compared to the control, without affecting the total motor activity. This effect was stereo-selective: D-enantiomer in doses of 0.05 and 0.1 mg/kg was inactive. Therefore, cycloprolylglycine is similar to piracetam in not only nootropic, but also anxiolytic activity. The existence of an endogenous system responsible for the co-regulation of memory and anxiety is hypothesized.

PMID: 11550054 [PubMed - indexed for MEDLINE]

#2 lynx

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Posted 03 January 2005 - 04:23 PM

Stellar,

Regarding cycloprolylglycine, there are so many peptides out there that do all sorts of interesting things, but one of the problems with them is they have to be injected in order to be effective, even glutathione, a very simple peptide.

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#3 power.bulls.x

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Posted 12 November 2005 - 01:25 AM

LEVETIRACETAM is just a replacement for benzo ?
does it cary nootropic actions ?

#4 goku

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Posted 12 November 2005 - 11:08 AM

Speaking of injecting Gluthianone. Why aren't we doing that? We really should. it's way way more effective antioxidant treatment than us popping r-lipoic acid and NAC, etc. Injecting is not at all a big deal, and I imagine injecting subcutaneously would be fine. Diabetics insulin dependant inject sub-q all the time, it's easy, painless and conveinant.

Would you need a particular type of Gluthianone, or could you simply emulsify some with bacteriostatic water and inject. If anyone has a suggestion as to go about this, I'm in in a heartbeat.

#5 goku

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Posted 12 November 2005 - 11:08 AM

Lynx, injection is not a problem. Needle paranoia is just that.

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#6 drmz

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Posted 22 January 2006 - 08:08 PM

Levetiracetam: An improvement of attention and of oral fluency in patients with partial epilepsy.

Piazzini A, Chifari R, Canevini MP, Turner K, Fontana SP, Canger R.

Regional Epilepsy Center, S. Paolo Hospital, University of Milan, Via A. Di Rudini 8, 20142 Milan, Italy.

PURPOSE: The aim of the present study is to verify whether patients with partial epilepsy receiving levetiracetam (LEV) as an add-on treatment show an improvement in cognitive function. METHODS: A neuropsychological battery of tests was administered to 35 patients with partial epilepsy before the assumption of LEV and after the achievement of the therapeutical dose of this drug, 7 weeks later. A control group of 35 patients with partial epilepsy was administered the same battery of tests twice, at the same time interval as the LEV group. The controls were administered the same pharmacological treatment, which did not include LEV in either of the two sessions. RESULTS: We found a statistically significant improvement in cognitive functioning, i.e. in attention and oral fluency, in patients receiving LEV compared to the controls. The responders to LEV were 28.6%. CONCLUSIONS: LEV as an add-on therapy improved attention level and verbal fluency in our sample of patients with partial epilepsy. It is reasonable to assume that LEV may influence the metabolism of attention and of language area, as already suggested for piracetam (PIR) from which LEV derives. Further studies are needed to confirm these findings.

2005 Dec 2




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