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PubMed1975

[Comparative clinical electroencephalographic study of cycloserine and terizidon tolerance].

The aim of the study was comparative investigation of cycloserin and terizidone tolerance by patients with the lung tuberculosis. The investigation procedure included parallel clinical observations and electroencephalographic studies (EEG) using light and sonic stimulation. Sixty six and 26 patients treated with cycloserin and terizidone respectively were observed. The results of the studies showed that by the mechanism of their action on the central nervous system terizidone and cycloserine were similar and increased the general reactivity of the brain. However, terizidone promoted an increase of the activating effect of the ascending part of the reticular formation of the brain stem to a lesser extent than cycloserine. Terizidone in a dose of 0.25 g 3 times a day was well tolerated by the patients with concomitant psycho-neurological impairements.

Adolescent↗
PubMedDate not supplied

[Effect of the antibiotic D-cycloserine and its dimer on the activity of tyrosine aminotransferase in liver tissue of intact, adrenalectomized and hypophysectomized rats].

In a period of lowest day activity of tyrosine aminotransferase, within 6-8 days after bilatheral adrenalectomy, the enzyme activity was decreased by about 20% as compared with an adequate control. At the same time, within a day and seven days after hypophisectomy, in rat liver tissue the enzyme activity was increased, approximately two-fold as compared with the normal state. Within four hrs after intraperitoneal administration into intact fasting rats at a dose of 2-2.5 g per 1 kg of body weight D-cycloserine and its dimer caused an induction of tyrosine aminotransferase by 75% and 180%, respectively. Induction of the enzyme by D-cycloserine and its dimer was inhibited by actinomycin D; the phenomenon was not observed in adrenalectomized rats. Within a day after hypophisectomy D-cycloserine did not cause the induction of tyrosine aminotransferase in rat liver tissue; to the contrary, the dimer of D-cycloserine caused induction of the enzyme, comparable to the ACTH effect, in liver tissue of hypophisectomized rats.

Adrenalectomy↗
PubMed1987

Inhibition of serine palmitoyltransferase activity in rabbit aorta by L-cycloserine.

Serine palmitoyltransferase (EC 2.3.1.50) initiates the biosynthesis of sphingolipids. Its activity is induced in the aortas of rabbits fed a Purina lab chow supplemented with 2% cholesterol (Williams, R. D., D. S. Sgoutas, and G. S. Zaatari. 1986. J. Lipid Res. 27: 763-770). Induction occurs during atherogenesis in parallel with increased arterial sphingomyelin concentrations. In this study, L-cycloserine was shown to be a potent inhibitor of serine palmitoyltransferase in aortas from New Zealand White rabbits. Activity was reduced in vitro by 50% using 5 microM L-cycloserine with 50 micrograms of microsomal protein. To assess in vivo inhibition, L-cycloserine was administered by intraperitoneal injection to rabbits maintained on either a standard Purina laboratory chow or one supplemented with 2% cholesterol. Serine palmitoyltransferase activity was inhibited by 76% in the aortas of rabbits on the standard chow 4 hr after a single 25 mg/kg body weight dose and 52% after a 10 mg/kg dose. Activity was reduced by 36% in animals on the standard chow and by 37% in the cholesterol-fed group after 1 week of daily doses. These experiments demonstrate that L-cycloserine inhibits serine palmitoyltransferase in aorta, and thus may be used to reduce sphingomyelin concentrations during experimental atherogenesis.

Acyltransferases↗
PubMed1995

The effects of D-cycloserine and MK-801 on the performance of rats in two spatial learning and memory tasks.

The present study was undertaken to investigate the effects of modulation of the N-methyl-D-aspartate (NMDA) receptor on learning and memory. Thus, the performance of rats treated with D-cycloserine, a partial agonist at the glycine recognition site of the NMDA receptor complex, and MK-801, a noncompetitive NMDA receptor antagonist, either alone or concurrently were assessed in radial arm maze and water maze tasks. Administration of MK-801 (0.1 mg/kg, i.p.) impaired acquisition in the water maze (increased escape latency and distance) and working memory in the radial arm maze (increased re-entries) in rats. Moreover, in the radial arm maze, MK-801 disrupted locomotion (increased latencies and decreased arm entries per minute) and impaired the acquisition of reference memory (increased number of errors) performance of rats. D-Cycloserine (0.03, 0.3, 1.0, 3.0, 10 mg/kg, i.p.) had no effects on acquisition or memory performance of control or MK-801-treated rats in either of these tasks. However, D-cycloserine (0.03, 0.3, 3.0 mg/kg) reversed the MK-801-induced disruption in locomotion. Furthermore, 3.0 mg/kg D-cycloserine increased behavioral activity and also decreased the time needed to complete the task in control animals. To conclude, our results suggest that the consequences of NMDA receptor modulation on learning and memory processes and sensorimotor functions may be functionally different or have distinct anatomical locations.

Adaptation, Psychological↗
PubMed1971

Cycloserine Induction, Propagation, and Antimicrobial Susceptibility of Wall-Defective Staphylococcus aureus.

A method of induction of L colonies of Staphylococcus aureus by cycloserine, the propagation of wall-defective staphylococci (WDS), and the development and antimicrobial susceptibility of stable WDS are presented. The growth and morphology of the cycloserine-induced L colonies and WDS were indistinguishable from those induced by methicillin or lysostaphin. The antimicrobial susceptibility of the stable cycloserine-induced WDS was similar to that of the stable methicillin-induced and lysostaphin-induced WDS by both broth dilution and agar diffusion techniques. A survey of the English literature reveals that wall-defective bacteria are always resistent to antimicrobial agents which inhibit cell wall synthesis (cycloserine, penicillins, and cephalosporins). They are virtually all susceptible to antimicrobial agents which have other modes of action. The susceptibility to vancomycin and bacitracin varied from study to study.

Journal Article↗
PubMed1995

Cycloserine-induced lichenoid drug eruption.

A 65-year-old male patient who has taken antituberculous drugs including cycloserine for 8 months showed multiple pruritic, violaceous, flat-topped papules and plaques on his back which had developed 5 months into therapy. Histopathologic findings were consistent with lichenoid drug eruption. Patch test with the drugs revealed a strongly positive reaction to cycloserine only. Four months after discontinuation of oral cycloserine, pruritus resolved and the lesions subsided without any new lesions. Cycloserine is one of the antituberculous drugs. Skin manifestations resulting from its administration are reported to be rare, but to our knowledge, this is the first case report of lichenoid drug eruption from its use.

Aged↗
PubMed1963

ANTAGONISM OF D-CYCLOSERINE INHIBITION OF MYCOBACTERIAL GROWTH BY D-ALANINE.

Zygmunt, Walter A. (Mead Johnson & Co., Evansville, Ind.). Antagonism of d-cycloserine inhibition of mycobacterial growth by d-alanine. J. Bacteriol. 85:1217-1220. 1963.-Reversal of the antimycobacterial activity of d-4-amino-3-isoxazolidinone (d-cycloserine) by alanine in two species of mycobacteria actively growing on chemically defined media was compared. In both instances, d-alanine was the most effective reversal agent. The specificity with which the d isomer reversed the antimycobacterial activity of d-cycloserine was more pronounced than that observed with other species of bacteria. Mycobactin, a growth factor for certain mycobacteria, showed no reversal activity.

Alanine↗
PubMed1994

Effects of D-cycloserine and (+)-HA-966 on the locomotor stimulation induced by NMDA antagonists and clonidine in monoamine-depleted mice.

We have previously observed that an N-methyl-D-aspartate (NMDA) antagonist in combination with the alpha 2-adrenoceptor agonist clonidine produces a marked locomotor stimulation in monoamine-depleted mice. In this paper we report on how the partial glycine agonists D-cycloserine (high intrinsic activity) and (+)-HA-966 [(+)-3-amino-1-hydroxypyrrolid-2-one; low intrinsic activity] affect this response; the interaction with both an uncompetitive and a competitive NMDA antagonist was investigated. (+)-HA-966 was found to counteract the locomotor stimulation produced by clonidine combined with either an uncompetitive (MK-801 = dizocilpine) or a competitive [D-CPPene = 3-(2-carboxypiperazine-4-yl)-1-propenyl-1-phosphonic acid] NMDA antagonist. D-cycloserine potentiated the locomotor stimulation produced by either NMDA antagonist combined with clonidine, although statistical significance was achieved only in the case of MK-801. If the present hyperactivity model has any relevance for psychosis the prediction based on the present results would be that d-cycloserine, contrary to current hopes, might not be so effective in schizophrenia, whereas (+)-HA-966 might be an interesting candidate.

Allosteric Site↗
PubMed1998

Cycloserine-induced decrease of cerebroside in myelin.

L-Cycloserine has been shown specifically to lower brain cerebroside levels in vivo, but the extent to which the decrease in whole brain cerebroside content reflects lower myelin cerebroside levels is not known since a substantial portion of cerebroside is found in nonmyelin membranes. The present report demonstrates that chronically administered cycloserine lowers the proportion of cerebroside in rat brain myelin. Cycloserine-induced decrease of myelin cerebroside should provide a useful tool in investigating the role of cerebroside in maintaining myelin stability.

Animals↗
PubMed1992

D-cycloserine reverses the working memory impairment of hippocampal-lesioned rats in a spatial learning task.

It is shown that D-cycloserine has cognition-enhancing properties in quinolinic acid hippocampal-lesioned rats. Lesioned rats had a severe impairment of working memory in an allocentric spatial reversal paradigm in the 8-arm maze, and performance could be restored with 12 mg/kg i.p. D-cycloserine, given 30 min before testing. The present findings favour the testing of D-cycloserine for clinical efficacy in patients with Alzheimer's disease with loss of pyramidal neurons and disconnected glycine-NMDA receptor activation.

Analysis of Variance↗
PubMed1992

Failure of d-cycloserine to reverse cognitive disruption induced by scopolamine or phencyclidine in primates.

The partial glycine agonist d-cycloserine may be of therapeutic use as a cognitive enhancer. We examined the ability of d-cycloserine (3-14 mg/kg i.m.) to reverse cognitive impairments induced by scopolamine (0.03 mg/kg) or PCP (0.25 mg/kg). There was no evidence for a dose-related improvement in visuospatial memory using retention intervals of 2,10 or 20 sec. A possible explanation for these findings is that central glycine function cannot be adequately increased using systemic administration of d-cycloserine in this dose range.

Animals↗
PubMed1992

D-cycloserine, a modulator of the N-methyl-D-aspartate receptor, improves spatial learning in rats treated with muscarinic antagonist.

The results of the present study indicate that D-cycloserine, a partial agonist at the glycine binding site, which is a positive modulation site of the N-methyl-D-aspartate receptor, could improve dose dependently the acquisition of a water maze task in rats treated with scopolamine, a muscarinic antagonist. The low to moderate doses of D-cycloserine which improved learning did not affect swimming speed in scopolamine-treated rats. The higher dose did not improve learning, but it increased swimming speed in scopolamine-treated rats. These results show a dissociation between impaired acquisition and abnormal behavioral activity in scopolamine-treated rats in the water maze task. Furthermore, the present results suggest that D-cycloserine can act as a cognitive enhancer at the appropriate doses.

Amnesia↗
PubMed1987

Simultaneous quantification of cycloserine and its prodrug acetylacetonylcycloserine in plasma and urine by high-performance liquid chromatography using ultraviolet absorbance and fluorescence after post-column derivatization.

D-Cycloserine is a broad-spectrum antibiotic used with other antibiotics to treat various forms of tuberculosis. Its prodrug sodium (R)-4-[(1-methyl-3-oxo-1-butenyl)amino]-3-isoxazolidinone hemihydrate, developed for better aqueous stability and solubility, is combined with another broad-spectrum antibiotic, fludalanine. An ion-pair, reversed-phase high-performance liquid chromatographic assay has been developed to simultaneously detect cycloserine and its prodrug in plasma and urine. The prodrug is detected directly by ultraviolet absorbance and cycloserine by fluorescence following post-column derivatization.

Adult↗
PubMed2006

A randomized controlled trial of the effect of D-cycloserine on exposure therapy for spider fear.

Previous research [Hofmann SG, Meuret AE, Smits JA, Simon NM, Pollack MH, Eisenmenger K, et al. Augmentation of exposure therapy for social anxiety disorder with D-cycloserine. Archives of General Psychiatry 2006;63:298-304; Ressler KJ, Rothbaum BO, Tannenbaum L, Anderson P, Graap K, Zimand E, et al. Cognitive enhancers as adjuncts to psychotherapy: use of d-cycloserine in phobic individuals to facilitate extinction of fear. Archives of General Psychiatry 2004;61:1136-44] suggests that d-cycloserine (DCS) facilitates the reduction of clinical fear in humans. We used a well established intervention to evaluate the effectiveness of administering DCS as an adjunct to exposure therapy in a heightened, but sub-clinical, fear population. Over two studies, 100 spider-fearful participants were allocated to DCS or placebo before treatment and were assessed at pre-, immediate post-, and 3.5 weeks post-treatment. Significant treatment effects and return of fear was observed at follow-up, particularly in non-treatment contexts; however, both studies failed to demonstrate any enhancing effects of DCS (50 or 500 mg). DCS did not enhance the reduction of spider fears or the generalisation of treatment of a single session of exposure-based therapy. These results suggest that DCS may not enhance loss of non-clinical levels of fear in human populations.

Adolescent↗
PubMed2000

IV glycine and oral D-cycloserine effects on plasma and CSF amino acids in healthy humans.

BACKGROUND: The amino acid glycine, modulates neurotransmission via actions at GLY-A receptor and GLY-B receptor. The latter are coagonist sites associated with N-Methyl-D-Aspartate (NMDA) glutamate receptors. The central bioavailability of peripherally administered glycine has not been adequately characterized in humans. METHODS: Healthy human subjects were administered either oral D-cycloserine (50 mg or placebo) and intravenous glycine (saline, 100 mg/kg or 200 mg/kg) in random order over 4 test days under double-blind conditions. Cerebrospinal fluid was collected by lumbar puncture performed on the first test day was analyzed to determine amino acid levels. The acoustic startle response was measured on the second test day. RESULTS: Intravenous glycine dose-dependently increased both serum and CSF glycine and serine levels. Neither glycine nor DCS produced any significant effects on behavior, cognition or the acoustic startle response. Neither IV glycine nor DCS were associated with any toxicity. CONCLUSIONS: Thus, peripheral glycine administration raised CSF glycine levels without producing any clear central nervous system effects. Glycine and D-cycloserine did not worsen cognitive test performance and did not induce behavioral symptoms on their own. The possibility that glycine and D-cycloserine enhanced cognitive test performance cannot be excluded given the psychometric limitations of the test battery.

Acoustic Stimulation↗
PubMed1998

The stereo-specific effect of D-serine ethylester and the D-cycloserine in ataxic mutant mice.

Spinocerebellar ataxia is one of the most common neurological disorders. However, few therapeutics are effective for the treatment of this disorder. In the present study, we investigated the efficacy of d-serine ethylester and a related substance, d-cycloserine, as therapeutic agents for ataxia in a murine model. Both compounds are known to stereospecific modulate N-methyl-d-aspartate type glutamate receptors, and impaired glutamate-mediated signaling has been implicated in spinocerebellar ataxia. Using a microdialysis method, we found that intraperitoneal administration of d-serine ethylester increases the extracellular content of endogenous d-serine in the mouse cerebellum for at least 3 h. Maximum elevation of the extracellular d-serine was observed at 40 min after injection. An open-field study was used to assay the effect of the d-serine derivatives on movement and ataxia. In mice exhibiting cytosine arabinoside-induced ataxia, d-serine ethylester reduced the falling index in a dose-dependent manner. The effect of d-serine ethylester was stereo-specific in that l-serine ethylester had no effect on the falling index at the maximum doses tested, and was partially inhibited by 5,7-dichlorokynurenate, an antagonist that binds to the glycine-binding site. Locomotor activity was not changed by the d-serine ethylester treatment. d-cycloserine also significantly reduced the falling index of the mice. Both d-serine ethylester and d-cycloserine had longer lasting effects than other potential therapeutic reagents for ataxia. Growing evidence suggests the essential involvement of endogenous d-serine in mammalian brain function, and our results suggest that d-serine derivatives may represent an effective new therapeutic for the treatment of spinocerebellar ataxia.

Animals↗
PubMed2000

Pre-training blocks the improving effect of tetrahydroaminoacridine and D-cycloserine on spatial navigation performance in aged rats.

We investigated the effect of pre-training on the improvement of spatial navigation performance provided by a cholinesterase inhibitor, tetrahydroaminoacridine (3 mg/kg, i.p.), and a positive modulator of NMDA receptor, D-cycloserine (10 mg/kg, i.p.), or their combination in aged rats. Pre-training consisted of spatial or non-spatial conditions and took place in either the same or a separate room. We found that any kind of pre-training was able to eliminate the enhancing effect of tetrahydroaminoacridine and D-cycloserine on spatial navigation. However, none of these pre-training conditions was able to block the age-related deficit in spatial navigation. These results indicate that tetrahydroaminoacridine and D-cycloserine, separately or in combination, do not themselves alleviate the age-related spatial memory deficit, but may enhance procedural aspects of water maze learning in aged rats.

Aging↗
PubMed1997

Infusion of D-cycloserine into temporal-hippocampal areas and restoration of mnemonic function in rats with disrupted glutamatergic temporal systems.

Partial transections of the fiber connections between the temporal cortex and the lateral entorhinal cortex at a site of the white matter corresponding to the perirhinal cortex result in impaired visual memory accompanied by reduced concentrations of glutamate in both the temporal cortex and lateral entorhinal cortex. Intraperitoneal administration of the glycinergic receptor agonist D-cycloserine produces complete restoration of memory function, as measured by a brightness discrimination task in rats with temporal cortex/lateral entorhinal cortex transections. The purpose of the present study was to identify in which brain structures the compensatory activity might take place. The results show that infusion of cycloserine into either the temporal cortex or lateral entorhinal cortex fully ameliorated the impairment of temporal cortex/lateral entorhinal cortex lesions, whereas infusion into the hippocampal region caused only a mild improvement of the retention performance. Infusion of cycloserine into the frontal cortex or saline into the temporal cortex or lateral entorhinal cortex had no ameliorating effects on the memory dysfunction of rats bearing temporal cortex/lateral entorhinal cortex transections. It is concluded that the temporal cortex, lateral entorhinal cortex and perirhinal cortex are highly critical in forming visual memory.

Analysis of Variance↗