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Bu çalışmanın amacı Akgiritotu'nun farmakolojik ve toksikolojik etkilerini araştırmaktır. Yaprak ve meyvalarmdan hazırlanan sulu ekstreler kobay derisi üzerinde 2,4-dinitrobenzen ile karşılaştırmalı olarak test edilmiştir. Ekstrelerin injekte edildiği kobay derisi üzerinde hislopatolojik inceleme yapıldığında mast hücrelerinde herhangi bir değişim gözlenmemiş, ancak hipodermisle eksudatif inflamasyon ve polimorfonükleer lökosit infiltrasyonu dikkat çekmiştir. Ayrıca ödem oluşturucu etkinlikleri sıçan pençe deneyinde de test edilmiş ve sözkonusu etkiler formalin ile oluşturulan etkiler ile karşılaştırılmıştır. Kobaylarda in vivo bronşiyal tonüs/kan basıncı ve izole ileum deneyleri gerçekleştirilmiştir. Sözkonusu bu bitkiden hazırlanan sulu ekstrelerin doza bağımlı olmayan bronkokonstriksiyon ve hipotansiyona neden olduğu bulunmuştur. Ekstreler izole kobay İleumunda klorpromazin, ketotifen ve deksametazon ile önlenemeyen ve konsantrasyona bağımlı olan kasılmalar oluşturmuşlardır. D. albus ekstrelerininfarelerde "Tail-Clip" deneylerinde ağrı eşiği üzerinde anlamlı bir etkisi olmamıştır. Ekstrelerin santral sinir sistemi üzerideki etkileri farelerde yüzme dayanıklılık testi ve gözlemsel tarama yardımı ile sınanmıştır. Burada sedatif etki gözlenmiştir. D. albus'tan hazırlanan sulu ekstrelerin akut fazlı inflamatuvar bir yanıta neden olduğu sonucuna varılmıştır., Purpose of the present study was to investigate pharmacological and toxicological effects of gas plant. Aqueous extracts prepared from its leaves and fruits were tested on the guinea-pig skin by comparing with 2,4-dinitrochlorobenzene. When histopathological examination was made on guinea-pig skin injected with the extracts, there was no change observed in mast cells, but acute exudative inflammation and infiltration of polymorphonuclear leukocytes were noticed in the hypodermis. Their edema forming activities were also tested in the rat paw experiment and their effects were compared to those induced by formalin. In vivo bronchial tone/blood pressure and isolated ileum experiments in guinea-pigs were performed. Aqueous extracts prepared from this plant were found to cause bronchoconstriction and hypotension, which were not dose-dependent. They also elicited concentration-dependent contractions of the isolated guinea-pig ileum, which were not abolished by chlorpheniramine, ketotifen and dexamethasone. D. albus extracts had no significant effect on the mouse pain threshold in "Tail-clip" experiments. Their effects on the central nervous system were examined by using swimming endurance test and observational screening on mice. In this case, a sedative activity was observed. It was concluded that aqueous macerates from leaves and fruits of D. albus causes an acute phase inflammatory response.

Loperamide-induced suppressive effects on central nervous system closely relate to a lack of or decline in the P-glycoprotein (P-gp) function. The aim of this study was to determine the loperamide-induced sedative effect quantitatively and to investigate possible alterations in the pharmacokinetics of digoxin, a substrate for P-gp, in Japanese subjects.Loperamide hydrochloride (2 mg) was administered orally to 26 subjects and the critical flicker-fusion frequency threshold (CFF) values were measured every 30 min separately by portable instrument. Further, digoxin (0.25 mg) was administered to 8 subjects, and the plasma concentration was determined.In five subjects who complained of drowsiness, the CFF values more remarkably decreased compared with those in the other subjects. The Tmax and mean residence time (MRT) values of digoxin pharmacokinetics in four subjects with drowsiness were significantly lower and Cmax was higher than those in four subjects with marginal effect. Moreover, there were good correlations between the CFF value-time profile and the Cmax, Tmax, and MRT of digoxin.The determination of the CFF value after oral administration of loperamide will be useful for evaluating varied P-gp function and for anticipating individual variations in the disposition of P-gp substrates in humans.

Clove oil has become a popular fish anaesthetic for invasive fisheries research procedures, but few studies have examined the use of low concentrations of clove oil to achieve sedation for aquaculture procedures such as fish handling and transport. In this study, we used largemouth bass as a model species to examine the behavioral and physiological responses of fish to a gradation of clove oil concentrations (0 to 20 mg l 1 ) while exposed to truck transport. Concentrations of clove oil ranging from ~5 to 9 mg l 1 elicited a sedative effect resulting in loss of reactivity and reduced cardiac output while maintaining equilibrium. Fish sedated by 5 to 9 mg l 1 clove oil achieved that level of anaesthetization rapidly and recovered behaviorally more quickly than at higher concentrations. During transportation, videography revealed that fish in deep sedation (stage 2

We have synthesized a series of 1,3-disilabenzo[5,6]cyclohexene derivatives starting from (o-bromomethylphenyl)dimethylchlorosilane. Based on NMR data, we have concluded that there is a transannular N → Si interaction in the 3',3'-5-trimethyl-2,8-dioxa-5-aza-1-silacyclooctane-1-spiro-1'-(1',3'-disilabenzo[4',5']cyclohexene) obtained. We have studied the psychotropic activity of this compound and its iodomethylate and also 3-(3-chloropropyl)-1,1,3-trimethyl-1,3-disilabenzo[5,6]cyclohexene, and we have shown that they have a sedative effect.

The sedative activity of eight aromatic natural medicines that are traditionally used in Japanese scent sachets was examined using an open field test with mice. Galangal (Kaempferia galanga), patchouli (Pogostemon cablin), sandalwood (Santalum album), spikenard (Nardostachys chinensis), cinnamon (Cinnamomum cassia), clove (Syzygium aromaticum), star anise (Illicium verum), and borneol (Dryobalanops aromatica) distilled oils were used. These natural medicines have various pharmacological effects. For example, galangal has insecticidal activity and clove extracts possess strong total antioxidant activity. Aromatherapy, a well-known complementary medicine system that uses inhalation, has recently attracted much attention. The sedative activity of inhaled aromatic compounds or essential oils has been examined by measuring the spontaneous motor activity of mice in an open field test. The galangal, patchouli, sandalwood, spikenard, and borneol oils showed significant sedative effects. The effect was stronger for a mixture of the five oils than for any of the single oils. This suggests that the oil mixture may have synergistic activity. Sedative activity was not observed when inactive oils (cinnamon, clove, and star anise) were added to the mixture of the five active oils.

Antianxiety action of diterpene alkaloid songorine was studied using Vogel conflict test. Songorine in a dose of 0.25 mg/kg demonstrated high anxiolytic activity comparable to that of phenazepam and produced no sedative effect.

The relationship between the cerebral pharmacokinetics of diazepam and its active metabolites (desmethyldiazepam, oxazepam) and the anxiolytic effect evaluated by the four-plates test and the light/dark test were investigated after a single intra-peritoneal injection of diazepam (1 mg/kg or 1.5 mg/kg). For up to 30 min after administration, the sedative effect interfered with the anxiolytic effect, thus the results of the anxiolytic effect were not interpretable. From 30 min to 60 min after administration, this interference disappeared, the cerebral level of benzodiazepines was stable (the brain elimination of diazepam was compensated for by the appearance of desmethyldiazepam followed by oxazepam) but the anxiolytic effect decreased dramatically in all the tests with diazepam 1 mg/kg or 1.5 mg/kg. The acute tolerance to benzodiazepines and the difference of affinity for subtypes of GABA(A) receptors between diazepam, desmethyldiazepam, oxazepam could explain this result.

The positive association between alcoholism and depression is a common clinical observation. We investigated the relationship between depression and reward mechanisms using a validated animal model for depressive-like behaviour, the olfactory bulbectomy in rats. The effects of bilateral olfactory bulbectomy on reward mechanisms were studied in two different experimental paradigms – the voluntary self-administration of ethanol and the conditioned place preference to alcohol injection and compared to the effects of ethanol on locomotor activity and body core temperature. The voluntary ethanol intake was increased significantly in bulbectomised rats in a drinking experiment and also after a period of abstinence. Conditioned place preference (CPP) was induced in all animals. However, bulbectomised rats needed a higher dose of alcohol to produce CPP. The sedative effect of ethanol on locomotor activity was reduced in bulbectomised animals. Measurement of body temperature revealed a dose-dependent hypothermic effect of ethanol in both groups. These results suggest that the reward mechanisms may be altered in this animal model as a common phenomenon associated with depression. Furthermore, they support the hypothesis that the addictive and/or rewarding properties of some drugs of abuse may be modified in depression.

Objective—To evaluate the thermal antinociceptive effects and duration of action of buprenorphine hydrochloride after IM administration to American kestrels (Falco sparverius). Animals—12 healthy 3-year-old American kestrels. Procedures—Buprenorphine hydrochloride (0.1, 0.3, and 0.6 mg/kg) and a control treatment (saline [0.9% NaCl] solution) were administered IM in a randomized crossover experimental design. Foot withdrawal response to a thermal stimulus was determined 1 hour before (baseline) and 1.5, 3, and 6 hours after treatment administration. Agitation-sedation scores were determined 3 to 5 minutes before each thermal stimulus. Adverse effects were monitored for 6 hours after treatment administration. Results—Buprenorphine hydrochloride at 0.1, 0.3, and 0.6 mg/kg, IM, increased thermal threshold for 6 hours, compared with the response for the control treatment. There were no significant differences among buprenorphine treatments. A mild sedative effect was detected at a dose of 0.6 mg of buprenorphine/kg. Conclusion and Clinical Relevance—At the doses tested, buprenorphine hydrochloride resulted in thermal antinociception in American kestrels for at least 6 hours, which suggested that buprenorphine has analgesic effects in this species. Further studies with longer evaluation periods and additional forms of noxious stimuli, formulations, dosages, and routes of administration are needed to fully evaluate the analgesic effects of buprenorphine in American kestrels.

Small platform (SP) stress was induced by placing mice on small platforms (3.5 cm diameter) surrounded by water for 24 h. This model contains several factors of stress like rapid eye movement (REM) sleep deprivation, isolation, immobilization and falling into the water. The staircase test consisted of placing a mouse in an enclosed staircase with 5 steps and recording (1) the number of steps and (2) rearings made during 3 min. SP stress increased the exploratory activity of mice in the staircase test as evidenced by an increase in the number of steps and rearings made In control mice diazepam (0.25 and 0.5 mg/kg) induced an anxiolytic effect in the staircase test as evidenced by a decrease in the number of rearings without changes in the number of steps. In SP stressed mice the anxiolytic effect of diazepam was not seen and the sedative effect as evidenced by a decrease in the number of steps was more pronounced. Buspirone at a dose of 1.0 mg/kg did not have effect on the behaviour of control or SP stressed mice in the staircase test. To study possible diurnal variations the staircase test was carried out at 3 different times of a day (08:00, 14:00, 20:00) with control and SP stressed mice. The exploratory activity of control mice in the staircase test gradually increased from 08:00 to 20:00 as evidenced by an increased number of steps and rearings made. SP stress increased the exploratory activity of mice irrespective of the time of testing. In conclusion, on the basis of these data the authors can propose that SP stress increases the exploratory activity of mice in the staircase test and induces a hyposensitivity of mice to the anxiolytic effect of diazepam. The effect of SP stress on the behaviour of mice in the staircase test is not caused by the disruptance of diurnal rhythms.

RESUMEN Recientes investigaciones senalan que las semillas de Erythrina americana Miller tienen un alto contenido de proteina y un adecuado contenido de lipidos, lo cual representa una alternativa para ser usadas como alimento humano. Las flores y semillas de E. americana conocidas como "Colorin" son altamente apreciadas por su sabor y son empleadas como complemento proteinico en algunos paises. En muchas regiones de Mexico, tradicionalmente son cocinadas las flores, pero las semillas no son consumidas por su alta toxicidad debido a la cantidad de alcaloides que contienen. Los cuales tienen un efecto sobre el sistema nervioso periferico, como relajante muscular y en el sistema nerviosos central como sedante. El objetivo del presente trabajo fue determinar el contenido y distribucion de alcaloides en las flores (caliz y corola) y localizar los alcaloides mas toxicos. Mediante las tecnicas de cromatografia de liquidos y espectrometria de masas, se analizo el extracto observandose un alto contenido de alcaloides en el caliz en comparacion con el encontrado en la corola, sin embargo, los alcaloides toxicos α y β-eritroidina fueron detectados en ambos tejidos. PALABRAS CLAVE: α- y β-eritroidina, Leguminosae, caliz, corola, cromatografia de liquidos, espectrometria de masas IDENTIFICATION OF ALKALOIDS IN THE INFLORESCENCES OF Erythrina americana Miller SUMMARY Recent research has shown that the seeds of Erythrina americana Miller are high in proteins and an adequate content of lipids, giving it possibilities as a human food. The E. americana flowers and seeds are known in Mexico as "Colorin", and are highly appreciated for their flavor; in some countries they are used as a protein complement. In several regions of Mexico, traditionally the flowers are cooked, but the seeds are not consumed because the presence of alkaloids makes them highly toxic. The alkaloids affect the peripheral nervous system: muscular relaxation and a strong sedative effect on the central nervous system. The objective of the present study was to determine the alkaloid content in some parts of the flowers (calyx and corolla) and where the most toxic alkaloids are located. By liquid chromatography and mass spectrometry of the extract, it was observed that alkaloid content was higher in the calyx than in the petal, although the toxic alkaloids α- y β-erythroidine were detected in both tissues.

Thirty-nine horses were given detomidine 10 micrograms/kg bodyweight (bwt) intravenously (iv) and six horses were given a corresponding volume of saline solution before minor procedures. Venous blood samples were collected for catecholamine and cortisol determination immediately before the detomidine or saline injection and 20 mins after it. The behaviour of the horse at the time of detomidine injection and the extent of sedation were evaluated. Plasma adrenaline, noradrenaline and the catecholamine metabolites, 3,4-dihydroxyphenylglycol (DHPG) and 3,4-dihydroxyphenylacetic acid (DOPAC), and cortisol concentrations decreased significantly after administration of detomidine, but they remained unchanged in the control group. A high plasma adrenaline concentration before detomidine injection, indicative of a high level of stress, seemed to correspond with a reduced sedative effect of detomidine. The extent of sedation also was related to the concentrations of adrenaline, noradrenaline and DHPG in plasma after the detomidine injection. The reductions in the plasma catecholamine concentrations may have been caused, in part, by decreased secretion of catecholamines due to the sedative effects of detomidine; but detomidine also influences the plasma catecholamine concentrations by reducing directly sympatho-adrenal activity.

Behavioral effects of a water-soluble extract of Agastache mexicana, a plant with purported anxiolytic actions, were studied in male Wistar rats. In the elevated plus-maze test, various doses of the plant extract (3.0 mg/kg body wt.; 9.0 mg/kg body wt.; 12.0 mg/kg body wt.) administered intraperitoneally (i.p.) decreased the exploration of open arms, showing an anxiogenic-like effect. Agastache mexicana (12 mg/kg body wt.; i.p.) did not change immobility in the forced swimming test (i.e., had no anti-depressant effect) but increased the anti-immobility action of 32.0 mg/kg body wt. (i.p.) of desipramine (i.e., increased the antidepressant-like effect of desipramine). A. mexicana had no effect on exploratory activity in an open field test, indicating that it had no sedative effect at the doses used. It is concluded that effects of the water extract of A. mexicana are more consistent with an anxiogenic-like property than an anxiolytic-like one.

Previous studies have suggested that psychological stress delays cutaneous barrier recovery following acute barrier disruption, and that sedative drugs block this delay. A sedative effect of some odorants has been reported. In the present study, we demonstrate that odorant inhalation affects cutaneous barrier homeostasis in both mice and humans. Odorants with a sedative effect prevented the delay of skin barrier recovery induced by stress after acute barrier disruption. Other odorants did not show this effect.

In this paper it is demonstrated that by adequate selection of topological descriptors we can make possible the prediction of different pharmacological properties, such as plasmatic concentration or sedative effect, within a group of antihistaminic drugs. Moreover, also demonstrated is the usefulness of molecular connectivity in the search of new active compounds. Examples of such compounds are 4-(l-buthylpenthyl)pyridine, N-(3-bromopropyl)-phtalimide and N-(3-chlorpropyl)-piperidin hydrochloride. All of them show antihistaminic activity values more than 30% higher than that of terfenadine, which is used as the reference drug.

Background The effect of propofol on anxiety has not been well studied. In humans, such investigations are confused by the fact that sedation often coexists with anxiolysis. Therefore, the authors evaluated the effects of minimal sedation with propofol in rats placed in an innate anxiogenic situation, the elevated plus-shaped maze. Methods In experiment 1, spontaneous locomotor activity was determined in rats as a measure of sedative effect induced by propofol (0-9 mg/kg administered intraperitoneally). In experiment 2, groups of rats received propofol (0-9 mg/kg) or diazepam (0-2 mg/kg) and then were placed on a plus-shaped maze elevated above the ground that was composed of two opposite closed arms and two opposite open arms. On an initial exposure to the maze, undrugged rats avoid the open arms, with the number of entries into and time spent within the open arms constituting approximately 20% of their total activity. This reflects normal anxiety in a rodent for any elevated open platform. Results In experiment 1, 0-9 mg/kg propofol did not alter spontaneous activity in rats. In experiment 2, propofol and diazepam significantly increased the number of entries into and the time spent within the open arms. Propofol at a dose of 9 mg/kg significantly increased the rats' level of exploration of the open arms to about 50% of all exploratory activity, and a similar observation was made with 2 mg/kg diazepam. Conclusions In a standard animal model, propofol has anxiolytic properties at doses that do not produce sedation.

Sedative effect of the aqueous extract of Centranthus longiflorus ssp. longiflorus (Cle-1) on intact and adrenalectomized rats was investigated using a thiopental sleeping test to clarify the relationship of this effect on adrenal gland hormones, particularly glucocorticoids. Adrenal gland hormones were found to play an important role in inhibiting the sedative effect of the investigated drugs. It is clear, however, that these hormones are not glucocorticoids. Glucocorticoids were not responsible for shortening the sleep period.

Electroencephalography (EEG) is an effective method for the evaluation of sedation or anesthesia. The purpose of this study was to examine the sedative effect of acupuncture by electroencephalographic spectral edge frequency (SEF) in Miniature Schnauzer dogs (4.2-6.1 kg, 1-2 years old). The acupuncture points "GV20 and Yintang" were applied for 20 min. Sedation level was assessed before, during, and after acupuncture by spectral edge frequency 95 values and the Ramsay sedation score. The spectral edge frequency 95 values were significantly reduced during acupuncture on GV20 or Yintang point and returned to the baseline values after acupuncture releasing. The Ramsay sedation score (RSS) also showed the acceptable sedation level during acupuncture. It was concluded that an acupuncture application at GV20 or Yintang point used in the present study would be a valuable method to induce the sedation in dogs.

ミダゾラム注腸による術前鎮静では,年少児ほど効果が減弱することが報告されている.この現象に年齢による代謝の違いが関与しているか,8歳までの手術患者13名を対象として血中濃度を測定し検討した.ミダゾラムは入室30分前に1mg/kgを注腸し,鎮静度は6点法で,血中濃度は観血的動脈路留置後,動脈血で測定した.鎮静度,年齢,血中濃度の関係をSpearmanの順位相関を用いてp

Monoamine oxidase (MAO) inhibitors are generally used in the treatment of depressive disorders and some neurodegenerative illnesses, such as Parkinson's disease and Alzheimer's disease. The aim of this preliminary study was to investigate the MAO [MAO (E.C.1.4.3.4)] inhibiting effect of various apitherapeutic products, such as chestnut honey, pollen and propolis. Extracts' MAO inhibition was measured using peroxidase-linked spectrophotometric assay in enzyme isolated from rat liver microsomes, and the values are expressed as the inhibition concentration (IC50) causing 50% inhibition of MAO. The antioxidant activity of the bee products was also determined in terms of total phenolic content (TPC) and ferric reducing/antioxidant power in aquatic extracts. All samples exhibited substantial inhibition of MAO, propolis having the highest. Inhibition was related to samples' TPCs and antioxidant capacities. These results show that bee products possess a sedative effect and may be effective in protecting humans against depression and similar diseases.

Introduction Poor sleep quality in pregnancy is frequent. A treatment with sedatives is problematic due to possible adverse effects for mother and embryo/foetus. In the present study, we investigated the sedative effect of Bryophyllum pinnatum , a phytotherapeutic medication used in anthroposophic medicine. In previous clinical studies on its tocolytic effect, B. pinnatum showed a good risk/benefit ratio for mother and child. A recent analysis of the prescribing pattern for B. pinnatum in a network of anthroposophic physicians revealed sleep disorders as one of the most frequent diagnoses for which these preparations are prescribed. Materials and methods In this prospective, multi-centre, observational study, pregnant women suffering from sleep problems were treated with B. pinnatum (350 mg tablets, 50% leaf press juice, Weleda AG, Arlesheim, dosage at physician's consideration). Sleep quality, daily sleepiness and fatigue were assessed with the aid of standardised questionnaires, at the beginning of the treatment and after 2 weeks. Possible adverse drug reactions perceived by the patients during the treatment were recorded. Results The number of wake-ups, as well as the subjective quality of sleep was significantly improved at the end of the treatment with B. pinnatum . The Epworth Sleeping Scale decreased, indicating a decrease of the tiredness during the day. There was, however, no evidence for prolongation of the sleep duration, reduction in the time to fall asleep, as well as change in the Fatigue Severity Scale after B. pinnatum . No serious adverse drug reactions were detected. Conclusion B. pinnatum is a suitable treatment of sleep problems in pregnancy. The data of this study encourage further clinical investigations on the use of B. pinnatum in sleep disorders.

Summary Symptoms of tiredness, lack of muscle co-ordination and dysarthria, and difficulty in maintaining attention in elderly people may be wrongly labelled as part of the ageing process and so ignored. If adequate sleep can reduce these symptoms and restore therapeutic activity, it is of enormous value to elderly people in retaining their independence and quality of life. Safe promotion of sleep without daytime lethargy is needed. In order to test the hypotheses that Essential Oil of Lavender has a sedative effect, and that the resultant sleep promotes therapeutic activity, a pilot study was arranged with acutely ill elderly people. This was followed by a more detailed trial with long-term patients. The results show a positive trend towards improvement with lavender.

Mitragyna speciosa, a plant from Rubiaceae family, was reported to have an opium-like effect and their coca-like stimulative ability to combat fatigue and enhance tolerance to hard work. There are lack of information regarding to the effect of Mitragyna speciosa on cognitive and behavioural performances. Therefore the project was conducted to observe the effect of Mitragyna speciosa on cognitive behavior of rats and mice. Mitragyna speciosa in methanol extract form and aqueous extract form with same dosage distributions were used; 10 mg/kg, 30 mg/kg, and 100 mg/kg. Four tests were conducted to observe the behavioural changes of the animal namely locomotor, cognitive performances, anxiety and rotarod performance. Results showed that all dosage of treatment reduced locomotor and impaired cognitive performance significantly. Study showed that Mitragyna speciosa induce sedative effect in dose dependant manner. Interestingly, Mitragyna speciosa increased the time spent in open arm of plus maze indicating low anxiety level of the rodent. As conclusion, Mitragyna speciosa caused sedative effect, impairment in working memory, and possess anxiolytic properties.

The current study was designed to assess the preliminary antinociceptive, sedative and muscle relaxants activates of crude extract and various solvent fractions of Caralluma tuberculata using established in-vivo protocols. The results illustrated significant (P

Once migraine becomes chronic and has transformed into a form of headache that occurs daily or almost, the treatment options available are few and complex. This makes it important to take action before this point is reached, using all the measures that can be obtained from our current knowledge of chronic migraine (or transformed migraine) on the one hand, and on the potential factors of chronification (or transformation) on the other. Therefore, in order to reduce the risk of migraine chronification, it would appear important to: (a) administer suitable preventive treatments for subjects who have been suffering from migraines ≥4 days a month for ≥3 months; (b) take special care not to overuse symptomatic medications, particularly when they contain substances with a sedative effect; and (c) investigate the concomitant presence of depression, hypertension and excess weight and administer appropriate treatment when present.

In order to investigate the link between aggression and 5-HT, we looked at effects of changes in plasma tryptophan on healthy male subjects. Twenty-four with high trait aggression (H) and 24 with low (L) drank an amino acid mixture with (T+) or without (T-) tryptophan. These caused plasma tryptophan enhancement and depletion, respectively, at 4.5 h. Group H subjects given T- became more angry, aggressive, annoyed, hostile and quarrelsome on subjective measures, whereas those given T+ responded in the opposite way. On a behavioural measure of aggression, group H subjects responded more aggressively after T- than T+. In contrast, there was no consistent effect on subjective or behavioural aggression in group L subjects. Feelings of well-being in group H were decreased by T- and increased by T+. In group L, T+ reduced feelings of well-being, possibly due to the sedative effect of tryptophan in this group, which correlated positively with plasma tryptophan concentration. Changes in plasma tryptophan are probably followed by changes in central 5-HT turnover. We conclude that, in those with pre-existing aggressive traits, acute falls in central 5-HT can cause increased subjective and objective aggression, while rises can have the opposite effect. The absence of changes in a low aggressive group suggests that the primary effect may be on impulsivity, possibly mediated by 5-HT1a receptors, expressing underlying aggressive traits. The findings on mood changes provide support for earlier reports of a lowering of mood with tryptophan depletion.

The present study was carried out to assessing the sedative effect of medetomidine and determining its optimal dose in thoroughbred horses. Excessive ataxia after sedative treatment is dangerous for horses. Therefore three doses which may cause sufficient sedation with only mild ataxia were examined. Response to stimulation and the severity of ataxia suggested that 7.5 micrograms/kg BW, i.v., is optimal.

Twenty great apes (six orangutans, eight chimpanzees and six gorillas) were anaesthetised prior to being transported for undergoing diagnostic and interventional procedures. Anaesthesia was induced with a combination of medetomidine and ketamine administered intramuscularly through a dart syringe. The onset of anaesthesia varied among apes: the mean (±sd) time from darting to recumbency was 12.13 (±1.9), 18.5 (±8.7) and 22.2 (±9.2) minutes in chimpanzees, orangutans and gorillas, respectively. The depth of anaesthesia was sufficient to allow safe removal of the animals from the enclosure, intravenous catheter placement and manipulation; however, the anaesthetic effect was short-acting (20 (±7) minutes in orangutans, 16 (±14) in gorillas, and 10 (±4) minutes in chimpanzees, respectively) and isoflurane administration was necessary in the majority of the apes to prolong the duration of anaesthesia, especially when lengthier procedures were performed. The sedative effect of medetomidine was reversed at the end of each procedure with atipamezole, and recovery was smooth and uneventful for all animals.

Terpinolene is a cyclic monoterpene compound found in some Labiatae herbs. In our previous study, we evaluated the sedative effect of inhaled essential oils of Microtoena patchoulii leaves in mice and isolated terpinolene as an active ingredient. We investigated the structure-activity relationships of terpinolene to identify the structural part essential to its sedative effect. Comparison of terpinolene analog activities showed that a double bond in the side-chain or pi bonds in the six-membered ring play important roles in the sedative effect. In another experiment using olfactory impaired mice, we further revealed that inhaled terpinolene exerted the effect after nasal absorption into the body.

Analgesic activities of Randia siamensis CRAIB (R. siamensis) extract and pseudoginsenoside-RP1, a constituent of the extract, were examined in the writhing test, hot plate test and Randall-Selitto test. Oral administration of R. siamensis extract dose-dependently decreased the number of writhings and stretchings induced by 0.6% acetic acid in the writhing test in mice. Moreover, in the Randall-Selitto test in rats, the extract raised the nociceptive threshold of the carrageenan-inflamed but not of non-inflamed paw. It did not affect the nociceptive response in the hot plate test in mice. The R. siamensis extract did not affect hexobarbital-induced sleep or spontaneous motor activity in mice, suggesting that it has no sedative effect. Pseudoginsenoside-RP1 produced similar effects to the R. siamensis extract, but its effective doses in the analgesic tests were lower than those with the extract. These results suggest that R. siamensis extract produces anti-nociceptive actions similar to those of a peripherally acting analgesic drug aspirin, and that pseudoginsenoside-RP1 may partly contribute, but is not the main contributor, to the antinociceptive action of the extract.

The acute effects of DX-9386, a traditional Chinese medicinal preparation (ginseng, polygala, acorus and hoelen), were studied on learning and memory performances in passive and active avoidance tests in normal, as well as in learning-impaired, mice. A single oral administration of the prescription had no effect on memory registration, consolidation or retrieval or on motor activity in normal mice. DX-9386 reduced the ethanol-induced impairment of memory registration in the step-down test and also tended to ameliorate the scopolamine-induced memory registration deficit in the same test. The preparation reduced the number of spontaneous responses in the active avoidance test. The preparation also prolonged the disappearance of righting reflex induced by pentobarbital. These results suggest that DX-9386 ameliorates the impairment effect of ethanol on learning and memory processes and also exhibits a sedative effect.

We evaluate the sedative and hypnotic activities of the methanolic and aqueous extract ofLavandula officinalisL. on central nervous system (CNS). In this study, the effect of the methanolic and aqueous extracts of this plant was investigated in a battery of behavioural models in mice. Stems and flowers ofLavandula officinalisL. have several therapeutic applications in folk medicine in curing or managing a wide range of diseases, including insomnia. The methanolic extract produced significant sedative effect at the doses of 200, 400, and 600 mg/kg (by oral route), compared to reference substance diazepam (DZP), and an hypnotic effect at the doses of 800 and 1000 mg/kg while the treatment of mice with the aqueous extract at the doses of 200 and 400 mg/kg via oral pathway significantly reduced in both the reestablishment time and number of head dips during the traction and hole-board tests. In conclusion, these results suggest that the methanolic and aqueous extracts ofLavandula officinalispossess potent sedative and hypnotic activities, which supported its therapeutic use for insomnia.

For tens of centuries, plants have been highly valued and regularly used as medicine amongst the masses. Insomnia, a loss of sleep, is mostly treated by synthetic sleeping tablets these days. However, questions have been raised about the safety of prolonged use of artificial sedatives due to their deleterious side effects such as physical dependence. In recent years, there has been an increasing propensity to preclude insomnia by herbal medicines throughout the world. Many herbs have a lengthy background in terms of insomnia treatment in Iran. This paper gives an account of previously published research on sedative and hypnotic effects of medicinal herbs used for treatment of insomnia in Iranian traditional medicine.

Publisher Summary This chapter highlights the nutritional and therapeutic effects of sour date. Sour date, or Semen ziziphi spinosae, is an excellent natural and safe “sedative” herb. In Chinese medicine, this herb nourishes the two organs responsible for sleep, the liver and heart. When balance is brought back to these organs, then sleep occurs naturally. Semen ziziphi spinosae is the main ingredient of the formula of ancient Chinese medicine, which is used for the treatment of deficiency and insomnia. The actions of the formula are to nourish the blood, clear heat, relieve restlessness, and treat insomnia. According to ancient prescriptions and theories, both raw and prepared Semen ziziphi spinosae can work as a natural herb for insomnia. Clinical practice has shown that the efficacy of these raw or prepared natural herbs is not opposing. Laboratory animal studies of Semen ziziphi spinosae extract confirm a sedative effect, though the constituents that contribute to this effect have not all been specifically identified. Semen ziziphi spinosae is reported to have very low toxicity when taken orally. In laboratory animals, a huge single dose of 50 g/kg body weight produced no toxic symptoms, and a daily dose of 20 g/kg for 30 days did not produce toxic reactions. Side effects have not been reported.

Objective: To evaluate a small dosage of Tenon's capsule anaesthesia as a less invasive substitute for retrobulbar anaesthesia in cataract surgery and intraocular lens (IOL) implantation. Study Design: Replacing the retrobulbar anaesthetic technique with the Tenon's capsule anaesthetic technique from April 1990. Setting: The Jikei University School of Medicine Department of Ophthalmology. Patients: Over 1500 patients requiring cataract surgery were given the Tenon's capsule method of anaesthesia. Main Outcome Measures: To show that complications attributable to retrobulbar anaesthesia would be less frequent with the Tenon's capsule method. Results: There is no suppression of ocular motility and no pain caused by the anaesthesia. Neither is there an elevation of blood pressure or arrhythmia. There are no complications either in the method of anaesthesia, or in the surgery. There is a definite sedative effect obtained with a small dosage (0.5–1.0 cc), and this effect is prolonged for 60 minutes or longer. Conclusion: Tenon's capsule anaesthesia is a very useful substitute for conventional retrobulbar anaesthesia, and is easy for inexperienced surgeons to use.

A variety of new title aminoethylquinazolinedione derivatives having structural similarities to the 4-hydroxy-2-quinolinone anesthetic chinoxicaine are synthesized and evaluated for their anesthesia penetration, motor block and sedative effect compared to chinoxicaine and lidocaine.

This study aimed at evaluating the reactivity of L-Tryptophan (TRP) 1 towards various chemical reagents to produce new bi- and tri-heterocyclic systems providing basic pharmacological activities. Indol-3-yl hydroxyoxazol-2-yl acetonitrile derivatives 5 and 6, indol-3-yl-hydroxyoxazol-2-yl-1,2,4-triazine derivatives 8 and 9, indol-3-yl-hydroxyoxazol-2-yl-aminopyrazole derivatives 11a, b, and indol-3-yl-hydroxyoxazol-2-yl-aminoisoxazole derivative 12 were synthesized via straightforward and efficient methods. The structures were characterized by spectral data (IR, (1)H-NMR, (13)C-NMR, and MS) and the purity was ascertained by microanalysis. Also, this work was extended to study the potential role of the novel synthesized TRP derivatives 5, 6, 9, 11a, and 12 as antidepressant and sedative agents in comparison with TRP. All compounds showed significant antidepressant activity in the forced-swimming test at two doses (50 or 100 mg/kg). Also, all tested compounds (at 50 or 100 mg/kg) produced a significant decrease in locomotor activity of mice during a 30 min observation period. The most potent antidepressant and sedative effect was produced by the tri-heterocyclic compounds 9 and 12, followed by 11a and TRP.

A series of 7-(2,2-dimethyl)propyl substituted xanthines were synthesized and tested for their antibronchospastic activity in comparison with theophylline. In vitro, the inhibition of carbachol-induced increase in bronchial tone was determined. In vivo, the inhibition of antigen-induced bronchoconstriction in guinea pigs was determined 1, 3 and 5 h after oral administration. Central side effects were evaluated. In vitro, the majority of compounds were more effective than theophylline. In vivo, three compounds 2, 14 and 15 showed an effect comparable to theophylline but longer lasting. A mild sedative effect was generally observed. Compound 2, 7-(2,2-dimethyl)propyl-1-methyl xanthine, coded MX2/120, was selected for a deeper evaluation.