CNS Depressant Activity Research Articles

Effect of Alcoholic Extract of Stem Bark of Anamirta cocculus Willd on Central Nervous System

Anamirta cocculus Willd is a well known medicinal plant belonging to the family Menispermaceae. Its ethanolic extract was evaluated for locomotor activity, analgesic activity and muscle relaxant activity. The rotarod apparatus was used for evaluation of muscle relaxant activity. The extract showed significant decrease in fall off time which indicated that it has CNS depressant activity when compared with diazepam. Photoactometer was used to study of locomotor activity in mice. The effects were found to be dose dependent statistically significant when compared with control groups. Hot plate was used to study of analgesic activity of extract. The reaction time was increased in the extract treated groups than that of morphine as standard drug. The antipyretic activity of extract was investigated experimental rats. The antipyretic was retained in all the dose of extract tested was comparable to that of paracetamol as standard drug.

Anti-inflammatory and Neuropharmacological activities of the seed extract of Setaria italica

Setaria italica (Poaceae) has been used in folk medicine to treat inflammation, pain, arthralgia and many neurological disorders. The objective of the study is screening of ethanolic extract of Setaria italica seeds for possible anti-inflammatory and neuropharmacological activities in rats and mice respectively. Antiinflammatory activity was evaluated by carrageenan induced paw edema inhibition method while the neuropharmacological potential was evaluated by three separate methods: Hole-cross test, Open-field method and Phenobarbitone induced sleeping time test. The crude ethanolic extract of seeds of Setaria italica at 400 mg/kg body weight showed a strong anti-inflammatory activity with 20.16, 65.44, 65.5 and 71.15% inhibition of paw edema respectively after 1 st , 2 nd , 3 rd and 4 th hrs of carrageenan injection which is comparable to that of standard drug diclofenac sodium at 100 mg/kg body weight (% inhibition 92.3% at 4 th hour **P<0.001). In Hole-cross test, ethanolic extracts of Setaria italica at 400 mg/kg body weight dose have prominent CNS depressant activity which is comparable to standard Diazepam. In open field test, S. italica at 400 mg/kg body weight significantly suppressed the movements which is comparable to standard Diazepam. In Phenobarbitone induced test, Setaria italica did not show any significant CNS-depressant activity. The findings of the studies demonstrate anti-inflammatory and neuropharmacological properties of Setaria italica which could be therapeutic option against inflammation and neurological disorders.

Analgesic and Neuropharmacological Activities of Methanol Extract from the Leaf of Nicotiana plumbaginifolia Viv.

The aim of study was to evaluate the analgesic and neuropharmacological activities of the leaf of Nicotiana plumbaginifolia. The central analgesic activity of the methanolic extract was evaluated in Swiss Albino mice by using tail immersion, hot plate and acetic acid-induced writhing tests at 100, 200 and 400 mg/kg body weight. These tests showed significant analgesic activity of the extract compared to the standard drug, diclofenac-Na (1 mg/kg b.w.). The neuropharmacological activities were evaluated using hole cross, open field, light/dark box and elevated plus maze stage tests in mice model at 100, 200 and 400 mg/kg body weight. The results of neuropharmacological assays demonstrated potential CNS depressant activity of the extract when compared to the standard drug, diazepam (1 mg/kg b.w.)Bangladesh Pharmaceutical Journal 18(2): 85-89, 2015

A one-pot synthesis of indole-appended heterocycles as potent anti-inflammatory, analgesic, and CNS depressant agents

A series of novel 3-[3-(2,5-dichloro-3-thienyl)-substituted-1H-pyrazol-5-yl]-2,5-disubstituted-1H-indoles, 3-[3-(2,5-dichloro-3-thienyl)isoxazol-5-yl]-2,5-disubstituted-1H-indoles, and 4-(2,5-dichloro-3-thienyl)-6-(2,5-disubstituted-1H-indol-3-yl)-substituted pyrimidin-2(5H)-ones were synthesized by means of a one-pot reaction. Structures of all compounds were confirmed by their melting points, elemental analysis, IR, 1H NMR, 13C NMR, and mass spectral data. The novel compounds were evaluated for pharmacological studies and discussed in terms of their structural differences. Among the screened compounds, three show excellent anti-inflammatory activity with maximum inhibition (50.0–59.1 %), i.e. better than the standard drug indomethacin (50.0 %). Four of the compounds revealed highest analgesic potency. In locomotor activity, six compounds exhibited promising results for CNS depressant activity.

Synthesis, Biological Activity, and Docking Study of Novel Isatin Coupled Thiazolidin-4-one Derivatives as Anticonvulsants.

A series of 2-(substituted-phenyl)-3-(2-oxoindolin-3-ylidene)amino)-thiazolidin-4-one derivatives were designed and synthesized under microwave irradiation, using an eco-friendly, efficient, microwave-assisted synthetic protocol that involves cyclocondensation of 3-substituted benzylidine-hydrazono-indolin-2-one 3a-j with thioglycolic acid in dimethyl formamide (DMF) as solvent and anhydrous zinc chloride as a catalyst, keeping in view the structural requirement of the pharmacophore. The intermediate compounds 3a-j were obtained by condensation of the hydrazone of indoline-2,3-dione with aromatic aldehydes. The synthesized derivatives were evaluated for CNS depressant activity and anticonvulsant activity in mice using the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (sc-PTZ) induced seizure tests. All the derivatives showed good CNS depressant activity and showed protection in the MES test, indicative of their ability to inhibit the seizure spread. A histopathological study was performed to evaluate liver toxicity caused by the synthesized compounds. The compounds were nontoxic. A computational study was performed, in which log P values were calculated experimentally. Virtual screening was performed by molecular docking of the designed compounds into the ATP binding sites of the NMDA and AMPA receptors, to predict if these compounds have analogous binding modes.

In vivo analgesic and CNS depressant activities of antioxidative stem bark fraction of Morus alba L.

Abstract not available DOI: http://dx.doi.org/10.3329/dujps.v13i2.21905 Dhaka Univ. J. Pharm. Sci. 13(2): 225-227, 2014 (December)

Evaluation of Analgesic and CNS Depressant Activities of Grewia Paniculata in Swiss albino Mice

Grewia paniculata (Family: Malvaceae) used to treat inflammation, pain, fever, wounds and also in psychological disorders. The present study was designed to investigate the analgesic and CNS depressant activities of different crude extract of Grewia paniculata. The analgesic activity was evaluated by using acetic-acid induced writhing, hot plate and tail immersion tests and the CNS depressant activity was examined by observing the reduction of locomotor and exploratory activities in the thiopental induced sleeping time, hole cross and open field tests in mice at the doses of 250 and 500 mg/kg, b.w. For analgesic and CNS depressant activity Diclofenac sodium (25 mg/kg i.p), Aspirin (100 mg/kg p.o), Morphine (5 mg/kg i.p) and Diazepam (1 mg/kg i.p) were used as reference drug, respectively. All the extract displayed significant analgesic effect (P<0.05-0.001) in acetic acid and heat induced pain models in a dose dependent manner. The extract prolonged the latency period to the thermal stimuli in both hot plate and tail immersion test. The spontaneous motor activity was decreased by (P<0.001) by all natural products in both hole cross and open field test. Statistical studies revealed that all the extracts prolong the duration of the thiopental sodium induced sleeping time in mice. Altogether, these results suggest that all the extracts of Grewia paniculata possesses potent analgesic and CNS depressant properties, which support its use in traditional medicine and suggesting that the plant should be further investigated for its pharmacological active natural products.

Bioactive Polyphenols from the Methanol Extract ofCnicus arvensis(L.) Roth Demonstrated Antinociceptive and Central Nervous System Depressant Activities in Mice

Cnicus arvensis is used by many ethnic groups for inflammation, pain, and other ailments. In this study, reducing sugar, carbohydrate, alkaloid, steroid, tannin, flavonoid, and saponin groups were identified using standard chromogenic method. In high-performance liquid chromatography, vanillic acid and epicatechin were identified in the extract. Antinociceptive test by acetic acid induced writhing inhibition resulted 43.17 and 95.08% inhibition for 100 and 200 mg/kg body weight, comparing with standard diclofenac Na with 74.86% inhibition for 25 mg/kg body weight. In formalin induced paw licking test for antinociceptive activity, the extract inhibited 69.87 and 75.55% licking for 150 and 300 mg/kg body weight comparing with the inhibition (68.56%) of diclofenac Na for 10 mg/kg body weight at first phase. At late phase, the extract showed 73.12 and 87.46% licking comparing with licking inhibition (71.69%) by diclofenac Na at the same dose. In open field test for CNS depressant activity, the extract showed depression of locomotor activity for 150 and 300 mg/kg body weight comparing with diazepam for 10 mg/kg body weight. All results were statistically significant (P < 0.01). The identified polyphenols are reputed for antinociceptive and CNS depressant activity. The present findings support the use of this plant in pain.

Pharmacological investigation of selected medicinal plants of Bangladesh

Purpose: To pharmacologically investigate the methanol and petroleum ether extracts of the plant leaves of Manilkara zapota (MZME and MZPE, respectively), Abroma augusta (AAME and AAPE, respectively) and Vitex negundo (VNME and VNPE, respectively).Methods: Analgesic and anti-diarrheal activities were assessed by acetic acid-induced writhing and castor oil-induced diarrhea in mice, respectively, while CNS depressant activity was evaluated using hole-cross and open-field method by observing the decrease in exploratory behavior and spontaneous motor activity in mice, respectively.Results: All the extracts exhibited good analgesic activity at a dose of 200 mg/kg with the following rank order of activity: MZME &gt; MZPE &gt; VNME &gt; VNPE &gt; AAME &gt; AAPE. Analgesic activity was insignificant at 100 mg/kg dose except for VNPE (67.81 % inhibition). The extracts produced significant reduction in diarrheal episodes in mice at a dose of 400 mg/kg MZPE (highest protection: 80.3 %, p &lt; 0.05) and VNME (lowest protection: 38.6 %, p &lt; 0.001). The extracts demonstrated CNS depressant activity in a dose-dependent manner (p &lt; 0.05 compared to the standard except for AAME and AAPE which showed insignificant activity).Conclusion: The results indicate that the traditional use of the investigated plants appears to be justified; however, further studies are required to unravel the underlying mechanisms of action.Keywords: Manilkara zapota, Abroma augusta, Vitex negundo, Analgesic, Central nervous system depressant, Anti-diarrhoeal

Design, Synthesis and Screening of Newer-8-Hydroxy Quinoline Derivatives as Novel Anti Tubercular Agents

A series of 8-hydroxyquinolines are synthesized and their Antitubercular, antifungal, and antibacterial activities are tested. Quinolines are found to possess antibacterial, antifungal, immunosuppressive, analgesic, vasorelaxing, Antiplasmodial, anticancer and PDE4 inhibitory activities. Aryloxypropanolamines were reported to be associated with β-adrenergic blocking, CNS depressant and hypotensive activities. In view of the potential nature of these moieties it was considered worthwhile to study the effects of two pharmacophoric moieties such as quinoline and propanolamines/amino ethane in a single molecule. In the present study the synthesis, antitubercular, antifungal, and antibacterial activities and structure activity relationship of aryloxypropanolamine substituted 8-hydroxy quinolines are reported. The compounds were characterized by IR, H-NMR, spectral and Elemental analysis. DOI: http://dx.doi.org/10.3126/ijasbt.v2i3.11100Int J Appl Sci Biotechnol, Vol. 2(3): 342-358

Pharmacological Potentials of Sea Cucumber Holothuria atra Extracts from the Indian Ocean

Drugs derived from marine organisms are currently used to cure infectious diseases. Marine invertebrates collected from the intertidal regions of the Indian coast have shown promising biological activities. Sea cucumbers are soft-bodied worm-like echinoderms which belong to the class Holothuroidae. Anti inflammatory activity was detected using Carrageenan induced rat paw edema method. The analgesic activity was performed using tail immersion method. Antipyretic activity was analysed using Brewer’s yeast induced hyperpyrexia method.CNS was determined using Locomotor activity. Immunomodulatory activity was tested using Carbon clearance test. Antioxidant activity was measured using DPPH method. Pharmacological studies showed that the anti inflammatory bustle of methanol extracts in Holothuria atra at the concentration of 100 and 200 mg/kg, p.o on rats showed significant decrease in the paw thickness in a dose dependent manner when compared to that of the control, at the 5th hour of administration. Similarly the highest inhibition rate seen in H. atra extracts was 84% showed analgesic activity. Then antipyretic, immunomodulatory and CNS depressant activities were found to be moderate. The methanol extract of H.atra showed high antioxidant activity with IC50 value of 300. Overall results provide information that sea cucumber H. atra could be explored as a potential source of high-value bioactive metabolites and could be used in the pharmaceutical industry.

Evaluation of analgesic, anti-inflammatory and CNS depressant activities of methanolic extract of Lawsonia inermis barks in mice.

The study was carried out to assess the analgesic, anti-inflammatory, and CNS depressant activity of the methanolic extract of the Lawsonia inermis barks (MELIB). Anti-inflammatory effects of MEBLI were studied using carrageenan-induced inflammatory method at the dose of 300 and 500 mg/kg b.wt., p.o. Analgesic activity was measured using acetic acid-induced writhing model and formalin-induced licking and biting in mice. The CNS depressant activity was evaluated by observing the reduction of locomotor and exploratory activities in the open field and hole cross tests at a dose of 300 and 500 mg/kg body weight. Statistical analysis showed that dose of 500 mg/kg exhibited higher analgesic activity against acetic acid-induced pain in mice than the standard drug diclofenac sodium. Furthermore, doses of 300 and 500 mg/kg caused higher percent of protection (91.16% and 95.03%, respectively) of licking and biting of formalin-induced mice than diclophenac sodium (70.72%). The Lawsonia inemis methanolic extract (300 and 500 mg/kg) also exhibited sustained inhibition (54.97% and 65.56%) of paw edema at the 4(th) hour compared with standard indomethacin (74.17%). Besides, the plant extract also had significant (p<0.05) dose-dependent CNS depressant activity. this study recommends that the methanolic extract of Lawsonia inermis barks has significant analgesic, anti-inflammatory, and CNS depressant properties.

Membrane stabilizing, thrombolytic, analgesic, anti-diarrheal and CNS activities of Polyalthia longifolia (Sonn.)

Different fractions of Polialthia longifolia (Sonn.) bark were evaluated for membrane stabilizing, thrombolytic, analgesic, anti-diarrheal and CNS de-pressant activities upon oral administration at 200 and 400 mg/kg body weight. The membrane stabilizing activity was assessed by heat and hypo-tonic solution. Carbon tetrachloride fraction of methanol extract of P. longi-folia bark demonstrated strong membrane stabilizing activity, while the crude methanol extract demonstrated mild to moderate thrombolytic activi-ty in human blood specimen. The analgesic activity was assessed by tail im-mersion and formalin-induced pain method in Swiss-albino mice. The crude methanol extract of P. longifolia bark exhibited significant peripheral and central analgesic activity, since inhibited chemical induced writhing at 200 mg/kg and increased tail flick latency time both at 200 and 400 mg/kg. The anti-diarrheal activity of the bark extract was assessed by using castor oil induced diarrhea in mice however significant anti-diarrheal activity was not revealed. The CNS inhibitory activity of the methanol extract was assessed in Swiss albino mice where it reduced phenobarbitone sodium induced sleep-ing time at 400 mg/kg.

ANTIOXIDANT, ANTHELMINTIC AND ENZYME INHIBITORY POTENTIAL OF STREPTOMYCES VARIABILIS STRAIN PO-178 ISOLATED FROM WESTERN GHAT SOIL OF AGUMBE, KARNATAKA, INDIA

INTRODUCTION Among various ecological habitats, soil is one of the richest reservoirs supporting a variety of organisms including microorganisms. Rhizosphere is the region of soil present in vicinity to plant roots and is influenced by secretions of plant roots called root exudates. This region is thought to be of great importance to plant health and soil fertility. The exudates from plant roots stimulate the growth of microbial populations in soil and thus, the microbial activity is greatest in rhizosphere region. Actinomycetes forms a key part of soil microorganisms. The species of the genus Streptomyces are saprophytic and are commonly associated with soils. It has been found that about 90 % of soil actinomycetes are reported to be Streptomyces species. In soil, Streptomyces species significantly contribute to the turnover of complex biopolymers such as cellulose, pectin, lignin etc. They are noteworthy as they are the prolific producers to a range of bioactive metabolites including antibiotics. Western Ghats of India covers an area of 1, 80, 000 km and represent just under 6 % of the land area of India. The area represents > 30 % of all plant, fish, herpeto-fauna, birds and mammal species found in India which include some of the globally threatened species. Agumbe, a region of Western Ghats of Shivamogga district, Karnataka, India is shown to be a rich reservoir for Streptomyces species having potent industrial and agricultural significance in terms of production of bioactive metabolites. Streptomyces species from Agumbe region of Western Ghats have shown to antimicrobial, antioxidant, enzyme inhibitory, insecticidal, cytotoxic, anthelmintic, analgesic, antiinflammatory, CNS depressant and antipyretic activities. Streptomyces variabilis strain PO-178 (Figure 1) of this study was isolated from a rhizosphere soil of Agumbe, Karnataka, India. The extract from this strain was shown to possess antimicrobial, insecticidal, cytotoxic, analgesic, antiinflammatory, antipyretic and CNS depressant activity. In continuation part of our previous study, the present study was conducted with an aim of determining antioxidant, anthelmintic and enzyme inhibitory activity of butanol extract of S.variabilis PO-178 isolated from rhizosphere soil of Agumbe, Karnataka, India.

Analgesic, Anti-inflammatory and CNS Depressant Activities of the Methanolic Extract of Abelmoschus esculentus Linn. Seed in Mice

Aims: The study was carried out to assess the analgesic, anti-inflammatory and CNS depressant activity of the methanolic extract of Abelmoschus esculentus Linn. Seeds. Study Design: The Present study was designed to observe pharmacological activities of the crude extract of the plant Abelmoschus esculentus seeds. The study consisted of hot extraction of the seeds of the A. esculantus with methanol. Afterwards, Methanolic crude extract was filtered and the filtrate was evaporated. Finally, screening of analgesic, anti-inflammatory and CNS depressant activity of crude extracts of A. esculantus on Swiss Albino mice. Place and Duration of Study: Department of Pharmacy, Atish Dipankar University of Science and Technology, Dhaka, Bangladesh. January, 2013- July 2013. Methodology: The animals are divided into Four groups and each group consists of five mice. Analgesic activity was performed by acetic acid-induced writhing model and formalin induced licking and biting in mice. Anti-inflammatory effects of Abelmoschus esculentus seed extract were done by carrageenan induced anti-inflammatory method at the dose of 100 and 200 mg/kg b.wt., (p.o). The CNS depressant activity was evaluated by observing the reduction of locomotor and exploratory activities in the hole cross and opens field tests at the dose of 100 and 200 mg/kg body weight. Results: In statistical analysis, the dose (200 mg/kg) was found to exhibit (significant p=0.05) better analgesic activity (65.16% and 54.38%) against both acetic acid and formalin induced pain in mice which is about similar to standard drug Indomethacin. The extract of A. esculentus (100 and 200mg/kg) also showed sustained inhibition (54.97% and 65.56%) of paw edema at the 4th hour compared to Indomethacin (74.17%). Besides this A. esculentus (significant p=0.05) seed extract (100 and 200mg/kg p.o.) also possesses depressant activity at 90min in both methods. Conclusion: this study recommends that the methanolic extract of the Abelmoschus esculentus seeds has significant CNS depressant, analgesic and anti-inflammatory properties.

Anticonvulsant and Depressant Activity of Methanol Leaf Extract of Croton zambesicus

Aims: To study anticonvulsant and central nervous system depressant activity of methanol leaf extract of Croton zambesicus (MECZ) in Swiss albino mice and investigate the role of serotonin in these activities. Methodology: Anticonvulsant activity of graded doses (200, 300 and 400 mg/kg p.o) of MECZ was assessed through seizures induced by picrotoxin and pentylenetetrazole (PTZ). Effects of the extract on pentobarbitone-induced sleep and amphetamine-induced stereotype behavior were also evaluated. Possible involvement of serotonergic pathways was studied using cyproheptadine (4mg/kg i.p), a non-selective serotonin antagonist (5HT1/5HT2). Results: In both picrotoxin and PTZ-induced seizures, the extract significantly delayed onset of seizure (p<0.05) in a dose-dependent manner and provided significant protection against death. There was a dose-dependent increase of pentobarbitone sleeping time and a significant reduction (p<0.05) in the sleep latency. The extract also produced a significant reduction in amphetamine-induced stereotype behavior. Pretreatment with cyproheptadine abolished the anticonvulsant effect of the extract. The inhibitory effect of the extract on amphetamine-induced hyperactivity and its potentiation of pentobarbitoneinduced sleep were also reversed by cyproheptadine. Conclusion: The results of this study showed that methanol extract of Croton zambesicus leaf possesses anticonvulsant activity and other CNS depressant activities and these activities are possibly mediated through interaction between serotonergic and GABAergic transmissions. Research Article

Sedative-Hypnotic Like Effect of the Essential Oil from the Leaves of Myrtus Communis on Mice

Myrtus communis has been recommended for relief of insomnia in Ethiopian traditional medicine and aromatherapy. However, no pharmacological studies have yet evaluated its sedative-hypnotic like effect. The aim of this study was to determine if the essential oil of Myrtus communis has sedative-hypnotic like activity. The essential oil of Myrtus communis (500,600, 800, and 1000 mg/kg) were administered orally to Swiss albino mice of both sex, 60 minutes before pentobarbital injection (50 mg/kg). Latency to sleep and sleep duration were recorded. More over the effect of the EO on motor-coordination and muscle relaxation were evaluated using Chimney and Traction test 60 and 90 min after administration of the respective doses of the EO respectively. The essential oil prolonged pentobarbital-induced sleeping time at 600, 800 (comparable to diazepam 3mg/kg), and at 1000 mg/kg compared to vehicle-treated group. The 50% negative response was observed on the Chimney and Traction test at 800 and 1000mg/kg respectively. The essential oil of Myrtus communis possesses dose dependent sedative-hypnotic like activity and CNS depressant activity.

Holoptelea integrifolia (Roxb.) Planch: a review of its ethnobotany, pharmacology, and phytochemistry.

Holoptelea integrifolia (Ulmaceae) is a versatile medicinal plant used in various indigenous systems of medicine for curing routine healthcare maladies. It is traditionally used in the treatment and prevention of several ailments like leprosy, inflammation, rickets, leucoderma, scabies, rheumatism, ringworm, eczema, malaria, intestinal cancer, and chronic wounds. In vitro and in vivo pharmacological investigations on crude extracts and isolated compounds showed antibacterial, antifungal, analgesic, antioxidant, anti-inflammatory, anthelmintic, antidiabetic, antidiarrhoeal, adaptogenic, anticancer, wound healing, hepatoprotective, larvicidal, antiemetic, CNS depressant, and hypolipidemic activities. Phytochemical analysis showed the presence of terpenoids, sterols, saponins, tannins, proteins, carbohydrates, alkaloids, phenols, flavonoids, glycosides, and quinines. Numerous compounds including Holoptelin-A, Holoptelin-B, friedlin, epifriedlin, β-amyrin, stigmasterol, β-sitosterol, 1, 4-napthalenedione, betulin, betulinic acid, hexacosanol, and octacosanol have been identified and isolated from the plant species. The results of several studies indicated that H. integrifolia may be used as an effective therapeutic remedy in the prevention and treatment of various ailments. However, further studies on chemical constituents and their mechanisms in exhibiting certain biological activities are needed. In addition, study on the toxicity of the crude extracts and the compounds isolated from this plant should be assessed to ensure their eligibility to be used as source of modern medicines.

Central nervous system activity of an aqueous acetonic extract of Ficus carica L. in mice.

Background:Ficus carica Linn. is reported to possess variety of activities, but its potential in CNS disorders is still to be explored.Objective:The present study was carried out to evaluate the CNS depressant activity of aqueous acetonic extract of Ficus carica Linn on different models in mice.Materials and Methods:The aerial parts of the plant Ficus carica L. were extracted with aqueous acetone and the solvent was removed by rotary vacuum evaporator under reduced pressure. A crude extract was given orally and its effects were tested on ketamine-induced sleeping time, muscle-coordination, anxiety (elevated-plus maze and Staircase test), convulsions [maximal electroshock (MES) and pentylenetetrazole (PTZ)-induced seizures], and nociception. In addition, we determined the levels of neurotransmitters, norepinephrine (NE) and 5-hydroxytryptamine (5-HT).Results:Results from the experimental models tested showed: (1) a delay on onset and prolongation of sleep of ketamine-induced sleeping time; (2) significant muscle relaxant activity; (3) a significant attenuation in the anxiety-response (4) a delay in the onset of seizures and reduction in duration of seizures and mortality induced by MES and PTZ; (5) a reduction in the licking time in nociception test and (6) increased levels of NE and 5-HT.Conclusion:This suggests that Ficus carica L. exerts its CNS depressive effect by modulating the neurotransmitters NE and 5-HT in the brain.

Synthesis and Biological Screening of New Derivatives of 2,3-dihydro quinazolin-4(1H)-one and Benzotriazepin- 5(2H)-one for Central Nervous System Activity

A new syntheses of novel series of 2,3-dihydroquinazolin-4(1H)-one and benzotriazepin- 5(2H)-one derivatives, starting from the same intermediate (IIa-g). By varying the substituent on the benzamide moiety of the key intermediate (IIa-g) or the conditions of the reactions utilized in this syntheses, the reaction gives rise either quinazolin-4(1H)-one or benzotriazepine-5(2H)-one. The intermediate; 2-methylamino-N-(substituted benzoyl)benzohydrazide (IIa-g); was prepared by condensation of N-methyl-isatoic anhydride with different benzoic acid hydrazides. Constructing the intermediates (IIa-g) on different cyclo-condensation reactions; either with ethylchloroformate /potassium hydroxide or carbon disulfide/potassium hydroxide, yielded a new series of benzotriazepin-5(2H)-one (IIIa-b, IVa-d) and a new series of quinazolin4(1H)-one (Va-c, VI a-d). Pharmacological screening of the new benzotriazepinone derivatives revealed that the compounds (VI a-b, IVc-d) exhibited strong CNS depressant activity over clozapine while compounds (VIa,IVc) showed the same antipsychotic activity as clozapine with an observed neurotoxicity.