• Toxicological Research
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• v.11 no.1
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• pp.63-68
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• 1995

N-methyl-D-aspartate(NMDA) receptor has been well known as an important mediator of several forms of neural and behavioral plasticity. But different results were reported about the effect of MK-801 or dextromethorphan on opioid dependence. The present studies examined whether NMDA receptor antagonists can alter the opioid dependence and tolerance in rodents. Naloxone precipitated withdrawal symptoms and changes of locomotor activities were observed in MK-801 or dextromethorphan pretreated morphine-dependent rats. Tail-flick assay was used for morphine analgesia and tolerance was found after 4 day's consecutive injections (10 mg/kg, s.c., twice/day) of morphine in mice. Locomotor activity was increased and the withdrawal symptoms were decreased by the pretreatment of MK-801 in morphine-dependent rats. But 0.3 mg/kg i.p. of MK-801 intensified the body weight loss and produced severe ataxia and rotation although some withdrawal signs were attenuated. Morphine induced analgesic tolerance was inhibited by the pretreatment of MK-801 and dextromethorphan. Dextromethorphan was more potent than MK-801 in inhibiting the development of the analgesic tolerance in mice. These results suggest that NMDA system may be involved in opioid withdrawal and analgesic tolerance but appropriate caution should be requested when MK-801 is used in combination with opioid because of untoward neurologic signs.

• Advances in Traditional Medicine
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• v.9 no.4
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• pp.315-319
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• 2009

In present study evaluate the analgesic and anti-inflammatory activity of the compound obtained from the petroleum ether (40 - 60$^{\circ}C$) extract of the fruits from Dregea volubilis in Swiss albino mice and in Wister albino rats respectively. Dried and crushed fruits of Dregea volubilis were extracted by petroleum ether (40 - 60$^{\circ}C$), the proper solvent system was developed by TLC and subjected to column chromatography for obtaining the pure compound/s. IR, MASS, NMR (PMR, C13 NMR and DEPT) spectroscopic analysis were done to elucidate the structure of the compound/s. The petroleum ether (40 - 60$^{\circ}C$) extract of the fruits of Dregea volubilis led to isolation of a pentacyclic triterpenoid designated as taraxerone and characterized as D- friedoolean- 14- en, 3 one. Taraxerone had been screened for analgesic activity in Swiss albino mice and anti-inflammatory activity in Wister albino rats at the dose of 5 mg/kg body weight orally and exhibit significant analgesic and anti-inflammatory properties.

• Korean Journal of Pharmacognosy
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• v.30 no.2
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• pp.137-144
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• 1999

Torilin was isolated from haxane fraction of Torilis Fructus extract. Torilin produced inhibition of the acetic acid-induced and phenylquinone-induced writhing syndrome at the oral doses of 30 and 90 mg/kg in mice. It also increased the pain threshold at the oral doses of 30, 90 and 270 mg/kg in the tail pressure method and the Randall-Selitto method. However, it did not show a hypothermic action at the oral doses of 30 and 90 mg/kg in mice. The compound exhibited strong anticarrageenan activity at the oral doses of 90 and 270 mg/kg in rats, and had inhibitory effect on the vascular permeability at the oral doses of 30 and 90 mg/kg in mice. It also showed potent inhibition of leucocyte emigration in CMC-pouch at the doses of 3 and 9 mg/rat, sc. The acute toxicity of torilin was very weak: the $LD_{50}$ values were more than 5000 mg/kg, po and 2000 mg/kg, ip in mice. From the above mentioned results, it was suggested that torilin had potent analgesic and anti-inflammatory activities.

• Natural Product Sciences
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• v.9 no.1
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• pp.10-12
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• 2003

In the present study, dikamali resin (obtained from the leaf buds and the young shoots of Gardenia gummifera Linn.) was extracted with diethyl ether and the extract was vacuum dried. Qualitative tests confirmed the presence of flavonoids and free phenolic compounds in the extract. The antioxidant property (qualitative) of the extract was performed by TLC method $({\beta}-carotene-linoleate method)$. The $LD_{50}$ of the extract was found to be 2227 mg/kg by Karber's arithmetic method. The extract was screened for analgesic, anti-inflammatory, antipyretic (100, 200 and 400 mg/kg) and anthelmintic (0.1,0.2 and 0.5%w/v) activities by standard methods. The extract exhibited antioxidant property and prevented oxidation of ${\beta}-carotene$. The extract exhibited significant graded dose response for analgesic, anti-inflammatory, antipyretic and anthelmintic activities. The extract caused the death of earthworms in all experimental concentration whereas the standard drug (piperazine) only effected paralysis. The present study proved the claims of dikamali resin mentioned in the Indian system of medicine.

• Journal of the Korean Chemical Society
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• v.57 no.6
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• pp.755-760
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• 2013

The present study is synthesis of derivatives of N'-(4-amino-5-sulfanyl-4H-1,2,4-triazole-3-yl)-2-(1H-benzimidazole-2-ylsulfanyl) acetohydrazide (IV). Antibacterial activity tested against the E. coli and A. Substilis. Biological activities conducted by disc diffusion method. Compound $2MB_1$, $2MB_3$, $2MB_5$ inhibit the appreciable microbial growth while rest of the compound possess the moderate activities. Anti-inflammatory activity tested by reduces local edema induced in the rat paw by injection of phlogestic agent. Compound $2MB_1$, $2MB_8$, $2MB_5$, $2MB_3$ and $2MB_6$ exhibit satisfying anti-inflammatory activity while analgesic activity conducted by acetic acid induced writhing effect in mice while compound $2MB_1$, $2MB_4$ and $2MB_7$ having the good analgesic activity. The chemical structures of all newly synthesized compounds were confirmed by their IR, $^1H$ NMR and mass spectral data.

• Archives of Pharmacal Research
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• v.7 no.2
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• pp.127-132
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• 1984

Systematic pharmacological astudies on pipeline have revealed that this compound elicited diverse pharmacological activities; CNS depressant activity characterized by antagonism against electo shock seizure and by muscle relaxant activity in mice; antipyretic activity in tyyhoid vaccinated rabbits; analgesic activity as evaluated by tail-clip pressure and writhing syndrome in mice; antiinflammatory activity in carrageenin-induced edema in rats.

• Natural Product Sciences
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• v.3 no.2
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• pp.135-140
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• 1997

The methanolic extract of Lysimachiae christinae Herba, which has been used for diuretic, calculi remover and jaundice remedy in oriental countries, was found to possess analgesic and antiinflammatory effect in Freund's complete adjuvant treated rat. From ethyl acetate fraction of the herb a phenyl propanoid isoferulic acid was isolated as an active principle.

• YAKHAK HOEJI
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• v.37 no.6
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• pp.631-637
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• 1993

In the previous report, it was described that the butanol fraction of the root bark extract of Aralia elata had potent antigastritic and antiulcerative effects in rats, In this pharmacological profile, the fraction revealed low acute toxicities in mice and rats, no central nervous system activities, moderate analgesic action, weak inhibitory action in carrageenin edema of rats and no direct effects on isolated smooth muscles of rats and guinea-pigs. Slight lowering of blood pressure as given i.v. in rabbit was observed.

• Archives of Pharmacal Research
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• v.12 no.3
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• pp.149-153
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• 1989

Seven 2, 3-diphenyl-5-methoxyindole derivatives were synthesized. The effect of structural variation of these molecules on biological activities was examined. None of the tested compounds was found to be toxic up 5 gm/Kg body weight. Four compounds demonstrated smooth muscle relaxant effects and one showed a persistent hypotensive effect. Only the parent compound, 2, 3-diphenyl-5-methoxyindole, showed a significant analgesic effect.

• Biomolecules & Therapeutics
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• v.5 no.1
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• pp.87-93
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• 1997

DA-5018, a new capsaicin derivative, showed potent analgesic effect comparable to that of morphine in various experimental acute pain models. in this study, whether the analgesic mechanism of DA-5018 is related to opiate receptors or prostanoids was investigated. The affinity of DA-5018 for opiate receptor was determined by receptor binding assay. The Ki values of DA-5018 for nonspecific and specific $\mu$, $textsc{k}$, $\delta$-opiate receptor was 299$\pm$8.88, 735$\pm$215, 2930$\pm$ 163, 1550$\pm$813 nM, respectively and DA-5018 exhibited lower affinity than morphine. DA-5018 (10-"~3$\times$10-′M) inhibited electrically-evoked contractions of the guinea ply ileum and rat vas deferens, and these inhibition was not antagonized by naloxone(10 nM), an opiate receptor antagonist. Antagonism of analgesic effect of 7A-5018 by naloxone was examined by tail pinch test. Analgesic action of DA-5018(0.1 ~2 mg/kg, 5.c.) was not antagonized by naloxone(1 mg/rg, i.p.). These results indicate that pharmacological action of DA-5018 is not related with opiate receptor. Cyclooxygenase and 5-lipoxygenase activities in rat peritoneal neutrophil treated with A23187 and arachidonic acid were measured by radioimmunoassay. DA-5018 stimulated the cyclooxygenase activity and the concentration show-ing the two fold increase of activity was 124$\mu$M. DA-5018 slightly inhibited 5-lipoxygenase activity and these results together indicate that analgesic action of 3A-5018 is not mediated through inhibition of cyclooxy genase or lipoxygenase. These results suggest that the analgesic effect of DA-5018 is not due to blocking opiate receptor or to inhibiting the synthesis of prostanoids in the arachidonic acid metabolism pathway.