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Antinociceptive Activity (antinociceptive + activity)

Distribution by Scientific Domains

Medical Sciences	88%
Chemistry	11%

Selected Abstracts

AMINO ACID AND FATTY ACID COMPOSITION OF AN AQUEOUS EXTRACT OF CHANNA STRIATUS (HARUAN) THAT EXHIBITS ANTINOCICEPTIVE ACTIVITY

CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, Issue 3 2007
ZA Zakaria
SUMMARY 1The present study was performed in order to determine the amino acid and fatty acid composition of an aqueous extract of the freshwater fish Channa striatus, obtained by soaking (1 : 2, w/v) fresh fillets overnight in a chloroform : methanol (2 : 1, v/v) solvent, to elucidate the mechanism responsible for its antinociceptive activity and to clarify the relationship between the presence of the amino and fatty acids and the expected activity. 2The aqueous extract was found to contain all amino acids with the major amino acids glycine, alanine, lysine, aspartic acid and proline making up 35.77 ± 0.58, 10.19 ± 1.27, 9.44 ± 0.56, 8.53 ± 1.15 and 6.86 ± 0.78% of the total protein, respectively. 3In addition, the aqueous extract was found to have a high palmitic acid (C16 : 0) content, which contributed approximately 35.93 ± 0.63% to total fatty acids. The other major fatty acids in the aqueous extract were oleic acid (C18 : 1), stearic acid (C18 : 0), linoleic acid (C18 : 2) and arachidonic acid (C20 : 4), contributing 22.96 ± 0.40, 15.31 ± 0.33, 11.45 ± 0.31 and 7.44,±,0.83% of total fatty acids, respectively. 4Furthermore, the aqueous extract was demonstrated to possess concentration-dependent antinociceptive activity, as expected, when assessed using the abdominal constriction test in mice. 5It is concluded that the aqueous extract of C. striatus contains all the important amino acids, but only some of the important fatty acids, which are suggested to play a key role in the observed antinociceptive activity of the extract, as well as in the traditionally claimed wound healing properties of the extract. [source]

Evidence for Antinociceptive Activity of Botulinum Toxin Type A in Pain Management

HEADACHE, Issue 2003
K. Roger Aoki PhD
The neurotoxin, botulinum toxin type A, has been used successfully, in some patients, as an analgesic for myofascial pain syndromes, migraine, and other headache types. The toxin inhibits the release of the neurotransmitter, acetylcholine, at the neuromuscular junction thereby inhibiting striated muscle contractions. In the majority of pain syndromes where botulinum toxin type A is effective, inhibiting muscle spasms is an important component of its activity. Even so, the reduction of pain often occurs before the decrease in muscle contractions suggesting that botulinum toxin type A has a more complex mechanism of action than initially hypothesized. Current data points to an antinociceptive effect of botulinum toxin type A that is separate from its neuromuscular activity. The common biochemical mechanism, however, remains the same between botulinum toxin type A's effect on the motor nerve or the sensory nerve: enzymatic blockade of neurotransmitter release. The antinociceptive effect of the toxin was reported to block substance P release using in vitro culture systems.1 The current investigation evaluated the in vivo mechanism of action for the antinociceptive action of botulinum toxin type A. In these studies, botulinum toxin type A was found to block the release of glutamate. Furthermore, Fos, a product of the immediate early gene, c- fos, expressed with neuronal stimuli was prevented upon peripheral exposure to the toxin. These findings suggest that botulinum toxin type A blocks peripheral sensitization and, indirectly, reduces central sensitization. The recent hypothesis that migraine involves both peripheral and central sensitization may help explain how botulinum toxin type A inhibits migraine pain by acting on these two pathways. Further research is needed to determine whether the antinociceptive mechanism mediated by botulinum toxin type A affects the neuronal signaling pathways that are activated during migraine. [source]

Antinociceptive Activity of a New Benzofuranone Derived from a Chalcone

BASIC AND CLINICAL PHARMACOLOGY & TOXICOLOGY, Issue 4 2009
Pâmela Padaratz
The aim of this work was the synthesis of a new benzofuranone compound and evaluation of its antinociceptive potential in mice. The new benzofuranone 4 was synthesized from chalcone 3. The antinociceptive activity of 4 was determined by writhing, formalin, capsaicin, and glutamate and hot-plate tests. Compound 4 caused potent and dose-related inhibition against the writhing test with ID50 6.1 (5.1,7.6) ,mol/kg, i.p., being about 15 times more active than the reference drugs, acetyl salicylic acid and acetaminophen. It was also effective in a dose-dependent manner in significantly reducing the painful stimulus in both phases of formalin, in the capsaicin and in the glutamate test with ID50 values of 27.3 (24.5,30.6) and 18.9 (18.5,19.4) ,mol/kg (first and second phase), 12.6 (9.8,16.2) and 24.5 (20.4,29.6) ,mol/kg respectively. The results showed that the studied compound exhibits both central and peripheral antinociceptive activities and might be further used as a model to obtain new and more potent analgesic drugs. [source]

ChemInform Abstract: Synthesis and Antinociceptive Activity of 6-Substituted-3-pyridazinone Derivatives.

CHEMINFORM, Issue 32 2001
Mehtap Gokce
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Antinociceptive, antiin,ammatory and acute toxicity effects of Salvia leriifolia Benth. seed extract in mice and rats

PHYTOTHERAPY RESEARCH, Issue 4 2003
Hossein Hosseinzadeh
Abstract The antinociceptive and antiin,ammatory effects as well as the acute toxicity of Salvia leriifolia aqueous seed extract were studied in mice and rats. Antinociceptive activity was assessed using the hot-plate and tail ,ick tests. The effect on acute in,ammation was studied using vascular permeability increased by acetic acid and xylene-induced ear oedema in mice. The activity against chronic in,ammation was assessed using the cotton pellet test in rats. The LD50 of the extract was found to be 19.5 g/kg (i.p.) in mice. The aqueous seed extract showed signi,cant and dose-dependent (1.25,10 g/kg) antinociceptive activity over 7 h, and was inhibited by naloxone pretreatment. Signi,cant and dose-dependent (2.5,10 g/kg) activity was observed against acute in,ammation induced by acetic acid and in the xylene ear oedema test. In the chronic in,ammation test the extract (2.5,5 g/kg) showed signi,cant and dose-dependent antiin,ammatory activity. The aqueous seed extract of S. leriifolia may therefore have supraspinal antinociceptive effects which may be mediated by opioid receptors, and showed considerable effects against acute and chronic in,ammation. Copyright © 2003 John Wiley & Sons, Ltd. [source]

Anti-angiogenic, antinociceptive and anti-inflammatory activities of Lonicera japonica extract

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 6 2008
Hye-Jung Yoo
This study aimed to elucidate some novel pharmacological activities of Lonicera japonica (Caprifoliaceae), which is widely used in Oriental folk medicine. The ethanolic extract of L. japonica (LJ) dose dependently inhibited chick chorioallantoic membrane angiogenesis. The antinociceptive activity of LJ was assessed using the acetic acid-induced constriction model in mice. LJ showed anti-inflammatory activity in two in-vivo models: the vascular permeability and air pouch models. LJ suppressed the production of nitric oxide via down-regulation of inducible nitric oxide synthase in lipopolysaccharide-stimulated RAW264.7 macrophage cells. However, LJ was unable to suppress induction of cyclooxygenase-2 in the stimulated macrophage cells. LJ decreased the reactive oxygen species level in the stimulated macrophage cells. In brief, the flowers of L. japonica possess potent anti-angiogenic and antinociceptive activities, in addition to anti-inflammatory activity, which partly supports its therapeutic efficacy. [source]

Analgesic and antiinflammatory activity of Cyclamen repandum S. et S.

PHYTOTHERAPY RESEARCH, Issue 7 2007
E. Speroni
Abstract According to folk medicine some species belonging to the genus Cyclamen were used for their biological activities. Early investigation of the different species of the genus resulted in the isolation of triterpenic saponins. No phytochemical and biological data are available on C. repandum. As part of a series of phytochemical investigations for bioactive compounds from medicinal plants, Cyclamen repandum S. et S. was investigated. The present study sought to find the antiinflammatory and antinociceptive activities of C. repandum tubers in rats and mice. A preliminary screening was conducted with three different extracts in the tests used, particularly the paw edema and the writhing tests. Subsequently some saponins isolated from the ME extract, the more effective one, have been identified. This paper also describes the results of fractionation and bioassay guided chemical studies. Chemical investigation of the active extract afforded the isolation and characterization of six triterpenic saponins. The possible antiinflammatory and analgesic properties were investigated as the saponin content of the fractions allows to speculate on such aspect. Copyright © 2007 John Wiley & Sons, Ltd. [source]

Antipyretic and analgesic activities of Caesalpinia bonducella seed kernel extract

PHYTOTHERAPY RESEARCH, Issue 5 2005
P. Archana
Abstract Ethanolic extract (70%) of Caesalpinia bonducella seed kernel has been subjected for its antipyretic and antinociceptive activities in adult albino rats or mice of either sex at 30, 100 and 300 mg/kg orally. The extract demonstrated marked antipyretic activity against Brewer's yeast-induced pyrexia in rats. The extract had significant central analgesic activity in hot plate and tail flick methods. It also exhibited marked peripheral analgesic effect in both acetic acid-induced writhing test in mice and Randall-Selitto assay in rats. It also significantly inhibited the formalin-induced hind paw licking in mice. In conclusion, the present study suggests that the ethanolic extract of Caesalpinia bonducella seed kernel possesses potent antipyretic and antinociceptive activities and thus, validates its use in the treatment of pain and pyretic disorders. Copyright © 2005 John Wiley & Sons, Ltd. [source]

Antinociceptive Activity of a New Benzofuranone Derived from a Chalcone

An introduction to enantiomers in psychopharmacology

HUMAN PSYCHOPHARMACOLOGY: CLINICAL AND EXPERIMENTAL, Issue S2 2001
Brian E. Leonard
Abstract There is growing scientific, clinical, commercial and regulatory recognition that enantiomers offer benefits over racemates in the management of psychiatric diseases as well as in clinical medicine generally. However, relatively few studies consider enantiomers' individual characteristics. This review considers some of the clinical benefits associated with using stereochemically pure drugs in psychiatric conditions other than depression. A review of the evidence shows that enantiomers offer four main benefits. Firstly, using a single enantiomer may allow a reduction in total dose, while maintaining or improving outcomes. For example, (+)-nefopam's antinociceptive activity is greater than that produced by both the racemate and (,)-nefopam, but with the same level of acute toxicity. Thus, a single enantiomer may offer greater efficacy, dose for dose, than the racemate. Secondly, assessing dose,response relationships is simpler. There is no reason to suppose that a racemate will necessarily contain the isomers' optimum therapeutic ratio, that one of the isomers will be inactive or that the enantiomers' dose,response curves will coincide. For example, the dose,response relationship for the induction of catalepsy in the rat by thioridazine suggested that the racemate was around 12 times more potent than (+)-thioridazine and three times more potent than (,)-thioridazine, when considering the actual concentrations in the striatum. Thirdly, using a single enantiomer may reduce pharmacokinetic and pharmacodynamic variability between patients. For example, the coefficients of variation for some of methadone's pharmacokinetic parameters may reach 70%, which might have clinical consequences. Finally, using a single enantiomer may reduce toxicity arising from the therapeutically inactive stereoisomer. For example, the single enantiomers of bupivacaine and ropivacaine are significantly less cardiotoxic than their respective racemates. This review illustrates why stereochemistry should be considered when assessing the toxicology, pharmacokinetics, metabolism and efficacy of a racemate. Indeed, the differences may be so marked that achiral analyses may be misleading, and clinicians should consider prescribing an enantiomer whenever possible. In many cases, prescribing a single enantiomer improves the benefit:risk ratio. Finally, there is no reason to suppose that a racemate's characteristics will apply to the constituent enantiomers. Copyright © 2001 John Wiley & Sons, Ltd. [source]

Anti-inflammatory and analgesic activities of the ethanolic extracts from Zanthoxylum riedelianum (Rutaceae) leaves and stem bark

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 8 2007
Leonardo Mandalho Lima
We have evaluated the anti-inflammatory and analgesic properties of the leaves (LCE) and stem bark (BCE) crude extracts of Zanthoxylum riedelianum (Rutaceae). Different fractions of the stem bark extract (hexane, BCEH; dichloromethane, BCED; ethyl acetate, BCEE; and lyophilized aqueous residual, BCEW) were also investigated. We studied the effects of the extracts and fractions using the rat paw oedema test induced by carrageenan, dextran, histamine or nystatin; the mouse abdominal constriction test; the mouse hot-plate test (only for LCE and BCE); and the mouse formalin test. Both extracts and all BCE fractions displayed anti-inflammatory activity in the carrageenan-induced oedema model, but not for dextran, histamine or nystatin. Considering the analgesic models, both extracts showed antinociceptive activity, but BCE was more active than LCE in models of central pain. All BCE fractions showed significant inhibition in the abdominal constriction test and in both phases of the formalin test. When BCED was submitted to phytochemical procedures it led to the isolation of six lignans (sesamin, methylpluviatolide, dimethylmatairesinol, piperitol-4,-O-,,,-dimethylallyl ether, kaerophyllin and hinokinin), and a triterpene (lupeol). Inhibition of cyclooxygenase and its metabolites may have been involved in the mechanism of action of this plant, considering previous studies reporting the anti-inflammatory and analgesic activity for the identified lignans, as well as anti-inflammatory activity for lupeol. [source]

Investigations into the antinociceptive activity of Sapindus trifoliatus in various pain models

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 5 2004
D. K. Arulmozhi
The effect of the aqueous extract of Sapindus trifoliatus (ST) on chemical, thermal-induced pain, nitroglycerin-induced hyperalgesia and pain on inflamed tissue was investigated. The extract (20 and 100 mg kg,1, i.p.) significantly inhibited acetic-acid-induced abdominal constrictions, formalin-induced pain licking and hotplate-induced pain in mice. Furthermore, the extract significantly increased the response latencies of nitroglycerin-induced hyperalgesia by the tail-flick method and mechanical pain on carrageenan-induced inflamed paw in rats. The data suggest that ST has an inhibitory activity on both peripheral and central pain mechanisms and has a modulatory role in NO-mediated nociceptive transmission. [source]

Effect of Rosmarinus of,cinalis L. aerial parts extract on morphine withdrawal syndrome in mice

PHYTOTHERAPY RESEARCH, Issue 8 2003
Hossein Hosseinzadeh
Abstract The effect the aqueous and ethanol extracts of Rosmarinus of,cinalis L. aerial parts on morphine withdrawal syndrome was investigated in mice. The aqueous and ethanol extracts induced a signi,cant antinociceptive activity in the writhing test. This activity was inhibited by naloxone pretreatment. Dependence was induced using subcutaneous injections of morphine daily for 3 days. On day 4, morphine was injected 2 h prior to the intraperitoneal injection of naloxone. The number of jumps during the 30 min period after naloxone injection was considered as a measure of the withdrawal syndrome. The results indicated that the aqueous (1.68 g/kg and 2.4 g/kg, i.p.) and ethanol (0.96 g/kg, i.p.) extracts reduced the number of jumps. Phytochemical study indicated that only the aqueous extract of R. of,cinalis has an alkaloid component. It is concluded that the aqueous and ethanol extracts of R. of,cinalis aerial parts could diminish morphine withdrawal syndrome. Copyright © 2003 John Wiley & Sons, Ltd. [source]

Antinociceptive, antiin,ammatory and acute toxicity effects of Salvia leriifolia Benth. seed extract in mice and rats

Synthesis and Pharmacological Evaluation of N -(Dimethylamino)ethyl Derivatives of Benzo- and Pyridopyridazinones

ARCHIV DER PHARMAZIE, Issue 1 2009
Wanda Pakulska
Abstract New N -(dimethylamino)ethyl derivatives of phthalazinones and pyridopyridazinones 7, 9 were synthesized and assayed as potential analgesic agents in the hot-plate, tail-flick, and writhing tests. Pharmacological assay demonstrated that eight (in ten) of the newly synthesized compounds showed antinociceptive activity. Especially, 2-[2-(dimethylamino)ethyl]-4-phenyl-2H -phthalazin-1-one 7a showed remarkably higher antinociceptive activity in all tests. This is connected with influence on supraspinal, spinal, and peripheral structures. The decreased sensitivity to the pain stimulus in the hot-plate was higher than that of metamizole. [source]