Syntheses and Evaluation of the Analgesic Activity of Some 4-Acetyl- 4-phenylpiperidine and 4-Hydroxy-4-phenylpiperidine Derivatives

1999 ◽  
Vol 54 (10) ◽  
pp. 1327-1336 ◽  
Author(s):  
Zafar Saeed Saify ◽  
Khalid Mohammed Khan ◽  
Syed Moazzam Haider ◽  
Syed Tasadaque Ali Shah ◽  
Muhammad Saeed ◽  
...  
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Analgesic Activity ◽  
Tail Flick ◽  
Spectroscopic Techniques ◽  
Tail Flick Test ◽  
Derivatives Of

Synthesis and analgesic activity of 4-phenylpiperidine derivatives is a topic of high actuality. A s part of a programme towards obtaining new potential analgesics, ten derivatives of 4- acetyl-4-phenylpiperidine and ten derivatives of 4-hydroxy-4-phenylpiperidine were synthesised and characterized through spectroscopic techniques. All derivatives along with the parent compounds were evaluated for analgesic activity in the acetic acid-induced writhing assay and tail-flick test in mice. All derivatives of 4-acetyl-4-phenylpiperidine except one com pound exhibited more or less protection against mice writhing, whereas all the compounds proved to be inactive in the tail-flick test at doses of 50 and 100 mg/kg body weight.

scholarly journals Onosma bracteatum wall: A Potent analgesic agent

2018 ◽  
Vol 17 (1) ◽  
pp. 36-41 ◽  
Author(s):  
Hina Imran ◽  
Atiq Ur Rahman ◽  
Tehmina Sohail ◽  
S Intasar H Taqvi ◽  
Zahra Yaqeen
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Analgesic Activity ◽  
Latency Period ◽  
Maximum Effect ◽  
Tail Flick ◽  
Significant Activity ◽  
Tail Flick Test ◽  
Writhing Test ◽  
Post Feeding

Background: This study was aimed to find out the central and peripheral analgesic activity of hydro methanolic extract of aerial parts of Onosma bracteatum.Material and methods: The central and peripheral analgesic activity is evaluated by tail flick test and acetic acid induced writhing test at the doses of 50, 100, 250 and 500mg/kg body weight respectively in animal models.Results: The results obtained from Tail flick test revealed that O. bracteatum possesses potent analgesic effects by inducing significant increase in latency period in dose dependent manner at all doses at 1, 2 and 3 hours post feeding respectively. The maximum effect was observed at a dose of 500mg/kg i.e. 258.9% (p<0.05) at 3hrs post feeding. Diclofenac sodium (5mg/kg body weight) run as standard also increased the latency period continuously and highest activity was noted at 3hr i.e. 284.5% (p<0.05). Acetic acid induced writhing test also showed significant activity in a similar manner by O. bracteatum i.e 54% (p<0.05) at 500mg/kg while standard drug Diclofenic sodium (5mg/kg body weight) showed 45.9% (p<0.05) activity.Conclusion: It is concluded that O. bracteatum possesses significant central and peripheral analgesic activity in animal model.Bangladesh Journal of Medical Science Vol.17(1) 2018 p.36-41

scholarly journals Analgesic activity of allopurinol and febuxostat in experimental animals

2018 ◽  
Vol 7 (4) ◽  
pp. 603
Author(s):  
Yajnesh P. Sahu ◽  
Sachchidanand Pandey ◽  
Sabita Mohapatra
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Physical Dependence ◽  
Experimental Pain ◽  
Opioid Analgesics ◽  
Analgesic Nephropathy ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Analgesic Effects ◽  
Peripheral Analgesia

Background: Currently, two classes of analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs) and opioid analgesics are used to manage pain in different clinical situations. Chronic uses of these drugs have various adverse effects like gastric ulceration/bleeding, analgesic nephropathy and respiratory depression, physical dependence, addiction, respectively. Xanthine oxidase inhibitors, used for chronic gout, might have a role in alleviation of pain, as per literature survey. Hence, the present study was carried out to evaluate the potential analgesic activity of allopurinol and febuxostat in different experimental models.Methods: The analgesic activity of allopurinol and febuxostat was assessed by employing two different experimental pain models-tail flick latency model in rats for central analgesia and acetic acid induced writhing model in mice for peripheral analgesia and was compared with tramadol and aspirin.Results: Allopurinol and febuxostat produced significant central and peripheral analgesic effects as is evident from increase in reaction time in tail flick test and inhibition in number of writhes in acetic acid induced writhing test.Conclusions: The results of the present study demonstrate marked analgesic effect of allopurinol and febuxostat.

Analgesic Activity of Tragia involucrata

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
M Alimuzzaman ◽  
Muniruddin Ahmed
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Oral Dose ◽  
Ethyl Acetate ◽  
Analgesic Activity ◽  
Methanolic Extract ◽  
Radiant Heat ◽  
Tail Flick ◽  
Methanolic Extracts ◽  
Whole Plant

The work was carried out to investigate the analgesic activity of the whole plant of Tragia involucrata Linn. The dried whole plant was successively extracted with petroleum ether, ethyl acetate and methanol. Experiments were carried out with these extracts for their peripheral and central antinociceptive potentials on acetic acid induced writhing and radiant heat tail-flick models in mice, respectively. Both the ethyl acetate and methanolic extracts showed significant writhing inhibition while the elongation of tail-flick time was most prominent with methanolic extract at an oral dose of 500 mg/kg body weight. Key words: Tragia involucrata, Analgesic activity, Acetic acid induced writhing, Radiant heat tail-flick. Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

scholarly journals Analgesic Activities of Synthesized Divalent Metal Complexes of Tolfenamic Acid

2016 ◽  
Vol 15 (1) ◽  
pp. 89-96 ◽  
Author(s):  
Md Mahabob Ullah Mazumder ◽  
Abhijit Sukul ◽  
Sajal Kumar Saha
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Metal Complexes ◽  
Divalent Metal ◽  
Tolfenamic Acid ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Analgesic Activities ◽  
Divalent Metal Complexes ◽  
Analgesic Potency

The objective of the study was to synthesize and to uncover the potentially interesting biological peripheral and central analgesic activities of some new divalent metal complexes of tolfenamic acid. The inception of the study was carried out with the formation of complexes [Cu(tolf)2(H2O)]2, [Co(tolf)2(H2O)2] and [Zn(tolf)2(H2O)] through the reaction of tolfenamic acid, a potent anti-inflammatory drug, with Cu, Co and Zn salts. Characterization of the metal complexes of tolfenamic acid was furnished with spectral (FTIR, UV-Visible) and calorimetric (DSC) analysis. The peripheral analgesic activities of the complexes were investigated by acetic acid-induced writhing method. In peripheral analgesia model, Cu, Co and Zn complexes of tolfenamic acid showed significantly promising analgesic potency at a dose of 25 mg/kg body weight with percentage of inhibition of acetic acid induced writhing by 49.67% (p < 0.01), 67.32% (p < 0.001) and 72.55% (p < 0.001), respectively compared to the standard tolfenamic acid 46.41%. Radiant heat tail-flick test was used to observe the central analgesic activity which showed analgesic effect evidenced by % elongation time (34.59%, 25.34% and 53.08%), respectively compared to that of morphine 2 mg/kg body weight at an equimolar dose of tolfenamic acid at 10 mg/kg body weight after 30 minutes. In the final analysis, it can be stipulated that newly synthesized stable metal complexes of tolfenamic acid have promising pharmacological effects like peripheral and central analgesic potency. Therefore, these complexes may be the better therapeutic options in the near future however it needs further extensive analysis in the pharmacokinetics, pharmacodynamics and toxicology perspective.Dhaka Univ. J. Pharm. Sci. 15(1): 89-96, 2016 (June)

scholarly journals Evaluation of the analgesic activity of the water soluble extract of stem of Tinospora cordifolia in experimentally induced pain in albino rats

2019 ◽  
Vol 7 (3) ◽  
pp. 938
Author(s):  
Sumanlata . ◽  
Akanksha Suman ◽  
Rajeev Kumar Sharma ◽  
Meenakshi Jindal ◽  
Adnan Khan
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Water Soluble ◽  
Tinospora Cordifolia ◽  
Albino Rats ◽  
Tail Flick ◽  
Soluble Extract ◽  
Hot Plate ◽  
Tail Flick Test ◽  
Water Soluble Extract

Background: Pain and pyrexia are the warning signals, primarily protective in nature, that cause discomfort and suffering and may even be unbearable and incapacitating. The modern drugs (like opioids, NSAIDs, corticosteroids) currently used for the management of pain, fever and inflammatory conditions, present with many known adverse effects. Tinospora cordifolia known as Giloe, widely used in folk medicine due to its property to cure a number of diseases. Hence the present study was undertaken to explore the analgesic activity of water-soluble extract of stem of T. cordifolia in albino rats in experimentally induced pain.Methods: Present study was done in the department of pharmacology, albino rats were used to study the analgesic activity of T. cordifolia aqueous extract at the dose of 1.25g/kg,2.5g/kg and 5g/kg p.o. Various methods like Eddy’s hot plate, tail flick test and acetic acid induced writhing were used for the anti- nociceptive study.Results: In Eddy’s hot plate and tail flick test an increase in reaction time was observed with peak effect at 90min. Results were similar to the standard drug Tramadol in acetic acid induced writhing increase in time of onset, decrease in number and duration of writhing was observed.Conclusions: Aqueous extract of T. cordifolia was effective in all the three models of pain suggesting its possible action by central and peripheral mechanisms. Activity of T. cordifolia can be attributed to various phytoconstituents viz. protoberberine alkaloids, terpenoids, glycosides and polysaccharides. It can be developed as potent analgesic agent in future.

Assessment ofOpuntia ficus-indicain vivo Following Ethnobotanical Survey: Confirmation of its Analgesic Activity

2018 ◽  
Vol 16 (S1) ◽  
pp. S191-S196
Author(s):  
A. Mouhaddach ◽  
A. El-hadi ◽  
K. Taghzouti ◽  
M. Bendaou ◽  
R. Hassikou
Keyword(s):  
Body Weight ◽  
Analgesic Activity ◽  
Prickly Pear ◽  
Tail Flick ◽  
Ethnobotanical Study ◽  
Ethnobotanical Survey ◽  
Hot Plate ◽  
Traditional Use ◽  
Opuntia Ficus Indica ◽  
Plant Parts

Opuntia ficus-indica(the cactus or prickly pear) is a cactus belonging to the Opuntiae family. Several Opuntiae plant parts have been used in traditional Moroccan medicine. In this study, we investigated its most common use as an analgesic. An ethnobotanical study ofOpuntia ficus-indicawas first conducted in 10 areas in Morocco. Extracts fromOpuntia ficus-indicacladodes were obtained using a decoction method and its analgesic activity in mice was investigated by the hot plate and tail flick methods. Cladode extracts had significant (p<0.05) analgesic activity at intraperitoneal doses of 300, 500, and 1000 mg/kg body weight. Both methods revealed significantly increased latency at all three doses (p<0.05) compared to controls. These data suggest that the traditional use of this plant as an analgesic is valid; in fact, perhaps it may be a centrally-acting analgesic.

scholarly journals Evaluation of Bioactivities of Gouania tiliaefolia Lam., an Indigenous Traditional Medicinal Plant of Bangladesh

2019 ◽  
Vol 22 (2) ◽  
pp. 200-207
Author(s):  
Tufael Ahmed ◽  
Rifat Khan ◽  
Nafisa Tabassum ◽  
Fahima Aktar ◽  
Mohammad Kaisarul Islam
Keyword(s):  
Body Weight ◽  
Blood Glucose ◽  
Analgesic Activity ◽  
Methanol Extract ◽  
Phenolic Content ◽  
Total Phenolic ◽  
Oral Glucose ◽  
Tail Flick ◽  
Cytotoxic Activities ◽  
Crude Methanol Extract

The crude methanol extract of Gouania tiliaefolia Lam. was partitioned by the modified Kupchan method and the fractions were evaluated for total phenolic content, antioxidant, cytotoxic, thrombolytic, hypotonic and heat-induced membrane stabilizing activities. The petroleum ether soluble fraction (PESF) and methanol extract (ME) showed the highest phenolic content of 78.30 ±1.60 mg and 70.37 ± 0.84 mg, respectively, which were expressed in gallic acid equivalent (GAE). Similar trends were observed in case of anti-oxidant and cytotoxic activities, where the PESF possessed the highest free radical scavenging activity and brine shrimp lethality (IC50 = 2.88 ± 0.02 μg/ml, LC50 = 2.59 ± 0.14 μg/ml), followed by ME (IC50 = 4.79 ± 0.17 μg/ml, LC50 = 3.38 ± 0.08 μg/ml) and CSF (IC50 = 37.51 ± 0.96 μg/ml, LC50 = 73.55 ± 0.26 μg/ml). In case of assays for thrombolytic and membrane stabilizing activities, all extractives showed insignificant results compared to the respective standards. The crude methanol extract of G. tiliaefolia was used to examine the in-vivo analgesic (central and peripheral), antidiarrheal and antidiabetic activities in Swiss albino mice. In case of castor oil induced diarrhea, the ME gave better reduction of diarrhea by 71.43% (at 400 mg/kg-body weight) compared to loperamide (64.29%). Antidiabetic activity was evaluated by oral glucose tolerance test and the ME showed 71.42% and 75.39% reduction of blood glucose at doses 200 and 400 mg/kg-body weight, respectively when compared with the standard glibenclamide that reduced blood glucose by 66.17%. The central- and peripheral-analgesic activity was evaluated by the tail-flick test and acetic acid induced writhing test, respectively. In both the cases, ME demonstrated dose-dependent analgesic activity compared to the standards. Bangladesh Pharmaceutical Journal 22(2): 200-207, 2019

The Role of Andrographolide in Andrographis paniculata as a Potential Analgesic for Herbal Medicine based Drug Development

2021 ◽  
pp. 6269-6274
Author(s):  
Lidya Tumewu ◽  
Irfan Rayi Pamungkas ◽  
Hilkatul Ilmi ◽  
Achmad Fuad Hafid ◽  
Indah Setyawati Tantular ◽  
...  
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Herbal Medicine ◽  
Drug Development ◽  
Analgesic Activity ◽  
Active Ingredient ◽  
Active Substance ◽  
Ethanol Extract ◽  
Positive Control ◽  
Andrographis Paniculata

Background: Andrographis paniculata is a herbaceous plant in the Acanthaceae family, that is widely used as a traditional medicine in Asian countries and known to exhibit a wide range of pharmacological effects. Recent studies have provided an overview of the great potential of A. paniculata as an analgesic. The ethanol extract and ethyl acetate (EA) fraction of A.paniculata were shown to contain diterpene lactone compounds, which may be useful as a potential active ingredient in analgesic drugs. The development of a herbal medicine based drug requires an effective and high quality active ingredient. Therefore, this research was aimed to compare the analgesic activity of ethanol extract and EA fraction based on their andrographolide content and further to determine the more viable active substance for analgesic herbal medicine based drug development. Method: The andrographolide content in the ethanol extract and EA fraction was determined by High Pressure Liquid Chromatography (HPLC). Measurement of analgesic activity was performed by writhing test. The experimental animals were randomly divided into eight groups consisting of 5 mice in each. Group 1 (negative control) received 1% Tween-80 in normal saline. Group 2 (positive control) received a standard analgesic drug (diclofenac sodium) at a dose of 40 mg/kg body weight. Group 3, 4, and 5 received ethanol extract while Group 6, 7, and 8 received EA fraction, each at a dose of 12.5, 25, and 50 mg andrographolide/kg body weight, respectively. Each mouse was injected intraperitoneally with 1% acetic acid at a dose of 10 ml/kg body weight 30 minutes after oral administration of the treatments. The number of writhes were counted 5 min after acetic acid injection over a period of 45 min. Results: Andrographolide content in ethanol extract and EA fraction was 15.66±0.28 and 21.25±1.08 % w/w, respectively. Ethanol extract and EA fraction displayed analgesic activity of 67.68% and 70.91% respectively, at a dose of 50 mg andrographolide/kg body weight. The positive control at a dose of 40 mg/kg body weight showed an analgesic activity of 74.33%. Statistical analysis showed no significant differences between EA fraction at a dose of 50 mg andrographolide/kg body weight and ethanol extract at the same dose as well as the positive control (P> 0.05). The effective dose 50% (ED50) of the ethanol extract and EA fraction was determined to be 29.49 and 25.55 mg/kg body weight, respectively. Conclusion: It was possible to use andrographolide content as an indicator for the analgesic activity of A.paniculata. Ethanol extract and EA fraction of A. paniculata at the same dose of andrographolide showed similar analgesic activity. The amount of ethanol extract which needed to reach similar analgesic activity was higher than EA fraction. Therefore, EA fraction likely has greater potential as an analgesic active substance due to its higher content of andrographolide; however further study is needed to develop it as a dosage form.

scholarly journals Analgesic and Antidiarrheal Activities of Leaf of Podocarpus neriifolius D. Don

2016 ◽  
Vol 19 (2) ◽  
pp. 215-218
Author(s):  
Md Rahatullah Razan ◽  
Muhammed Mahfuzur Rahman ◽  
Faiza Tahia ◽  
Md Khalid Hossain ◽  
Mohammad A Rashid
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Analgesic Activity ◽  
Castor Oil ◽  
Methanol Extract ◽  
Methanolic Extract ◽  
Pharmaceutical Journal ◽  
Activity Assay ◽  
Swiss Albino Mice

The methanol extract of leaf of Podocarpus neriifolius D. Don exhibited in vivo peripheral analgesic and antidiarrheal activities in Swiss Albino mice. In the peripheral analgesic activity assay, the methanolic extract showed 50.00 ± 8.57% and 70.25 ± 1.18% inhibition of acetic acid-induced writhing at 200 and 400 mg/kg body weight, respectively. In addition, the extract also revealed a dose dependant inhibition of castor oil- induced diarrhea with 43.77 ± 3.13% and 56.23 ± 6.49% inhibition of feces at 200 and 400 mg/kg body weight, respectivelyBangladesh Pharmaceutical Journal 19(2): 215-218, 2016

scholarly journals Co-administration of Pregabalin and Curcumin Synergistically Decreases Pain-Like Behaviors in Acute Nociceptive Pain Murine Models

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4172
Author(s):  
Sarinee Leksiri ◽  
Hasriadi Hasriadi ◽  
Peththa Wadu Dasuni Wasana ◽  
Opa Vajragupta ◽  
Pornchai Rojsitthisak ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Area Under The Curve ◽  
Synergistic Interaction ◽  
Nociceptive Pain ◽  
Fixed Dose ◽  
Tail Flick ◽  
Dose Ratio ◽  
Tail Flick Test ◽  
Analgesic Effects ◽  
Pain Models

Analgesic drugs in a combination-form can achieve greater efficacy with lesser side effects compared to either drug alone. The combination of drugs acting at different targets or mechanisms of action has been recognized as an alternative approach for achieving optimal analgesia. In this study, the analgesic effects of pregabalin (30, 60, 100, 200 mg/kg), curcumin (15, 30, 60, 100, 120 mg/kg), and 1:1 fixed-dose ratio of the pregabalin-curcumin combination were assessed using two acute nociceptive pain models, the acetic acid-induced writhing and tail-flick tests in mice. The pregabalin-curcumin combination produced a dose-dependent decrease in mean of writhes and an increase in the percentage of antinociception by the acetic acid-induced writhing test. In the tail-flick test, the combination also showed an improvement in antinociception indicated by the tail-flick latency, % antinociception, and area under the curve (AUC). Isobolographic analysis of interactions demonstrated a significant synergistic interaction effect between pregabalin and curcumin in both acute nociceptive pain models with the experimental ED50 below the predicted additive line and the combination index < 1. These findings demonstrate that the combination of pregabalin and curcumin exhibits a synergistic interaction in mouse models of acute nociceptive pain.

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