scholarly journals Possible Involvement of Serotonergic Mechanism(s) in the Antinociceptive Effects of kaempferol

2020 ◽  
pp. 64-70
Keyword(s):  
Locomotor Activity ◽  
Receptor Antagonist ◽  
Serotonin Receptors ◽  
Metabolic Diseases ◽  
Male Rats ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Way 100635 ◽  
Antinociceptive Effects ◽  
Male Wistar Rats

Background and Objectives: A flavonoid kaempferol (KM) exerts an anti-inflammatory effect and is reportedly capable of preventing metabolic diseases. Nonetheless, a limited number of studies have been carried out on the antinociceptive effects of kaempferol. Objectives: The present study aimed to investigate the involvement of serotonin receptors in the antinociceptive-like activity of KM in male Wistar rats using the tail-flick test. Materials and Methods: The compounds (i.e., KM, morphine, and diclofenac) were intracerebroventricularly administered to rats for the examination of central effects on the thermal pain using the tail-flick test. For the evaluation of the involvement of serotonin receptors in the possible antinociceptive effects of kaempferol, several antagonists (i.e., tropisetron, ketanserin, GR113808, WAY 100635, and penbutolol) were used. Additionally, locomotor activity and motor responses were investigated by the rotarod test after KM treatment. Results: The intracerebroventricular microinjections of KM showed antinociceptive effects using the tail-flick test. The pretreatment with tropisetron as a 5-HT3 receptor antagonist at 1 and 10 mg completely reversed the KM-related antinociception. Furthermore, ketanserin (5-HT2A receptor antagonist) and GR113808 (5-HT4 receptor antagonist) both at 10 mg reduced KM-related antinociception; however, 5-HT1A receptor antagonist WAY 100635 and 5-HT1B antagonist penbutolol did not decrease KM-related antinociception. All KM doses were not observed with a significant effect on locomotor activity or motor reactions. Conclusion: The results of the current study suggested that serotonergic receptors (i.e., 5-HT2A, 5-HT3, and 5-HT4) are effective in the KM antinociceptive activity in male rats.

Attenuation of Morphine-Induced Tolerance and Dependence by Pretreatment with Cerebrolysin in Male rats

Drug Research ◽  
2017 ◽  
Vol 68 (01) ◽  
pp. 33-37 ◽  
Author(s):  
Hamed Ghavimi ◽  
Sara Darvishi ◽  
Saeed Ghanbarzadeh
Keyword(s):  
Male Rats ◽  
Control Group ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Attenuation Effect ◽  
Morphine Administration ◽  
Male Wistar Rats ◽  
Potent Growth ◽  
Induced Tolerance ◽  
Withdrawal Signs

Abstract Background Dependence and tolerance to morphine are major problems which limit its chronic clinical application. Purpose This study was aimed to investigate the attenuation effect of Cerebrolysin, a mixture of potent growth factors (BDNF, GDNF, NGF, CNTF etc,), on the development of Morphine-induced dependence and tolerance. Methods Male Wistar rats were selected randomly and divided into different groups (n=8) including: a control group, groups received additive doses of morphine (5–25 mg/kg, ip, at an interval of 12 h until tolerance completion), and groups pretreated with Cerebrolysin (40, 80 and 160 mg/kg, ip, before morphine administration). Development of tolerance was assessed by tail-flick test and the attenuation effect of Cerebrolysin on morphine-induced dependence was evaluated after injection of naloxone (4 mg/kg, ip, 12 h after the morning dose of morphine). Seven distinct withdrawal signs including: jumping, rearing, genital grooming, abdominal writhing, wet dog shake and teeth grinding were recorded for 45 min and total withdrawal score (TWS) was calculated. Results Results showed that administration of Cerebrolysin could prolonged development (10 and 14 days in administration of 80 mg/kg and 160 mg/kg Cerebrolysin) and completion (4, 10 and 14 days in administration of 40, 80 and 160 mg/kg Cerebrolysin, respectively) of tolerance. Results also indicated that administration of Cerebrolysin (40, 80 and 160 mg/kg) could significantly decreased the TWS value (62±2, 77±4 and 85±6%, respectively). Conclusion In conclusion, it was found that pretreatment with Cerebrolysin could attenuated morphine-induced tolerance and dependence.

scholarly journals Comparing the Antinociceptive Effects of Methamphetamine, Buprenorphine, or Both After Chronic Treatment and Withdrawal in Male Rats

2019 ◽  
Vol 10 (4) ◽  
pp. 313-322
Author(s):  
Farshid Etaee ◽  
◽  
Arezoo Rezvani-Kamran ◽  
Mohammad Taheri ◽  
Ghazaleh Omidi ◽  
...  
Keyword(s):  
Pain Perception ◽  
Synergistic Effects ◽  
Reaction Times ◽  
Male Rats ◽  
Tail Flick ◽  
Hot Plate ◽  
Analgesic Effects ◽  
Antinociceptive Effects ◽  
Male Wistar Rats ◽  
Post Hoc

Introduction: Methamphetamine (Meth) and Buprenorphine (BUP) modulate pain perception. However, the antinociceptive effects of their interactions, which affect through different systems, are unclear in rats. This study aimed to compare the analgesic effects of Meth, BUP, and their coadministration, as well as the effect of withdrawal from these substances on nociception in male rats. Methods: In this experiment, 40 male Wistar rats (weight: 250-300 g) were categorized into four groups: control, Meth, BUP, or BUP+Meth. After seven days of treatments, the antinociceptive effects were assessed using the hot plate and the tail flick tests. The differences among the groups were analyzed with ANOVA and Tukey’s post hoc tests. P values less than 0.05 were considered significant. Results: Meth and BUP increased the reaction times during the hot plate and tail flick tests. The combination of Meth and BUP increased reaction time more than Meth or BUP alone.  Conclusion: The significantly high reaction times in rats treated with Meth and BUP indicate that these substances have antinociceptive effects. In addition, Meth enhanced the antinociceptive effects of BUP. These synergistic effects might occur through the dopaminergic, serotonergic, and or adrenergic systems.

scholarly journals Effects of peripheral FAAH blockade on NTG-induced hyperalgesia—evaluation of URB937 in an animal model of migraine

Cephalalgia ◽  
2015 ◽  
Vol 35 (12) ◽  
pp. 1065-1076 ◽  
Author(s):  
R Greco ◽  
T Bandiera ◽  
AS Mangione ◽  
C Demartini ◽  
F Siani ◽  
...  
Keyword(s):  
Animal Model ◽  
Antinociceptive Effect ◽  
Acid Amide ◽  
Male Rats ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Brain Nuclei ◽  
Nociceptive Responses ◽  
Fos Expression ◽  
Baseline Conditions

Background Systemic nitroglycerin (NTG) activates brain nuclei involved in nociceptive transmission as well as in neuroendocrine and autonomic functions in rats. These changes are considered relevant for migraine because NTG consistently provokes spontaneous-like migraine attacks in migraineurs. Several studies have suggested a relationship between the endocannabinoid levels and pain mediation in migraine. URB937, a peripheral inhibitor of fatty acid amide hydrolase (FAAH)—the enzyme that degrades anandamide, produces analgesia in animal models of pain, but there is no information on its effects in migraine. Aim We evaluated whether URB937 alters nociceptive responses in the animal model of migraine based on NTG administration in male rats, using the tail flick test and the plantar and orofacial formalin tests, under baseline conditions and after NTG administration. Furthermore, we investigated whether URB937 affects NTG-induced c-Fos expression in the brain. Results During the tail flick test, URB937 showed an antinociceptive effect in baseline conditions and it blocked NTG-induced hyperalgesia. URB937 also proved effective in counteracting NTG-induced hyperalgesia during both the plantar and orofacial formalin tests. Mapping of brain nuclei activated by NTG indicates that URB937 significantly reduces c-Fos expression in the nucleus trigeminalis caudalis and the locus coeruleus. Conclusions The data suggest that URB937 is capable of changing, probably via indirect mechanisms, the functional status of central structures that are important for pain transmission in an animal model of migraine.

Antinociceptive Profiles of Platycodin D in the Mouse

2004 ◽  
Vol 32 (02) ◽  
pp. 257-268 ◽  
Author(s):  
Seong-Soo Choi ◽  
Eun-Jung Han ◽  
Tae-Hee Lee ◽  
Ki-Jung Han ◽  
Han-Kyu Lee ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Control Level ◽  
Tail Flick ◽  
Triterpene Saponins ◽  
Tail Flick Test ◽  
Platycodin D ◽  
Pain Models ◽  
Antinociceptive Effects ◽  
Dose Dependent ◽  
Higher Doses

Platycodin D (PD), one of several triterpene saponins, was isolated from roots of Platycodon grandiflorum. We previously reported that intracerebroventricular (i.c.v.) administration of PD showed an antinociceptive effect as measured by the tail-flick assay. However, its exact role in the regulation of antinociception in the various types of pain models has not yet been characterized. Thus, we attempted to find antinociceptive profiles of PD in various pain models. PD administered intraperitoneally (i.p.), i.c.v. or intrathecally (i.t.) showed antinociceptive effects in dose-dependent manners as measured by the tail-flick, writhing and formalin tests. In the tail-flick test, PD at the low doses reached the peak after 15 minutes and returned to the control level after 60 minutes. However, higher doses of PD showed a strong antinociception at least for 1 hour. PD administered i.t. showed stronger antinociception than that induced by i.c.v. administration PD in both tail-flick and writhing tests. In the formalin test, PD administered i.p., i.c.v. or i.t. showed antinociceptive effects during both the first (direct nociceptive stimulation) and second (late inflammatory) phases. Pretreatment with naltrexone i.p., i.c.v. or i.t. did not affect PD-induced inhibition of the tail-flick response. Our results suggest that PD shows a strong antinociceptive effect on the tail-flick, writhing and formalin tests, acting on central nervous system. However, PD-induced antinociception may not be mediated by the opioid receptors.

scholarly journals The Role of NMDARs Ligands on Antinociceptive Effects of Pregabalin in the Tail Flick Test

2015 ◽  
Vol 5 (5) ◽  
Author(s):  
Manzumeh-Shamsi Meymandi ◽  
Fariborz Keyhanfar ◽  
Omid Yazdanpanah ◽  
Gioia Heravi
Keyword(s):  
Tail Flick ◽  
Tail Flick Test ◽  
Antinociceptive Effects

scholarly journals Investigation of Origanum compactum essential oil for analgesic and anti-inflammatory activities

2021 ◽  
Vol 319 ◽  
pp. 01104
Author(s):  
Jamila Hamamouchi ◽  
Mohammed El Mahi ◽  
Moulay El Abbes Faouzi
Keyword(s):  
Essential Oil ◽  
Opiate Receptors ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Aerial Parts ◽  
Male Wistar Rats ◽  
Origanum Compactum ◽  
Specific Antagonist ◽  
Anti Inflammatory ◽  
Dose Dependent

Origanum compactum Benth. has been widely used in moroccan traditional medicine for various therapeutic treatments. Belonging to the same genus, O. onites was found to have marked analgesic and anti-inflammatory activities. The aim of this work is to evaluate theses pharmacological properties of the essential oil of O. compactum in order to provide a basis for the folkloric use of the plant. Aerial parts of plant were subjected to steam distillation, according to the French Pharmacopoeia. Male OF1 mice and male Wistar rats were used for these studies. The analgesic effect was done using Writhing test in mice and Tail-Flick test in rats. The mechanism investigation was evaluated employing an antagonism assay using naloxone, a specific antagonist of opiate receptors. Anti- inflammatory property has been studied using carrageenin and experimental trauma induced edema in rats. The essential oil of the aerial parts of Origanum compactum was found to exert central analgesic properties. Such a dose-dependent action was obtained against chemical and thermic stimuli, respectively, from the doses of 6.25 and 12.5 mg/kg and it was inhibited by a naloxone pretreatment, a specific morphinic antagonist compound. Significant and dose-dependent anti-inflammatory effects were observed on an acute inflammatory process from the dose of 100 mg/kg.

scholarly journals Blockade of Serotonin 2C Receptors with SB-242084 Moderates Reduced Locomotor Activity and Rearing by Cannabinoid 1 Receptor Antagonist AM-251

Pharmacology ◽  
2019 ◽  
Vol 103 (3-4) ◽  
pp. 151-158 ◽  
Author(s):  
Emese Bogáthy ◽  
Diana Kostyalik ◽  
Peter Petschner ◽  
Szilvia Vas ◽  
Gyorgy Bagdy
Keyword(s):  
Locomotor Activity ◽  
Receptor Antagonist ◽  
Cb1 Receptor ◽  
Behavioral Effects ◽  
Receptor Antagonists ◽  
Plus Maze ◽  
Male Wistar Rats ◽  
Cb1 Receptor Antagonist ◽  
Cb1 Receptor Antagonists ◽  
Sb 242084

The endocannabinoid and serotonin (5-HT) systems have key roles in the regulation of several physiological functions such as motor activity and food intake but also in the development of psychiatric disorders. Here we tested the hypothesis, whether blockade of serotonin 2C (5-HT2C) receptors prevents the reduced locomotor activity and other behavioral effects caused by a cannabinoid 1 (CB1) receptor antagonist. As a pretreatment, we administered SB-242084 (1 mg/kg, ip.), a 5-HT2C receptor antagonist or vehicle (VEH) followed by the treatment with AM-251 (5 or 10 mg/kg, ip.), a CB1 receptor antagonist or VEH. The effects of the two drugs alone or in co-administration were investigated in social interaction (SI) and elevated plus maze (EPM) tests in male Wistar rats. Our results show that AM-251 decreased the time spent with rearing in the SI test and decreased locomotor activity in EPM test. In contrast, SB-242084 produced increased locomotor activity in SI test and evoked anxiolytic-like effect in both SI and EPM tests. When applied the drugs in combination, these behavioral effects of AM-251 were moderated by SB-242084. Based on these findings, we conclude that certain unwanted behavioral effects of CB1 receptor antagonists could be prevented by pretreatment with 5-HT2C receptor antagonists.

Comparative Neurotoxicity of Intrathecal and Epidural Lidocaine in Rats

2003 ◽  
Vol 99 (4) ◽  
pp. 961-968 ◽  
Author(s):  
Yumiko Kirihara ◽  
Yoji Saito ◽  
Shinichi Sakura ◽  
Keishi Hashimoto ◽  
Tomomune Kishimoto ◽  
...  
Keyword(s):  
Spinal Anesthesia ◽  
Epidural Catheter ◽  
Functional Impairment ◽  
Dose Effect ◽  
Male Rats ◽  
Clinical Impression ◽  
Tail Flick ◽  
Epidural Administration ◽  
Tail Flick Test ◽  
Potency Ratio

Background Although there is a considerable difference in the number of clinical reports of neurologic injury between spinal anesthesia and other regional techniques, there are no animal data concerning a difference in the local anesthetic neurotoxicity between intrathecal and epidural administration. In the current study, the functional and morphologic effects of lidocaine administered intrathecally and epidurally were compared in rats. Methods Male rats were implanted with an intrathecal or epidural catheter through L4-L5 vertebra in the caudal direction. In experiment 1, to determine relative anesthetic potency, 16 rats received repetitive injections of 2.5% lidocaine into intrathecal or epidural space in different volumes and were examined for tail flick test for 90 min. In experiment 2, to ascertain whether the relative potency obtained in experiment 1 would apply to other concentrations of lidocaine, additional rats received saline, 1%, 2.5%, or 5% lidocaine in a volume of 20 or 100 microl through the intrathecal or epidural catheter, respectively. In experiment 3, additional rats that received saline, 2.5% lidocaine, or 10% lidocaine in a volume of 20 or 100 microl through the intrathecal or epidural catheter, respectively, were examined for persistent functional impairment and morphologic damage. Results In experiment 1, the two techniques produced parallel dose-effect curves that significantly differed from each other. The potency ratio calculated was approximately 4.72 (3.65-6.07):1 for intrathecal:epidural lidocaine. In experiment 2, every lidocaine solution produced a similar increase in tail flick latency for the two techniques. In experiment 3, five of eight rats given 10% intrathecal lidocaine incurred functional impairment 4 days after injection, whereas no rats in the other groups did. Significantly more morphologic damage was observed in rats given 10% intrathecal lidocaine than in those given 10% epidural lidocaine. Conclusions Persistent functional impairment occurred only after intrathecal lidocaine. Histologic damage in the nerve roots and the spinal cord was less severe after epidural lidocaine than after intrathecal lidocaine. The current results substantiate the clinical impression that neurologic complications are less frequent after epidural anesthesia than after spinal anesthesia.

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