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K Raafat, M Wurglics, M Schubert-Zsilavecz
Prunella vulgaris L. (Lamiaceae) (PV) is a herbaceous plant traditionally utilized in management of diabetes and it has immunomodulatory activity. In this study, acute and subchronic antidiabetic, in-vivo antioxidant and antinociceptive effects of PV were evaluated in alloxan-induced type 1 diabetes (T1D) in a mouse model. Bio-guided fractionation, isolation, RP-HPLC, and (1)H and (13)C NMR identification of the active components responsible for PV effects were determined. RP-HPLC analysis showed that PV contained rosmarinic acid (RA) 4...
October 18, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Patricia Ribeiro de Carvalho, Denise Ricoy Ropero, Mariana Martins Pinheiro, Patricia Dias Fernandes, Fabio Boylan
Choisya 'Aztec-Pearl', a hybrid of Choisya ternata and Choisya dumosa var. arizonica, had the antinociceptive activity in the ethanol extract (EECA) of its leaves evaluated. Two quinoline alkaloids, anhydroevoxine (A) and choisyine (C), isolated from these leaves were also tested. The results obtained pointed out to a very high antinociceptive activity measured by the hot plate model for EECA (at doses of 10, 30 and 100 mg/kg) as well as for A and C (at doses of 1, 3 and 10 mg/kg). The magnitude of the activity was two-fold higher than the one observed for the morphine treated animals for the higher doses of extracts/compounds (30, 100 mg/kg and 3, 10 mg/kg respectively)...
2016: PloS One
Raquel Tonello, Camilla Fusi, Serena Materazzi, Ilaria M Marone, Francesco De Logu, Silvia Benemei, Muryel C Gonçalves, Elisabetta Coppi, Celio J Castro-Junior, Marcus Vinicius Gomez, Pierangelo Geppetti, Juliano Ferreira, Romina Nassini
BACKGROUND AND PURPOSE: Peptides from venomous animals have long been important tools for understanding pain mechanisms and for the discovery of pain treatments. Here, we hypothesized that Phα1β, a peptide purified from the armed spider Phoneutria nigriventer venom, produces analgesia by blocking the transient receptor potential ankyrin 1 (TRPA1) channel. EXPERIMENTAL APPROACH: Cultured rat dorsal root ganglion (DRG) neurons, human IMR90 fibroblasts or HEK293 cells expressing the human TRPA1 (hTRPA1-HEK293), TRPV1 (hTRPV1-HEK293) or TRPV4 (hTRPV4-HEK293), were used for calcium imaging and electrophysiology...
October 19, 2016: British Journal of Pharmacology
Pranav Prasoon, Shivani Gupta, Rahul Kumar, Mayank Gautam, Saroj Kaler, Subrata Basu Ray
OBJECTIVES: Opioids such as morphine form the cornerstone in the treatment of moderate to severe pain. However, opioids also produce serious side effects such as tolerance. Fosaprepitant is a substance P (SP) receptor antagonist, which is used for treating chemotherapy-induced nausea and vomiting. SP is an important neuropeptide mediating transmission of pain at the spinal level. Thus, it was hypothesized that combining morphine with fosaprepitant would increase the antinociceptive effect of morphine...
July 2016: Indian Journal of Pharmacology
Angélica S Reis, Mikaela Pinz, Luis Fernando B Duarte, Juliano A Roehrs, Diego Alves, Cristiane Luchese, Ethel A Wilhelm
A growing body of evidence demonstrates that quinoline compounds have attracted much attention in the field of drug development. Accordingly, 4-phenylselenyl-7-chloroquinoline (4-PSQ) is a new quinoline derivative containing selenium, which showed a potential antioxidant, antinociceptive and anti-inflammatory effect. The present study was undertaken to evaluate the anxiolytic-like properties of 4-PSQ. Mice were orally pretreated with 4-PSQ (5-50 mg/kg) or vehicle, 30 min prior to the elevated plus-maze (EPM), light-dark (LDT) or open field (OFT) tests...
October 11, 2016: Journal of Psychiatric Research
Jenny L Wiley, Julie A Marusich, Brian F Thomas
Originally developed as research tools for use in structure-activity relationship studies, synthetic cannabinoids contributed to significant scientific advances in the cannabinoid field. Unfortunately, a subset of these compounds was diverted for recreational use beginning in the early 2000s. As these compounds were banned, they were replaced with additional synthetic cannabinoids with increasingly diverse chemical structures. This chapter focuses on integration of recent results with those covered in previous reviews...
October 18, 2016: Current Topics in Behavioral Neurosciences
Giorgia Macedonio, Azzurra Stefanucci, Cristina Maccallini, Sako Mirzaie, Ettore Novellino, Adriano Mollica
The endocannabinoid system is activated by the binding of natural arachidonic acid derivatives (endogenous cannabinoids or endocannabinoids) as lipophilic messengers to cannabinoid receptors CB1 and CB2. The endocannabinoid system comprises also many hydrolytic enzymes responsible for the endocannabinoids cleavage, such as FAAH and MAGL. These two enzymes are possible therapeutic targets for the development of new drugs as indirect cannabinoid agonists. Recently a new family of endocannabinoid modulators was discovered; the lead of this family is the nonapeptide hemopressin produced from enzymatic cleavage of the α-chain of hemoglobin and acting as negative allosteric modulator of CB1...
October 7, 2016: Protein and Peptide Letters
Carla Marrassini, Claudia Anesini
There is a well known link between inflammation and cancer during initiation, propagation and metastasis. Urera aurantiaca (UA) Wedd. (Urticaceae) is a medicinal plant used in traditional medicine to treat inflammatory processes with proven in vivo antiinflammatory and antinociceptive effects. The effects of a methanolic extract (UA) and a purified fraction (PF) on the proliferation of normal and tumoral lymphocytes under the effect of prostaglandin E2 (PGE2 ) and on nitric oxide production by lipopolysaccharide-stimulated macrophages was evaluated...
October 17, 2016: Phytotherapy Research: PTR
Rui He, Yongsong Xu, Jingjing Peng, Tingting Ma, Jing Li, Muxin Gong
Paeoniflorin (PF), the main active component of Shaoyao-Gancao-tang, possesses significantly antinociceptive effects and many other pharmacological activities. However, its poor intestinal absorption results in low bioavailability. Therefore, enhancing PF absorption plays a vital role in exerting its therapeutic effect. Shaoyao combined with Gancao exhibited a synergistic effect. The enhancement of PF absorption through the interaction of its constituents in intestinal absorption would be greatly implicated...
October 17, 2016: Journal of Natural Medicines
Bassem Yousef Sheikh, S M Neamul Kabir Zihad, Nazifa Sifat, Shaikh J Uddin, Jamil A Shilpi, Omer A A Hamdi, Hemayet Hossain, Razina Rouf, Ismet Ara Jahan
In addition to the rich nutritional value, date palm is also used in various ethnobotanical practices for the treatment of various disease conditions. Present investigation was undertaken to examine the neuropharmacological and antinociceptive effect of the ethanol extract of three date cultivars growing in Saudi Arabia, namely Ajwah, Safawy and Sukkari. Neuropharmacological effect was observed by pentobarbitone induced sleeping time, open field, and hole board test. Antinociceptive activity was tested by acetic acid induced writhing and hot plate test...
2016: Oriental Pharmacy and Experimental Medicine
Ram Kandasamy, Jonas J Calsbeek, Michael M Morgan
Opioids are effective at inhibiting responses to noxious stimuli in rodents, but have limited efficacy and many side effects in chronic pain patients. One reason for this disconnect is that nociception is typically assessed using withdrawal from noxious stimuli in animals, whereas chronic pain patients suffer from abnormal pain that disrupts normal activity. We hypothesized that assessment of home cage wheel running in rats would provide a much more clinically relevant method to assess opioid efficacy to restore normal behavior...
October 13, 2016: Behavioural Brain Research
Fabíula Francisca Abreu, Ana Carla Araujó de Souza, Simone Aparecida Teixeira, Antônio Garcia Soares, Daiane Franco Teixeira, Rosilene Calazans Soares, Marilia Trindade Santana, Sandra Lauton Santos, Soraia Kátia Pereira Costa, Marcelo Nicolas Muscará, Enilton Aparecido Camargo
INTRODUCTION: Acute pancreatitis (AP) may be severe and cause hospitalization or death, and the available treatment is insufficient to control pancreatic inflammation and pain. Rutin is a natural flavonoid with the potential to treat AP via anti-inflammatory, antinociceptive and antioxidant activities. AIM: This study investigated the beneficial effects of rutin on experimental AP induced by L-arginine administration in mice. METHODS: The L-arginine-induced AP model was used in Swiss mice (n = 6-8)...
October 13, 2016: Free Radical Research
- Barkatullah, Muhammad Ibrar, Nazia Ikram, Abdur Rauf, Taibi Ben Hadda, Saud Bawazeer, Haroon Khan, Samreen Pervez
The current study was designed to assess the antinociceptive and skeleton muscle relaxant effect of leaves and barks of Buddleja asiatica in animal models. In acetic acid induced writhing test, pretreatment of ethanolic extract of leaves and barks evoked marked dose dependent antinociceptive effect with maximum of 70% and 67% pain relief at 300mg/kg i.p. respectively. In chimney test, the ethanolic extract of leaves and barks evoked maximum of 66.66% and 53.33% muscle relaxant effect after 90min of treatment at 300mg/kg i...
September 2016: Pakistan Journal of Pharmaceutical Sciences
Handong Ouyang, Peizong Wang, Wan Huang, Qian Li, Bilin Nie, Weian Zeng
[This corrects the article DOI: 10.1155/2015/902914.].
2016: Pain Research & Management: the Journal of the Canadian Pain Society
Pauline W Ondachi, Ana H Castro, Benjamin Sherman, Charles W Luetje, M Imad Damaj, Samuel Wayne Mascarella, Hernán A Navarro, Frank Ivy Carroll
The synthesis, nAChR in vitro and in vivo pharmacological properties of 2'-fluoro-3'-(substituted thiophenyl)deschloroepibatidine analogues (5a-f, 6a-d, and 7a-c) are presented herein. All had subnanomolar affinity at α4β2*-nAChRs. Contrary to lead structure epibatidine, a potent nAChR agonist, all were potent α4β2- and α3β4-AChR antagonists in an in vitro functional assay. In vivo, the compounds were also nAChR antagonists with various degrees of agonist activity. Compounds 5e, 5f, 6a, 6c, 6d, and 7c had no agonist effects in the tail-flick, hot-plate, hypothermia, or spontaneous activity tests whereas 5a-d, 7a and 7b did not have agonist activity in the tail-flick and hot-plate tests but like varenicline, were agonists in the hypothermia and spontaneous activity tests...
October 11, 2016: ACS Chemical Neuroscience
Bruno H Pypendop, Yael Shilo-Benjamini, Jan E Ilkiw
OBJECTIVE: To determine the effects of morphine, methadone, hydromorphone or oxymorphone on the thermal threshold in cats, following buccal and intravenous (IV) administration. STUDY DESIGN: Randomized crossover study. ANIMALS: Six healthy adult female ovariohysterectomized cats weighing 4.5 ± 0.4 kg. METHODS: Morphine sulfate (0.2 mg kg(-1) IV or 0.5 mg kg(-1) buccal), methadone hydrochloride (0.3 mg kg(-1) IV or 0...
November 2016: Veterinary Anaesthesia and Analgesia
B E Brito, E Vazquez, P Taylor, Y Alvarado, H Vanegas, A Millan, V Tortorici
BACKGROUND: Opioid effectiveness to treat cancer pain is often compromised by the development of tolerance and the occurrence of undesirable side effects, particularly during long-term treatment. Hence, the search for more efficient analgesics remains a necessity. The main goal of this study was to relieve neuropathic symptoms associated with tumour growth by administering the non-opioid analgesic dipyrone (DIP) alone or in combination with magnesium chloride (MgCl2 ), an adjuvant that blocks the NMDA receptor channel...
October 10, 2016: European Journal of Pain: EJP
Yuvaraj Neelakandan, Arul Venkatesan
AIM: The aim of this objective is to evaluate the antinociceptive and anti-inflammatory potential of sulfated polysaccharide purified fractions isolated from brown seaweed Sargassum wightii and seagrass Halophila ovalis in male Wistar rats. SUBJECTS AND METHODS: Crude sulfated polysaccharide from S. wightii and H. ovalis was subjected to anion exchange chromatography, and the chemical composition was investigated. The antinociceptive activity of purified fractions was investigated using formalin and hot plate test...
September 2016: Indian Journal of Pharmacology
O Prezzavento, E Arena, C Sánchez-Fernández, R Turnaturi, C Parenti, A Marrazzo, R Catalano, E Amata, L Pasquinucci, E J Cobos
cis-N-Substituted N-normetazocine enantiomers possess peculiar pharmacological profiles. Indeed, dextro enantiomers bind with high affinity σ1 receptor while opposite enantiomers bind opioid receptors. In spite of their stereochemistry, cis-N-2-phenylethyl N-normetazocine (phenazocine) enantiomers showed mixed opioid/σ1 receptor profiles and a significant in vivo analgesia. To the best of our knowledge, there is no information available regarding the evaluation of σ1 pharmacological profile in the antinociceptive effects of (+)- and (-)-phenazocine...
September 26, 2016: European Journal of Medicinal Chemistry
Ramanathan Srinivasan, Kannan Rama Devi, Arunachalam Kannappan, Shunmugiah Karutha Pandian, Arumugam Veera Ravi
ETHNOPHARMACOLOGICAL RELEVANCE: Piper betle, a tropical creeper plant belongs to the family Piperaceae. The leaves of this plant have been well known for their therapeutic, religious and ceremonial value in South and Southeast Asia. It has also been reported to possess several biological activities including antimicrobial, antioxidant, antinociceptive, antidiabetic, insecticidal and gastroprotective activities and used as a common ingredient in indigenous medicines. In Indian system of ayurvedic medicine, P...
October 6, 2016: Journal of Ethnopharmacology
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