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Weijuan Du, Lisha Jin, Liping Li, Wei Wang, Su Zeng, Huidi Jiang, Hui Zhou
The tuber of Corydalis yanhusuo is a famous traditional Chinese medicine and found to have potent pharmacological effects, such as antinociceptive, antitumor, antibacterial, anti-inflammatory, and anti-depressive activities. Although there are several methods to be developed for the analysis and detection of the bioactive ingredients' alkaloids, so far, only few prominent alkaloids could be quantified, and in vitro and in vivo changes of comprehensive alkaloids after oral administration are still little known...
March 21, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Candy S Hwang, Lauren C Smith, Yoshihiro Natori, Beverly Ellis, Bin Zhou, Kim D Janda
The sharp increase in overdose deaths involving illicit opioid use has been declared a national crisis in the United States. This growing number of overdose deaths can in part be attributed to the increased frequency of fentanyl contamination in the United States heroin supply. To combat this growing trend, we designed a vaccine containing a mixture of heroin and fentanyl hapten-conjugates as a proof-of-concept immunotherapy targeting a combination of these drugs. Rodents immunized with the admixture vaccine showed drug retention in serum and reduced distribution in the brain after administration of an intravenous bolus of heroin coadministered with fentanyl (10% w/w)...
March 23, 2018: ACS Chemical Neuroscience
Jing Huang, Erika Polgár, Hans Jürgen Solinski, Santosh K Mishra, Pang-Yen Tseng, Noboru Iwagaki, Kieran A Boyle, Allen C Dickie, Mette C Kriegbaum, Hendrik Wildner, Hanns Ulrich Zeilhofer, Masahiko Watanabe, John S Riddell, Andrew J Todd, Mark A Hoon
Stimuli that elicit itch are detected by sensory neurons that innervate the skin. This information is processed by the spinal cord; however, the way in which this occurs is still poorly understood. Here we investigated the neuronal pathways for itch neurotransmission, particularly the contribution of the neuropeptide somatostatin. We find that in the periphery, somatostatin is exclusively expressed in Nppb+ neurons, and we demonstrate that Nppb+ somatostatin+ cells function as pruriceptors. Employing chemogenetics, pharmacology and cell-specific ablation methods, we demonstrate that somatostatin potentiates itch by inhibiting inhibitory dynorphin neurons, which results in disinhibition of GRPR+ neurons...
March 19, 2018: Nature Neuroscience
Shayne P Bisetto, Cristiano F Melo, Adriano B Carregaro
OBJECTIVE: To evaluate dexmedetomidine, midazolam and dexmedetomidine-midazolam for sedation and antinociception in tegus. STUDY DESIGN: Prospective, crossover, randomized, blinded study. ANIMALS: Six healthy tegus (Salvator merianae) weighing 1.6±0.3 kg. METHODS: Tegus were administered intramuscularly saline (0.5 mL; CON), dexmedetomidine (0.2 mg kg-1 ; DX), midazolam (1 mg kg-1 ; MZ) and dexmedetomidine-midazolam (same doses; DM)...
January 17, 2018: Veterinary Anaesthesia and Analgesia
Jun-Bin Yin, Ya-Cheng Lu, Ban Feng, Zhen-Yu Wu, Ying-Biao Chen, Ting Zhang, Zhen-Zhen Kou, Ming-Ming Zhang, Han Zhang, Jin-Lian Li, Hui Li, Tao Chen, Yu-Lin Dong, Yun-Qing Li
BACKGROUND/AIMS: Spinal dorsal horn (SDH) is one of the most important regions for analgesia produced by endomorphin-2 (EM2), which has a higher affinity and specificity for the µ-opioid receptor (MOR) than morphine. Many studies have focused on substantia gelatinosa (SG, lamina II) neurons to elucidate the cellular basis for its antinociceptive effects. However, the complicated types and local circuits of interneurons in the SG make it difficult to understand the real effects of EM2...
March 15, 2018: Neuro-Signals
Stephen R Humble, Nicolas Varela, Asantha Jayaweera, Arun Bhaskar
PURPOSE OF REVIEW: Chronic postsurgical pain (CPSP) is an important and well recognized cause of much long-term suffering, which in some cases may be preventable and affects many people living with cancer. Unfortunately, general consensus is lacking as to how best reduce the risk of developing CPSP. RECENT FINDINGS: Cancer is now not always a short-lived, fatal disease and is now moving towards a chronic illness. Poorly managed perioperative pain is the greatest risk factor for CPSP...
March 16, 2018: Current Opinion in Supportive and Palliative Care
Jennifer Luk, Yong Lu, Amanda Ackermann, Xiaoxue Peng, Diane Bogdan, Michelino Puopolo, David E Komatsu, Simon Tong, Iwao Ojima, Mario J Rebecchi, Martin Kaczocha
Background: Metabolism of the endocannabinoid 2-arachidonoylglycerol (2-AG) yields arachidonic acid (AA), the precursor to proalgesic eicosanoids including prostaglandin E2 (PGE2 ). Diacylglycerol lipase β (DAGLβ) is an enzyme that synthesizes 2-AG and its inhibition reduces eicosanoid levels and produces antinociceptive effects in models of inflammatory pain. Here we test whether inhibition of DAGLβ produces antinociceptive effects in a model of postoperative pain. Methods: Rats were administered the selective DAGLβ inhibitor KT109 or vehicle and underwent plantar incision...
2018: Journal of Pain Research
Lígia Renata Rodrigues Tavares, Daniela Baptista-de-Souza, Azair Canto-de-Souza
It is well-known that the exposure of rodents to threatening environments [e.g., the open arm of the elevated-plus maze (EPM)] elicits pain inhibition. Systemic and/or intracerebral [e.g., periaqueductal gray matter, amygdala) injections of antiaversive drugs [e.g., serotonin (5-HT) ligands, selective serotonin reuptake inhibitors (SSRIs)] have been used to change EPM-open arm confinement induced antinociception (OAA). Here, we investigated (i) the role of the 5-HT1A and 5-HT2C receptors located in the amygdaloid complex on OAA as well as (ii) the effects of systemic pretreatment with fluoxetine (an SSRI) on the effects of intra-amygdala injections of 8-OH-DPAT (a 5-HT1A agonist) or MK-212 (a 5-HT2C agonist) on nociception in mice confined to the open arm or enclosed arm of the EPM...
March 13, 2018: Neuropharmacology
Alok Kumar Paul, Nuri Gueven, Nikolas Dietis
In current clinical practice, morphine is dosed in older patients based on patient-weight, with different calculations for adjustment. However, at present, neither clinical experience nor the literature offers a clear evidence base for the relationship between antinociception, behavioral effects and morphine administration in older patients. In this study, we compared the nociceptive response of 8 and 24 week old rats after subcutaneous administration of morphine per body weight and analyzed their behavior using an advanced multi-conditioning system...
March 13, 2018: Pharmacology, Biochemistry, and Behavior
Rita Turnaturi, Carmela Parenti, Orazio Prezzavento, Agostino Marrazzo, Paschalina Pallaki, Zafiroula Georgoussi, Emanuele Amata, Lorella Pasquinucci
The opioid pharmacological profile of cis -(-)- N -normetazocine derivatives is deeply affected by the nature of their N -substituents. Here, our efforts were focused on the synthesis and pharmacological evaluation of novel derivatives of the lead LP1, a multitarget opioid analgesic compound featuring an N -phenylpropanamido substituent. LP1 derivatives 5a - d and 6a - d were characterized by flexible groups at the N -substituent that allow them to reposition themselves relative to cis -(-)- N -normetazocine nucleus, thus producing different pharmacological profiles at the mu, delta and kappa opioid receptors (MOR, DOR and KOR) in in vitro and in vivo assays...
March 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Edgar Isaac Rojas-Bedolla, Jorge Luis Gutiérrez-Pérez, Mario Iván Arenas-López, Marco Martin González-Chávez, Juan Ramón Zapata-Morales, Claudia Leticia Mendoza-Macías, Candy Carranza-Álvarez, Juan José Maldonado-Miranda, Martha Alicia Deveze-Álvarez, Angel Josabad Alonso-Castro
ETHNOPHARMACOLOGICAL RELEVANCE: Celtis pallida Torr (Cannabaceae) is employed as a folk medicine for the treatment of inflammation, pain, skin infections, and diarrhea, among other diseases. AIM OF THE STUDY: The purpose of this work was to assess the chemical composition, the in vitro and in vivo toxicity, the antimicrobial, anti-inflammatory, antidiarrheal, antinociceptive, locomotor, and sedative effects of an ethanolic extract obtained from Celtis pallida aerial parts (CPE)...
March 12, 2018: Journal of Ethnopharmacology
Narges Pachenari, Hossein Azizi, Elmira Ghasemi, Maryam Azadi, Saeed Semnanian
During the past decades, the use/misuse of opioids has increased dramatically among adolescent population. It is now well acknowledged that various morphological and physiological changes occur in the brain during adolescence. During this critical period, brain development and maturation could be affected by several factors including stress, drug abuse, nutritional status, etc. Although studies on transgenerational effects of substances such as alcohol, nicotine, and cocaine have focused on both paternal and maternal drug exposure, most reports on transgenerational effects of morphine are restricted to maternal exposure...
April 2018: Behavioural Pharmacology
Xiaofeng Wang, Wei Wang, Wei Li, Zhiduo Niu, Qing Wang, Dianwen Zhang, Hui Li, Jincheng Wang
Local drug delivery systems have been proposed for the treatment of periodontitis, and Hylotelephium purpureum may be a suitable agent for use in such a system. The present study aimed to formulate a Hylotelephium purpureum gel (HPG) and evaluate the anti-inflammatory activity and antinociceptive effects of Hylotelephium purpureum and to assess the duration of action and efficacy of HPG in the treatment of experimental periodontitis in a KM mouse model. First, an acute toxicity study was performed, and secondly, xylene-induced mouse-ear edema, acetic acid-induced mouse peritoneal capillary permeability and carrageenan-induced hind-paw edema tests were used to investigate the anti-inflammatory activity of the gel...
April 2018: Biomedical Reports
Zachary Curry, Jenny Wilkerson, Deniz Bagdas, Sarah Kyte, Nipa Patel, Giulia Donvito, Mohammed A Mustafa, Justin Poklis, Micah Niphakis, Ku-Lung Hsu, Benjamin F Cravatt, David A Gewirtz, M Imad Damaj, Aron H Lichtman
Although paclitaxel effectively treats various cancers, its debilitating peripheral neuropathic pain side effects often persist long after treatment has ended. Therefore, a compelling need exists for the identification of novel pharmacologic strategies to mitigate this condition. As inhibitors of monoacylglycerol lipase (MAGL), the primary hydrolytic enzyme of the endogenous cannabinoid 2-arachidonyolglycerol, produce antinociceptive effects in numerous rodent models of pain, we investigated whether inhibitors of this enzyme (i...
March 14, 2018: Journal of Pharmacology and Experimental Therapeutics
Kelly Barbosa Gama, Dourivaldo Silva Santos, Afrânio Ferreira Evangelista, Daniela Nascimento Silva, Adriano Costa de Alcântara, Ricardo Ribeiro Dos Santos, Milena Botelho Pereira Soares, Cristiane Flora Villarreal
Neuropathic pain is a type of chronic pain caused by injury or dysfunction of the nervous system, without effective therapeutic approaches. Mesenchymal stromal cells (MSCs), through their paracrine action, have great potential in the treatment of this syndrome. In the present study, the therapeutic potential of MSC-derived conditioned medium (CM) was investigated in a mouse model of neuropathic pain induced by partial sciatic nerve ligation (PSL). PSL mice were treated by endovenous route with bone marrow-derived MSCs (1 × 106 ), CM, or vehicle...
2018: Stem Cells International
István Z Bátai, Ádám Horváth, Erika Pintér, Zsuzsanna Helyes, Gábor Pozsgai
Transient receptor potential ankyrin 1 (TRPA1) non-selective ligand-gated cation channels are mostly expressed in primary sensory neurons. Polysulfides (POLYs) are Janus-faced substances interacting with numerous target proteins and associated with both protective and detrimental processes. Activation of TRPA1 in sensory neurons, consequent somatostatin (SOM) liberation and action on sst4 receptors have recently emerged as mediators of the antinociceptive effect of organic trisulfide dimethyl trisulfide (DMTS)...
2018: Frontiers in Endocrinology
Michael D Raleigh, Megan Laudenbach, Federico Baruffaldi, Samantha J Peterson, Michaela J Roslawski, Angela K Birnbaum, Frank I Carroll, Scott P Runyon, Scott Winston, Paul R Pentel, Marco Pravetoni
Heroin and oxycodone abuse occurs over a wide range of drug doses and by various routes of administration characterized by differing rates of drug absorption. The current study addressed the efficacy of a heroin vaccine (M-KLH) or oxycodone vaccine (OXY-KLH) for reducing drug distribution to brain after i.v. heroin or oxycodone, or s.c. oxycodone. Rats immunized with M-KLH or KLH control received an i.v. bolus dose of 0.26 or 2.6 mg/kg heroin. Vaccination with M-KLH increased retention of heroin and its active metabolites 6-acetylmorphine (6-AM) and morphine in plasma compared to KLH controls, and reduced total opioid (heroin + 6-AM + morphine) distribution to brain but only at the lower heroin dose...
March 13, 2018: Journal of Pharmacology and Experimental Therapeutics
Paloma T Birmann, Fernanda S S Sousa, Daniela H de Oliveira, Micaela Domingues, Beatriz M Vieira, Eder J Lenardão, Lucielli Savegnago
Several pathologies, such as pain and inflammation, are modulated by different pathways, making it necessary to develop drugs capable of modulating different pathways. Based on that, we investigated the antinociceptive and anti-inflammatory effect of 3-(4-chlorophenylselanyl)-1-methyl-1H-indole (CMI), as well as the systems involved in these actions. This study evaluated the antinociceptive and anti-inflammatory effects of CMI [0.0001-10mg/kg administered intragastrically (i.g.)] in the formalin, glutamate, hot plate, ear edema induced by croton oil and paw edema induced by formalin tests...
March 10, 2018: European Journal of Pharmacology
Leandro G Franco, Carlos Henrique M Wilges, Daniel P Junior, Sofia A Cerejo, Lilian T Nishimura, Isabela P Bittar
OBJECTIVE: To evaluate the effects of ketamine continuous rate infusions (CRI) at two dose rates on cardiovascular function and serum creatine kinase MB isoenzyme (CK-MB) and troponin I in healthy conscious dogs. STUDY DESIGN: Experimental, prospective, crossover, randomized, blinded study. ANIMALS: Eight adult mixed-breed dogs, aged 6±1 years and weighing 19±8.6 kg (mean±standard deviation). METHODS: Dogs were administered an intravenous bolus of ketamine (0...
December 18, 2017: Veterinary Anaesthesia and Analgesia
Karl Messlinger
BACKGROUND: Calcitonin gene-related peptide (CGRP) has long been a focus of migraine research, since it turned out that inhibition of CGRP or CGRP receptors by antagonists or monoclonal IgG antibodies was therapeutic in frequent and chronic migraine. This contribution deals with the questions, from which sites CGRP is released, where it is drained and where it acts to cause its headache proliferating effects in the trigeminovascular system. RESULTS: The available literature suggests that the bulk of CGRP is released from trigeminal afferents both in meningeal tissues and at the first synapse in the spinal trigeminal nucleus...
March 12, 2018: Journal of Headache and Pain
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