Read by QxMD icon Read


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
Jenny L Wilkerson, Zachary A Curry, Pamela D Kinlow, Brittany L Mason, Ku-Lung Hsu, Mario van der Stelt, Benjamin F Cravatt, Aron H Lichtman
A great need exists for the identification of new effective analgesics to treat sustained pain. However, most preclinical nociceptive assays measure behavioral responses evoked by noxious stimuli (i.e., pain-stimulated behavior), which presents a challenge to distinguish between motor impairing and antinociceptive effects of drugs. Here, we demonstrate that chronic constriction injury of the sciatic nerve (CCI) elicits common pain-stimulated responses (i.e., mechanical allodynia and thermal hyperalgesia) as well as reduces marble burying/digging behaviors that occur during the early stages of the neuropathy and resolve within one week...
March 8, 2018: Pain
N Dietis, H Niwa, R Tose, J McDonald, V Ruggieri, M Filaferro, G Vitale, L Micheli, C Ghelardini, S Salvadori, G Calo, R Guerrini, D J Rowbotham, D G Lambert
BACKGROUND AND PURPOSE: Targeting more than one opioid receptor type simultaneously may have analgesic advantages in reduced side effect profile. We have evaluated the mixed MOP (μ, mu) agonist/DOP (δ, delta) antagonist UFP-505 in vitro and in vivo. EXPERIMENTAL APPROACH: We measured receptor density and function in single MOP, DOP and MOP/DOP double expression systems. GTPγ35 S binding, cAMP formation and arrestin recruitment were measured. Antinociceptive activity was measured in vivo using tail withdrawal and paw pressure tests following acute and chronic treatment...
March 10, 2018: British Journal of Pharmacology
Hiba Natsheh, Elka Touitou
The goal of this work was to investigate a new nasal carrier for enhanced drug delivery to brain, we call Phospholipid Magnesome. The system contains soft phospholipid vesicles, composed of phospholipid, water, propylene glycol, magnesium salt, and the mucoadhesive polymer, alginate. The carrier was characterized by various methods: electron microscopy, calorimetry, and dynamic light scattering. The ability of the carrier's vesicles to entrap various molecules was studied by CLSM and ultracentrifugation combined with HPLC quantification...
March 9, 2018: Drug Delivery and Translational Research
Tamires Rocha Falcão, Aurigena Antunes de Araújo, Luiz Alberto Lira Soares, Rhayanne Thaís de Moraes Ramos, Isabelle Cristinne Ferraz Bezerra, Magda Rhayanny Assunção Ferreira, Manoel André de Souza Neto, Maria Celeste Nunes Melo, Raimundo Fernandes de Araújo, Andreza Conceição Véras de Aguiar Guerra, Juliana Silva de Medeiros, Gerlane Coelho Bernardo Guerra
BACKGROUND: This study showed phytochemical composition and evaluates the anti-inflammatory, and analgesic activities of crude extract (CE) and fractions from E. uniflora Linn leaves. METHODS: Polyphenols present in crude extract (CE), in aqueous fraction (AqF), and ethyl acetate (EAF) treated fractions from E. uniflora Linn leaves were shown by chromatographic analysis in order to conduct a phytochemical characterization. Antibacterial activity was evaluated based on minimum inhibitory concentrations (MICs) determined using the agar dilution method...
March 9, 2018: BMC Complementary and Alternative Medicine
M Barletta, S M Ostenkamp, A C Taylor, J Quandt, B D X Lascelles, K M Messenger
Buprenorphine is a partial μ agonist opioid used for analgesia in dogs. An extended-release formulation (ER-buprenorphine) has been shown to provide effective analgesia for 72 hr in rats and mice. Six healthy mongrel dogs were enrolled in a randomized, blinded crossover design to describe and compare the pharmacokinetics and pharmacodynamics of ER-buprenorphine administered subcutaneous at 0.2 mg/kg (ER-B) and commercially available buprenorphine for injection intravenously at 0.02 mg/kg (IV-B). After drug administration, serial blood samples were collected to measure plasma buprenorphine concentrations using liquid chromatography/mass spectrometry detection...
March 9, 2018: Journal of Veterinary Pharmacology and Therapeutics
Damiana Scuteri, Laura Rombola, Laura Tridico, Hirokazu Mizoguchi, Chizuko Watanabe, Tsukasa Sakurada, Shinobu Sakurada, Maria TIziana Corasaniti, Giacinto Bagetta, Luigi Antonio Morrone
1.1. BACKGROUND: Alzheimer's Disease (AD) accounts for approximately 50% of all cases of dementia and, in spite of the great effort for the development of disease-modifying drugs, a definitive treatment of cognitive impairment is not available yet. A perfect adherence to the current therapy of cognitive decline is needed for a better control of the disease and this is proven to reduce, though not completely abolish, the associated Behavioural and Psychological Symptoms of Dementia (BPSDs) from occurring...
March 6, 2018: Current Medicinal Chemistry
Catherine J A Williams, Aage K O Alstrup, Mads F Bertelsen, Heidi M Jensen, Cleo A C Leite, Tobias Wang
Alfaxalone is becoming a popular anesthetic for nonmammalian vertebrates, but the physiological effects of its administration remain largely unknown in these taxa. Therefore, the cardiovascular responses to a clinically relevant dose of alfaxalone (10 mg/kg) are reported in the bullfrog ( Lithobates catesbeianus), following intramuscular (IM) and intravascular (IV) administration (via a femoral artery catheter) and compared with an IV dose of propofol, another parenteral GABA (γ-aminobutyric acid) agonist in common veterinary use as an induction agent...
March 2018: Journal of Zoo and Wildlife Medicine: Official Publication of the American Association of Zoo Veterinarians
Md Shafiullah Shajib, Ridwan B Rashid, Long C Ming, Shanta Islam, Md Moklesur R Sarker, Lutfun Nahar, Satyajit D Sarker, Bidyut K Datta, Mohammad A Rashid
Polymethoxylavones (PMFs) are known to exhibit significant anti-inflammatory and neuroprotective properties. Nicotiana plumbaginifolia , an annual Bangladeshi herb, is rich in polymethoxyflavones that possess significant analgesic and anxiolytic activities. The present study aimed to determine the antinociceptive and neuropharmacological activities of polyoxygenated flavonoids namely- 3,3',5,6,7,8-hexamethoxy-4',5'-methylenedioxyflavone ( 1 ), 3,3',4',5',5,6,7,8-octamethoxyflavone (exoticin) ( 2 ), 6,7,4',5'-dimethylenedioxy-3,5,3'-trimethoxyflavone ( 3 ), and 3,3',4',5,5',8-hexamethoxy-6,7-methylenedioxyflavone ( 4 ), isolated and identified from N...
2018: Frontiers in Pharmacology
Justin N Siemian, Shushan Jia, Jian-Feng Liu, Yanan Zhang, Jun-Xu Li
Chronic pain is a significant public health problem with a lack of safe and effective analgesics. The imidazoline I2 receptor (I2 R) is a promising analgesic target, but the neuroanatomical structures involved in mediating I2 R-associated behaviors are unknown. I2 Rs are enriched in the arcuate nucleus, dorsal raphe (DR), interpeduncular nucleus, lateral mammillary body, medial habenula, nucleus accumbens (NAc), and paraventricular nucleus, thus this study investigated the antinociceptive and hypothermic effects of microinjections of the I2 R agonist 2-(2-benzofuranyl)-2-imidazoline hydrochloride (2-BFI)...
March 7, 2018: European Journal of Neuroscience
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"