Antinociceptive and Antihyperalgesic Activity of a Traditional Maya Herbal Preparation Composed of Pouteria Campechiana, Chrysophyllum Cainito, Citrus Limonum, and Annona Muricata
ABSTRACT
The purpose of this work was to assess the antinociceptive and antihyperalgesic properties of an herbal preparation, composed of four vegetal species: Pouteria campechiana (P. campechiana), Chrysophyllum cainito (C. cainito), Citrus limonum (C. limonum), and Annona muricata (A. muricata), that is commonly used in combination (PCCA) in traditional Mayan medicine for the treatment of diabetes and pain. An ethanolic extract of PCCA was prepared at a ratio of 1:1:1:1 for each plant. The systemic antinociceptive effect of PCCA extract (50–600 mg/kg, p.o.) was dose‐dependent in the rat formalin (1%) producing...
Source: Drug Development Research - February 7, 2017 Category: Drugs & Pharmacology Authors: Myrna D éciga‐Campos, Rolffy Ortiz‐Andrade, Amanda Sanchez‐Recillas, José Salvador Flores‐Guido, Mario A. Ramírez Camacho Tags: Research Article Source Type: research
Isobolographic Analyses of Proglumide –Celecoxib Interaction in Rats with Painful Diabetic Neuropathy
ABSTRACT
The aim of the present study was to analyze the antihyperalgesic and antiallodynic interaction between the non‐selective cholecystokinin (CCK) antagonist receptor, proglumide, and the selective cyclooxygenase‐2 inhibitor, celecoxib in streptozotocin (STZ)‐induced diabetic rats. Hyperalgesia was evaluated in the formalin test and tactile allodynia using von Frey filaments. Isobolographic analyses were employed to define the nature of the compound interactions, using a fixed dose ratio (0.5:0.5). Proglumide (20–160 mg/kg) and celecoxib (0.3–30 mg/kg) in these fixed dose ratio combinations induced do...
Source: Drug Development Research - February 1, 2017 Category: Drugs & Pharmacology Authors: Samuel Suarez ‐Mendez, Carlos A. Tovilla‐Zarate, Luis F. Ortega‐Varela, Deysi Y. Bermudez‐Ocaña, Jorge L. Blé‐Castillo, Thelma B. González‐Castro, Alma M. Zetina‐Esquivel, Juan C. Diaz‐Zagoya, Isela Esther Juárez‐Rojop Tags: Research Article Source Type: research
Antiallodynic Activity of Ceftriaxone and Clavulanic Acid in Acute Administration is Associated with Serum TNF ‐α Modulation and Activation of Dopaminergic and Opioidergic Systems
ABSTRACT
The aim of this study was to determine the antiallodynic effect of acute administration of the β‐lactam antimicrobials, ceftriaxone (CFX) and clavulanic acid (CLAV), for the control of established pain on a model of neuropathic pain (NP). We also investigated the involvement of dopaminergic and opioidergic pathways as well as alterations in serum concentrations of TNF‐α in the antiallodynic actions of these drugs. CFX, CLAV, or gabapentin (GAP), a reference drug, were administered i.p. twelve days after constriction of the sciatic nerve in rats. Mechanic and cold allodynia were evaluated for 3 h and a...
Source: Drug Development Research - February 1, 2017 Category: Drugs & Pharmacology Authors: A. Ochoa ‐Aguilar, M.A. Sotomayor‐Sobrino, R. Jaimez, R. Rodríguez, R. Plancarte‐Sánchez, R. Ventura‐Martinez Tags: Research Article Source Type: research
Antihyperalgesic Effects of Indomethacin, Ketorolac, and Metamizole in Rats: Effects of Metformin
In this study, the effect of local peripheral or systemic administration of metformin on the local peripheral or systemic antinociception induced by indomethacin, ketorolac and metamizole was assessed in the rat carrageenan‐induced thermal hyperalgesia model. Rats were injected with carrageenan (1%, 50 µl) into the right hindpaw which reduced paw withdrawal latency, a measure of thermal hyperalgesia. Local peripheral or systemic administration of indomethacin, ketorolac or metamizole dose‐dependently reduced carrageenan‐induced thermal hyperalgesia. Local peripheral pre‐treatment with metformin (800 µg/paw) parti...
Source: Drug Development Research - January 31, 2017 Category: Drugs & Pharmacology Authors: Crystell Guadalupe Guzm án‐Priego, Roberto Méndez‐Mena, Manuel Alfonso Baños‐González, Claudia Ivonne Araiza‐Saldaña, Gabriela Castañeda‐Corral, Jorge Elías Torres‐López Tags: Research Article Source Type: research
NS1209/SPD 502, A Novel Selective AMPA Antagonist for Stroke, Neuropathic Pain or Epilepsy? Drug Development Lessons Learned
ABSTRACT
The selective AMPA (α‐amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid) receptor antagonist, NS1209 (also known as SPD 502) has been explored in several research and development campaigns since its selection as a lead drug candidate in the early 1990s by the Danish biotechnology company, NeuroSearch. The compound was successively tested in animal models of stroke, neuropathic pain and epilepsy. The preclinical data to support development for the treatment of stroke were incomplete, as the compound was administered after the stroke episode, and did not protect subcortical areas of the brain....
Source: Drug Development Research - January 31, 2017 Category: Drugs & Pharmacology Authors: Jan M. Keppel Hesselink Tags: Miscellaneous Source Type: research
Morin Inhibits Proliferation, Migration, and Invasion of Bladder Cancer EJ Cells via Modulation of Signaling Pathways, Cell Cycle Regulators, and Transcription Factor ‐Mediated MMP‐9 Expression
In this study, we investigated the inhibitory activity of morin on bladder cancer EJ cells. Morin significantly inhibited EJ cell proliferation, which was related to the G1‐phase cell cycle arrest together with the reduced expression of cyclin D1, cyclin E, CDK2, and CDK4 via increased expression of p21WAF1. Morin also increased ERK1/2 phosphorylation and decreased JNK and AKT phosphorylation without altering the p38MAPK phosphorylation levels. Morin treatment suppressed the migration and invasion of EJ cells in wound‐healing and transwell cell invasion assays. Zymographic and electrophoretic mobility shift assays show...
Source: Drug Development Research - January 31, 2017 Category: Drugs & Pharmacology Authors: Seung ‐Shick Shin, Se Yeon Won, Dae‐Hwa Noh, Byungdoo Hwang, Wun‐Jae Kim, Sung‐Kwon Moon Tags: Research Article Source Type: research
Instruction to Authors
(Source: Drug Development Research)
Source: Drug Development Research - December 14, 2016 Category: Drugs & Pharmacology Tags: Instruction to Authors Source Type: research
Issue Information ‐TOC
(Source: Drug Development Research)
Source: Drug Development Research - December 14, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐TOC Source Type: research
The Antinociceptive Effect of a Tapentadol ‐Ketorolac Combination in a Mouse Model of Trigeminal Pain is Mediated by Opioid Receptors and ATP‐Sensitive K+ Channels
ABSTRACT
The aim of the present study was to evaluate the antinoceptive interaction between the opioid analgesic, tapentadol, and the NSAID, ketorolac, in the mouse orofacial formalin test. Tapentadol or ketorolac were administered ip 15 min before orofacial formalin injection. The effect of the individual drugs was used to calculate their ED50 values and different proportions (tapentadol‐ketorolac in 1:1, 3:1, and 1:3) were assayed in the orofacial test using isobolographic analysis and interaction index to evaluate the interaction between the drugs. The combination showed antinociceptive synergistic and additive...
Source: Drug Development Research - November 30, 2016 Category: Drugs & Pharmacology Authors: Israel Barreras ‐Espinoza, José Alberto Soto‐Zambrano, Nicolás Serafín‐Higuera, Ramón Zapata‐Morales, Ángel Alonso‐Castro, Ronell Bologna‐Molina, Vinicio Granados‐Soto, Mario A. Isiordia‐Espinoza Tags: Research Article Source Type: research
The Antinociceptive Effects of a Tapentadol ‐Ketorolac Combination in a Mouse Model of Trigeminal Pain is Mediated by Opioid Receptors and ATP‐Sensitive K+ Channels
ABSTRACT
The aim of the present study was to evaluate the antinoceptive interaction between the opioid analgesic, tapentadol, and the NSAID, ketorolac, in the mouse orofacial formalin test. Tapentadol or ketorolac were administered ip 15 min before orofacial formalin injection. The effect of the individual drugs was used to calculate their ED50 values and different proportions (tapentadol‐ketorolac in 1:1, 3:1, and 1:3) were assayed in the orofacial test using isobolographic analysis and interaction index to evaluate the interaction between the drugs. The combination showed antinociceptive synergistic and additive...
Source: Drug Development Research - November 30, 2016 Category: Drugs & Pharmacology Authors: Israel Barreras ‐Espinoza, José Alberto Soto‐Zambrano, Nicolás Serafín‐Higuera, Ramón Zapata‐Morales, Ángel Alonso‐Castro, Ronell Bologna‐Molina, Vinicio Granados‐Soto, Mario A. Isiordia‐Espinoza Tags: Research Article Source Type: research
Instruction to Authors
(Source: Drug Development Research)
Source: Drug Development Research - November 13, 2016 Category: Drugs & Pharmacology Tags: Instruction to Authors Source Type: research
Issue Information ‐TOC
(Source: Drug Development Research)
Source: Drug Development Research - November 13, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐TOC Source Type: research
Breaking Sad: Unleashing the Breakthrough Potential of Ketamine's Rapid Antidepressant Effects
ABSTRACT
The surprising results of a small clinical trial on the effects of low dose ketamine, a 65‐year old anesthetic drug that is also used off‐label for chronic pain and recreationally as a club drug, in eight depressed subjects unleashed the most significant advance in antidepressant drug development in decades. That study and subsequent ones have demonstrated that low dose, infused ketamine is able to induce a remission of depression in patients who have failed conventional medications, within 24 h. The apparent increased efficacy and rapid onset of effect of ketamine distinguish it from all other current ...
Source: Drug Development Research - October 31, 2016 Category: Drugs & Pharmacology Authors: David Feifel Tags: Research Overview Source Type: research
Synthesis of Five ‐ and Six‐Membered N‐Phenylacetamido Substituted Heterocycles as Formyl Peptide Receptor Agonists
ABSTRACT
Formyl peptide receptors (FPRs) are G‐protein‐coupled receptors that play an important role in the regulation of inflammatory process and cellular dysfunction. In humans, three different isoforms are expressed (FPR1, FPR2, and FPR3). FPR2 appears to be directly involved in the resolution of inflammation, an active process carried out by specific pro‐resolving mediators that modulate specific receptors. Previously, we identified 2‐arylacetamido pyridazin‐3(2H)‐ones as FPR1‐ or FPR2‐selective agonists, as well as a large number of mixed‐agonists for the three isoforms. Here, we report a new ...
Source: Drug Development Research - October 31, 2016 Category: Drugs & Pharmacology Authors: Claudia Vergelli, Igor A. Schepetkin, Giovanna Ciciani, Agostino Cilibrizzi, Letizia Crocetti, Maria Paola Giovannoni, Gabriella Guerrini, Antonella Iacovone, Liliya N. Kirpotina, Richard D. Ye, Mark T. Quinn Tags: Research Article Source Type: research
Fucoidan Induces ROS ‐Dependent Apoptosis in 5637 Human Bladder Cancer Cells by Downregulating Telomerase Activity via Inactivation of the PI3K/Akt Signaling Pathway
ABSTRACT
Fucoidan, a sulfated polysaccharide, is a compound found in various species of seaweed that has anti‐viral, anti‐bacterial, anti‐oxidant, anti‐inflammatory, and immunomodulatory activities; however, the underlying relationship between apoptosis and anti‐telomerase activity has not been investigated. Here, we report that fucoidan‐induced apoptosis in 5637 human bladder cancer cells was associated with an increase in the Bax/Bcl‐2 ratio, the dissipation of the mitochondrial membrane potential (MMP, Δψm), and cytosolic release of cytochrome c from the mitochondria. Under the same experimental c...
Source: Drug Development Research - September 20, 2016 Category: Drugs & Pharmacology Authors: Min Ho Han, Dae ‐Sung Lee, Jin‐Woo Jeong, Su‐Hyun Hong, Il‐Whan Choi, Hee‐Jae Cha, Suhkmann Kim, Heui‐Soo Kim, Cheol Park, Gi‐Young Kim, Sung‐Kwon Moon, Wun‐Jae Kim, Yung Hyun Choi Tags: Research Article Source Type: research
