Abstract：
PURPOSE:Gabapentin, a drug for neuropathic pain, exerts its therapeutic effect via inhibition of the a2d subunit of N-type Ca2+ channels. Thus, finding peptides that specifically displace gabapentin from its binding site may lead to the development of new drugs. METHODS:Displacement of bound [3H]-gabapentin in membrane preparations of rat cerebral cortex and of human Cav2.2/β3/α2δ1 expressed in CHO cell line. RESULTS:Neuropeptide FLFQPQRF-NH2 specifically displaced bound [3H]-gabapentin in membrane preparations from rats and CHO cells. Truncation of the C-terminus of FLFQPQRF-NH2 by three amino acid residues to produce FLFQP-NH2 improved the displacement of gabapentin. FLFQP-NH2 displaced bound [3H]-gabapentin with IC50 and Ki values of 2.7 µM and 1.7 µM, respectively. Deletion of two amino acid residues (FQ) in the middle of the FLFQP-NH2 sequence yielded FLP-NH2 that displaced bound [3H]-gabapentin with a lower affinity. IC50 and Ki values were 11.9 µM and 7.8 µM, respectively. Neutral binding cooperativity existed when of FLFQP-NH2, FLP- NH2 and gabapentin when incubated together. FLFQPQRF-NH2 but not FLFQP-NH2 displaced bound [3H]- gabapentin to membrane preparations of human Cav2.2/b3/a2d1 expressed in CHO cells. CONCLUSION:FLFQPQRF-NH2, FLFQP-NH2 and FLP-NH2 displace bound gabapentin in membrane preparations of rat cerebral cortex. Binding cooperativity was detected when GBP/FLFQP-NH2/FLP-NH2 were incubated together. These novel binding sites may provide new approaches to modulate L-type Ca2+ channels.
journal_name
J Pharm Pharm Sciauthors
Skubatz Hdoi
10.18433/jpps30358subject
Has Abstractpub_date
2019-01-01 00:00:00pages
292-300issue
1issn
1482-1826journal_volume
22pub_type
杂志文章abstract：PURPOSE:To investigate the suitability of an SCMC (sodium carboxymethyl cellulose/polyethylene glycol 400/carbopol 934P) and an HPMC (hydroxypropylmethyl cellulose/polyethylene glycol 400/carbopol 934P) films as drug vehicle for buccal delivery. METHODS:The mechanical and in vitro bioadhesive strength properties of th...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：1999-05-01 00:00:00
abstract：PURPOSE:The aim of this work was to prepare the stable water/oil/water multiple emulsions (MEs), to investigate the usage of poloxamine 908, to observe the influence of surfactant percentage on the properties of MEs. METHOD:MEs were prepared by liquid paraffin, cetyl dimethicone copolyol and poloxamine 908 by a two-st...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2005-08-11 00:00:00
abstract：PURPOSE:A high performance liquid chromatographic method was developed for the determination of glucosamine (GlcN) in rat plasma. METHOD:Internal standard, galactosamine, was added to 100 micro L of plasma containing GlcN followed by precipitation of plasma proteins with acetonitrile. Evaporation of the decanted super...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2002-05-01 00:00:00
abstract：:Hepatic clearance (CLh) of carvedilol (CAR), which is eliminated via stereoselective metabolism by the CYP2D subfamily of cytochromes P450 (CYPs), was predicted using liver microsomes and hepatocytes from Sprague-Dawley (SD) rats and CYP2D-deficient Dark Agouti (DA) rats to determine the usefulness of prediction metho...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/jpps30237
更新日期：2019-01-01 00:00:00
abstract：:Life-threatening fungal infections have increased dramatically in recent decades in immunocompromised patients. An estimated 40% of all deaths from hospital-acquired infections are due to infections caused by opportunistic fungi. The current treatment options are either causing serious toxicity, or becoming inactive a...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3h010
更新日期：2008-07-06 00:00:00
abstract：PURPOSE:Aim of this study is to investigate the mechanism of self-emulsification through rheological analysis of intermediate liquid crystalline (LC) phase formed during self-emulsification process. METHODS:Binary system of tween 80 (T80) and imwitor 742 (I742) was used and different SES were prepared with I742 at 10,...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j30w2p
更新日期：2009-01-01 00:00:00
abstract：PURPOSE:Comparison of the effects of one year treatment with sibutramine compared to placebo on insulin resistance parameters, body weight, glycemic control, and lipid profile, in type 2 diabetic patients. METHODS:Two hundred and forty-six patients with uncontrolled type 2 diabetes mellitus in therapy with different o...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,多中心研究,随机对照试验
doi：10.18433/j3388p
更新日期：2010-01-01 00:00:00
abstract：PURPOSE:Clinical studies have suggested that proton pump inhibitors may decrease levothyroxine absorption and an in vitro study suggested that the effect of pH on dissolution may differ with formulation. To determine the impact of formulation on the pharmacokinetics of levothyroxine in altered gastric pH conditions, th...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j36p5m
更新日期：2015-01-01 00:00:00
abstract：PURPOSE:The present study was undertaken to investigate the effect of plastic, hydrophilic and hydrophobic types of polymers and their content level on the release profile of drug from matrix systems. As the physico-chemical nature of the active ingredients influence the drug retarding ability of these polymers, three ...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2003-05-01 00:00:00
abstract：PURPOSE:The aim of this study was to correlate the relationship between the pharmacokinetic behaviors and the toxicity of a new investigational anticancer agent CZ48, a C20-propionate ester of camptothecin (CPT) in mice. METHODS:In this study, the safety and pharmacokinetics of oral doses of CZ48 were compared with th...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3b604
更新日期：2013-01-01 00:00:00
abstract：PURPOSE:To determine the merits of a robot at the community pharmacy in a quasi-experiment. METHOD:The applied methods for data-collection were barcode-time measurements, direct observations, time-interval studies, and tally at a Dutch community pharmacy. The topics consisted of workload, waiting times, congestion, sl...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2006-01-01 00:00:00
abstract：PURPOSE:To review microbial contamination rates about preparation of individual and batch doses using aseptic techniques within pharmaceutical (controlled) and clinical (ward and theatre) environments. METHODS:Systematic review, involving amalgamation of data using a random effect model and metaanalysis. RESULTS:A to...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,meta分析,评审
doi：10.18433/j3jp4b
更新日期：2009-01-01 00:00:00
abstract：:Alzheimer's disease (AD) is an irreversible neurodegenerative disease characterized by a progressive decline in cognition and memory, leading to significant impairment in daily activities and ultimately death. It is the most common cause of dementia, the prevalence of which increases with age; however, age is not the ...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,评审
doi：10.18433/J3VS8P
更新日期：2017-01-01 00:00:00
abstract：PURPOSE:The purpose of this work was to investigate the potential effectiveness of polaprezinc in the treatment of stomatitis. Its effect on oral mucous membrane lesions was studied focusing on acetic acid-induced stomatitis in an animal model. METHOD:Stomatitis was induced in hamsters by local injection of 30 microL ...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2000-01-01 00:00:00
abstract：PURPOSE:To examine the inhibitory effects of star fruit (Averrhoa carambola) juice towards seven major cytochrome P450 (CYP) isoforms and NADPH-cytochrome P450 reductase (CPR). METHODS:The inhibitory effects of star fruit juice (0.5 to 5%, v/v) against the activities of seven CYP isoforms including CYP1A2, CYP2A6, CYP...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j30593
更新日期：2007-01-01 00:00:00
abstract：PURPOSE:To synthesize current knowledge about the effectiveness and the magnitude of the effect, of Academic Detailing (AD), as a stand-alone intervention, at modifying drug prescription behavior of Family Physicians (FPs) in primary care settings. METHODS:A search of MEDLINE, EMBASE, CENTRAL, and Web of Science datab...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,评审
doi：10.18433/j3kk6c
更新日期：2013-01-01 00:00:00
abstract：PURPOSE:To determine the risk of clinical trial failure for drugs developed for type-2 diabetes. METHODS:Drugs were investigated by reviewing phase I to phase III studies that were conducted between 1998 and February 2013. The clinical trial success rates were calculated and compared to the industry standard. The drug...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3hg73
更新日期：2014-01-01 00:00:00
abstract：PURPOSE:To develop an HPLC method using fluorescence detection for the pharmacokinetic evaluation of levels of zabofloxacin, a novel broad spectrum fluoroquinolone antibiotic, in the plasma, bile and urine of rats. METHODS:A simple reversed-phase HPLC method using a C18 column with fluorescence detection was developed...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3j592
更新日期：2011-01-01 00:00:00
abstract：:Hypochlorhydria is a condition where the production of hydrochloric acid in the stomach is decreased. As a result, the intragastric pH is elevated. This condition can be due to a series of causes, such as disease (gastric mucosal infection caused by Helicobacter pylori and is prominent in AIDS patients), ethnicity, ag...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/jpps30227
更新日期：2018-01-01 00:00:00
abstract：PURPOSE:We have previously reported that the Australian Northern Kaanju (Kuuku I'yu) medicinal plant Dodonaea polyandra has anti-inflammatory activity. This is attributed largely to the presence of clerodane diterpenoids contained within the leaf resin. We envisaged developing a topical preparation to treat indications...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j38p57
更新日期：2015-01-01 00:00:00
abstract：PURPOSE:To examine the impact of adding droperidol to fentanyl-based intravenous patient- controlled analgesia (IVPCA) on the discontinuation of IVPCA use due to postoperative nausea and vomiting (PONV). METHODS:Patients who underwent surgeries other than abdominal surgeries and used IVPCA between April 2014 and March...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/jpps30902
更新日期：2020-01-01 00:00:00
abstract：PURPOSE:To study the effect of encapsulation of recombinant adenovirus type 5 encoding Beta-galactosidase (Ad5-Betagal) in poly (D,Llactic-co-glycolic acid) (PLGA) microspheres on viral delivery to professional antigen presenting cells (APCs) in vitro, viral dissemination in vivo, and induction of protective immune res...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2007-01-01 00:00:00
abstract：:This review discusses issues largely from the biological point of view about the targeted approaches for the use of natural products for the discovery of anti-diabetic drugs in collaboration with medicinal chemists and computer-aided drug design. A major thrust of this review reflects the collaborative research of fou...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,评审
doi：10.18433/j3t60g
更新日期：2013-01-01 00:00:00
abstract：PURPOSE:The preclinical pharmacokinetic and pharmacodynamic properties of a potent fluoroketolide RBx14255 against Streptococcus pneumoniae and Haemophilus influenzae was compared with telithromycin and human clinical dose was predicted for preclinical development. METHODS:The in vitro pharmacokinetic characterization...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/jpps30942
更新日期：2020-01-01 00:00:00
abstract：PURPOSE:To design a buccal mucoadhesive system for systemic delivery of acyclovir using a novel mucoadhesive, copolymers of acrylic acid and poly(ethylene glycol), and to determine the feasibility of transbuccal delivery of acyclovir using this system. METHODS:The buccal delivery system was prepared using an adhesive,...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：1998-05-01 00:00:00
abstract：PURPOSE:To systematically review and quantitatively synthesize associations between HLA genotypes and oxcarbazepine-induced cutaneous adverse drug reactions (OXC-cADRs), including Stevens-Johnson syndrome (SJS) and maculopapular rash. METHODS:Studies investigating associations between HLA genotypes and OXC-cADRs were ...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章,meta分析
doi：10.18433/J36S7D
更新日期：2018-01-01 00:00:00
abstract：PURPOSE:The purpose of our study was to optimize lipid-lowering therapy in patients undergoing coronary revascularization and to determine whether the percentage change in low-density lipoprotein-cholesterol (LDL-C) level in the 3 months after coronary revascularization could be used as a predictor of the time to recur...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3hg6q
更新日期：2010-01-01 00:00:00
abstract：PURPOSE:Concomitant use of nutraceuticals with chemotherapy is very common. Cancer patients self-medicate to relieve the side effects associated with chemotherapy, improve disease outcome and to regain control of their medical care. However, there is limited empirical evidence on potential drug-nutraceutical interactio...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3m30k
更新日期：2015-01-01 00:00:00
abstract：PURPOSE:The extent of palmitate uptake by hepatocytes is dependent upon the surface charge of the extracellular binding protein. Specifically, hepatocyte uptake is greater when palmitate is bound to cationic binding proteins than when it is bound to anionic proteins. To further understand the role of protein surface ch...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：10.18433/j3bc8w
更新日期：2012-01-01 00:00:00
abstract：PURPOSE:To predict Caco-2 permeability is a valuable target for pharmaceutical research. Most of the Caco-2 prediction models are based on commercial or special software which limited their practical value. This study represents the relationship between Caco-2 permeability and molecular descriptors totally based on ope...
journal_title：Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques
pub_type： 杂志文章
doi：
更新日期：2006-01-01 00:00:00
