Abstract:
:The effects of tertiary amine-containing basic drugs on the enzymes located in the mitochondria and the effect of monoamine oxidase inhibitors (MAOIs) on drug accumulation in lung mitochondria have been studied. Various basic drugs inhibited MAO activity but not other mitochondrial marker enzymes. The potency of MAO inhibition correlated well with their lipid solubility, and the basic drugs inhibited MAO activity dose dependently and competitively. Further, MAO inhibition correlated well with binding affinity to lung mitochondria, and the binding of tertiary amine drugs to lung mitochondria was decreased by treatment with MAOIs. A good correlation was observed between the potency of MAOIs to inhibit the binding of the basic drug to the high-affinity site in mitochondria and the MAO inhibitory activity in mitochondria. These results indicate that mitochondrial MAO is one of the binding sites for tertiary basic drugs in the lung. We think that the action and/or adverse reaction of some drugs may result from inhibition of mitochondrial MAO to metabolize various biogenic amines and that mitochondrial MAO may function as a reservoir for basic drugs.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Yoshida H,Kamiya A,Okumura K,Hori Rdoi
10.1023/a:1015964623098subject
Has Abstractpub_date
1989-10-01 00:00:00pages
877-82issue
10eissn
0724-8741issn
1573-904Xjournal_volume
6pub_type
杂志文章abstract:PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2249-5
更新日期:2017-12-01 00:00:00
abstract::We describe an assay for acrolein in urine, employing derivatization with m-aminophenol in the presence of ferrous sulfate solution in sulfuric acid. The derivative (7-OH quinoline; DER) and the internal standard (quinine-bisulfate; IS) were separated on a 10-micron particle, 8 mm x 10-cm C18 cartridge in conjunction ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018964401677
更新日期:1993-11-01 00:00:00
abstract:PURPOSE:The purpose of this study was to assess the antifungal activity and renal and hepatic toxicity of amphotericin B (AmpB) following administration of Fungizone (FZ) and a heat-treated form of FZ (HFZ) to rats infected with Aspergillus fumigatus. METHODS:Infected rats were administered FZ and HFZ at a dosing regi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000041449.46054.b4
更新日期:2004-09-01 00:00:00
abstract::The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015840320410
更新日期:1991-05-01 00:00:00
abstract::A new method of analysis for the antihypertensive drug, hydralazine, is introduced. The assay involves the addition of p-nitrobenzaldehyde to blood samples containing hydralazine, to form a stable Schiff's base, hydralazine p-nitrobenzaldehyde hydrazone. The derivative is extracted from the blood into hexane and the s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015915812987
更新日期:1988-06-01 00:00:00
abstract:PURPOSE:This study examined the rheological and textural characteristics (hardness, compressibilty, adhesiveness and cohesiveness) of bioadhesive oral gels containing the antimicrobial agent chlorhexidine. METHODS:Textural analysis was performed using a Stable Micro Systems texture analyser (model TA-XT 2) in texture ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012091231023
更新日期:1997-04-01 00:00:00
abstract:PURPOSE:Fusogenic liposomes (FLs) are unique delivery vehicles capable of introducing their contents directly into the cytoplasm with the aid of envelope glycoproteins of Sendai virus (SeV). The objective of this study was to evaluate the potential of FL to improve the mucosal absorption of insulin from rat intestinal ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-9175-7
更新日期:2006-02-01 00:00:00
abstract:PURPOSE:To identify the aggregation mechanism and the stability characteristics of three different monoclonal antibodies under acidic conditions. METHODS:The aggregation kinetics is analyzed by a combination of light scattering, size exclusion chromatography and fluorescence techniques and the aggregation data are cor...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0885-3
更新日期:2013-03-01 00:00:00
abstract:PURPOSE:The purpose of the present study was to investigate changes of blood-brain barrier (BBB) and brain parenchymal protein expression due to type II diabetes mellitus (T2DM) induced by a high-fat diet (HFD) by using SWATH-based quantitative proteomics. METHODS:Mice were fed a HFD for 2 or 10 weeks, and then SWATH-...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2674-8
更新日期:2019-07-31 00:00:00
abstract:PURPOSE:To investigate the potential of chitosan nanoparticles as a system for improving the systemic absorption of insulin following nasal instillation. METHODS:Insulin-loaded chitosan nanoparticles were prepared by ionotropic gelation of chitosan with tripolyphosphate anions. They were characterized for their size a...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018908705446
更新日期:1999-10-01 00:00:00
abstract:PURPOSE:The organic cation transporters (OCTs) and multidrug and toxin extrusions (MATEs) together are regarded as an organic cation transport system critical to the disposition and response of many organic cationic drugs. Patient response to the analgesic morphine, a characterized substrate for human OCT1, is highly v...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2526-y
更新日期:2018-10-25 00:00:00
abstract::Cyclosporine (CsA) is commercially available for oral administration as a solution in olive oil with alcohol and an emulsifier. To improve its variable absorption and low patient acceptability, several oral formulations were prepared and tested in vitro and in vivo in dogs. A tablet formulation prepared by direct comp...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015815614959
更新日期:1991-04-01 00:00:00
abstract:PURPOSE:To improve the delivery of liposomes to tumors using P-selectin glycoprotein ligand 1 (PSGL1) mediated binding to selectin molecules, which are upregulated on tumorassociated endothelium. METHODS:PSGL1 was orientated and presented on the surface of liposomes to achieve optimal selectin binding using a novel st...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0875-5
更新日期:2013-02-01 00:00:00
abstract:PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000033016.36825.2c
更新日期:2004-07-01 00:00:00
abstract:PURPOSE:To measure the diffusion of nanometer polymersomes through tissue engineered human oral mucosa. METHODS:In vitro models of full thickness tissue engineered oral mucosa (TEOM) were used to assess the penetration properties of two chemically different polymersomes comprising two of block copolymers, PMPC-PDPA an...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9882-6
更新日期:2009-07-01 00:00:00
abstract:PURPOSE:Locoregional recurrence is the most common complication after adenocarcinoma resection in the colon, despite adjuvant chemotherapy. Therapy efficacy could be improved if designed to target malignant cells by incorporating specific recognition factors in the drugs or the drug vehicles. The aim of this study was ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9330-4
更新日期:2008-02-01 00:00:00
abstract::The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016292232513
更新日期:1995-03-01 00:00:00
abstract:PURPOSE:Within-subject dependency of observations has a strong impact on the evaluation of population pharmacokinetic (PK) and/or pharmacodynamic (PD) models. To our knowledge, none of the current model evaluation tools correctly address this issue. We present a new method with a global test and easy diagnostic plot wh...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0422-9
更新日期:2011-08-01 00:00:00
abstract:PURPOSE:This study examines methylprednisolone (MPL) effects on the dynamics of hepatic low-density lipoprotein receptor (LDLR) mRNA and plasma lipids associated with increased risks for atherosclerosis. MATERIALS AND METHODS:Normal male Wistar rats were given 50 mg/kg MPL intramuscularly (IM) and sacrificed at variou...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9371-8
更新日期:2008-04-01 00:00:00
abstract:PURPOSE:Monoamine oxidases (MAOs) are non-CYP enzymes that contribute to systemic elimination of therapeutic agents, and localized on mitochondrial membranes. The aim of the present study was to validate quantitative estimation of metabolic clearance of MAO substrate drugs using human liver microsomes (HLMs). METHODS:...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2140-4
更新日期:2017-06-01 00:00:00
abstract::Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-020-02818-8
更新日期:2020-06-03 00:00:00
abstract::Seven healthy, male volunteers were entered into a randomized, open crossover study of the gastrointestinal transit of two enteric-coated 500-mg naproxen tablets. Two radiolabeled tablets were given to each volunteer on two occasions separated by 7 days, once in the fasted state and once after breakfast. Radiolabeling...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1023/a:1015858829187
更新日期:1992-11-01 00:00:00
abstract:PURPOSE:Cationic liposomes are expected to be useful as nonviral vectors for gene delivery. Cationic liposomes showed cytotoxicity, and we proposed that the cytotoxicity is through apoptosis. In this study, we examined the effects of liposomal properties, such as liposomal charge, size, membrane fluidity, and PEG coati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1024441702398
更新日期:2003-07-01 00:00:00
abstract:BACKGROUND:With the recent approval of the first small interfering RNA (siRNA) therapeutic formulated as nanoparticles, there is increased incentive for establishing the factors of importance for the design of stable solid dosage forms of such complex nanomedicines. METHODS:The aims of this study were: (i) to identify...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2663-y
更新日期:2019-08-02 00:00:00
abstract:PURPOSE:Studies were conducted to investigate dilute solutions of the monoclonal antibody (mAb) bevacizumab, mAb fragment ranibizumab and fusion protein aflibercept, develop common procedures for formulation of low concentration mAbs and identify a stabilizing formulation for anti-VEGF mAbs for use in in vitro permeati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2368-7
更新日期:2018-02-28 00:00:00
abstract::To achieve time-controlled or site-specific drug delivery in the gastrointestinal tract, a sigmoidal release system (SRS) was developed, which achieved a prolonged lag time, followed by rapid release. The theophylline beads with a thick Eudragit RS film coating showed very low drug release in water, whereas the releas...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018910114436
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:Evista (raloxifene HCl) is a nonsteroidal selective estrogen receptor modulator that displays estrogen agonist effects on bone and lipid metabolism but estrogen antagonist effects on the breast and endometrium. The potential for drug-drug interaction between raloxifene and warfarin was assessed in 15 healthy po...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1010904815275
更新日期:2001-07-01 00:00:00
abstract:PURPOSE:The clinical utility of anthracyclines like idarubicin (IDA) is limited by the occurrence of multidrug resistance and cardiotoxicity. Previous studies have demonstrated that the multidrug transporter P-glycoprotein (P-gp) is present in the heart and have suggested that it exerts a protective function. We sought...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1013022212738
更新日期:2001-11-01 00:00:00
abstract:PURPOSE:In this study, we aimed to illustrate the utility of fractional radiofrequency (RF) that generated microchannels in the skin, allowing delivery of peptide and siRNA via the skin. The mechanisms involved in the correlation between macromolecule permeation and skin structure were also elucidated. METHODS:The mor...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1568-z
更新日期:2015-05-01 00:00:00
abstract:PURPOSE:The purpose of the current study is to evaluate the solubility advantage offered by celecoxib (CEL) amorphous systems and to characterize and correlate the physical and thermodynamic properties of CEL and its amorphous molecular dispersions containing poly(vinylpyrrolidone) (PVP). METHODS:The measurement of cr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000045226.42859.b8
更新日期:2004-10-01 00:00:00