Abstract：
PURPOSE:To determine the correlation among progesterone dose, rate of import of progesterone-occupied progesterone receptor (PR) complexes into the nucleus of cells, and transcriptional activity of progesterone-PR complexes. METHODS:Live cell imaging and time-lapse microscopy of green fluorescent protein-tagged PR were performed to measure the rate of import into the nucleus of progesterone-PR complexes. To measure transcriptional activity, a progesterone-PR-sensitive luciferase reporter gene assay was used. RESULTS:For low doses of progesterone, there was a correlation among dose, import into the nucleus, and transcriptional activity. At higher doses of progesterone (beyond 12.5 nM), transcriptional activity increased, but there was no further increase in the rate of import, indicating a saturation of the import machinery. In both cases, a simple one-compartment model was sufficient to describe the import data. CONCLUSIONS:At low doses, progesterone dose correlates well with rate of import and transcriptional activity. At high doses, more progesterone can get into the nucleus and can activate unoccupied receptors already in the nucleus, leading to higher transactivation than would be expected from rates of import of progesterone-PR complexes into the nucleus.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Li H,Yan G,Kern SE,Lim CSdoi
10.1023/a:1026127015761subject
Has Abstractpub_date
2003-10-01 00:00:00pages
1574-80issue
10eissn
0724-8741issn
1573-904Xjournal_volume
20pub_type
杂志文章abstract：:A new transdermal therapeutic system (TTS) for nitroglycerin is presented that controls release of the active substance by means of desorption and diffusion. The drug release, in the dosage range examined under sink conditions, is independent of electrolytes and pH of the aqueous acceptor medium, but it does depend on...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016361921803
更新日期：1985-01-01 00:00:00
abstract：PURPOSE:The purpose of this study was to evaluate the feasibility of delivering vapreotide, a somatostatin analogue, by transdermal iontophoresis. METHODS:In vitro experiments were conducted using dermatomed porcine ear skin and heat-separated epidermis. In addition to quantifying vapreotide transport into and across ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-5276-6
更新日期：2005-08-01 00:00:00
abstract：PURPOSE:To employ in vitro experiments combined with computational fluid dynamics (CFD) analysis to determine which aerodynamic factors were most responsible for deaggregating carrier-free powders to form micrometer and submicrometer aerosols from a capsule-based platform. METHODS:Eight airflow passages were evaluated...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1001-z
更新日期：2013-06-01 00:00:00
abstract：PURPOSE:This study was carried out to examine the blood-brain barrier (BBB) transport of human basic fibroblast growth factor (bFGF) and investigate its mechanism. METHODS:The BBB transport of 125I-bFGF was measured by several in vivo methods including intravenous administration, in situ internal carotid artery perfus...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007570509232
更新日期：2000-01-01 00:00:00
abstract：:Nanoparticles, including lipopolyamines leading to lipoplexes, liposomes, and polyplexes are targeted drug carrier systems in the current search for a successful delivery system for polynucleic acids. This review is focused on the impact of gene and siRNA delivery for studies of efficacy, pharmacodynamics, and pharmac...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-008-9646-8
更新日期：2009-01-01 00:00:00
abstract：PURPOSE:For determination of the transit time through various parts of the gastrointestinal (GI) tract, we developed a method that provides the location of disintegration and drug release. This method involves GI magnetomarkergraphy (GIMG) using a 129-channel Shimadzu vector biomagnetic measurement system (BMS). METHO...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章
doi：10.1023/a:1007561129221
更新日期：2000-02-01 00:00:00
abstract：:A new technique has been developed to calculate rapidly the solid-state room-temperature degradation rate of drugs and drug candidates. The technique utilizes measurements of the initial rate of heat output at several elevated temperatures by isothermal calorimetry and the degradation rate of the compound determined a...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015865319250
更新日期：1992-07-01 00:00:00
abstract：PURPOSE:To investigate in vitro if P-glycoprotein (P-gp) transport can differentiate between antibiotic drugs exhibiting increased active renal clearance (CL(r)) in cystic fibrosis (CF) patients (i.e., dicloxacillin, trimethoprim) and drugs that do not exhibit this phenomenon (i.e.. cefsulodin, sulfamethoxazole). METH...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015191511817
更新日期：2002-04-01 00:00:00
abstract：PURPOSE:Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune response...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2180-9
更新日期：2017-08-01 00:00:00
abstract：PURPOSE:One of the drawbacks of polycationic and cationic liposomal gene transfer is its sensitivity to serum. Gene therapy requires the transfectant-DNA complex to be resistant to serum as well as blood. Since Ca2+ has proved to be an efficient cofactor of polycationic gene transfer, we decided to investigate its effe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007581700996
更新日期：2000-02-01 00:00:00
abstract：PURPOSE:Our previous studies indicated that drug leaked from discoidal reconstituted high density lipoprotein (d-rHDL) during the remodeling behaviors induced by lecithin cholesterol acyl transferase (LCAT) abundant in circulation, thus decreasing the drug amount delivered into the target. In this study, arachidonic ac...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1273-3
更新日期：2014-07-01 00:00:00
abstract：PURPOSE:To develop a non-viral gene delivery system in the form of an oil-in-water (o/w) lipid emulsion. METHOD:Cationic lipid emulsions were formulated with soybean oil, 1,2-dioleoyl-sn-glycero-3-trimethylammonium-propane (DOTAP) as a cationic emulsifier and other co-emulsifiers. The physical characteristics of the l...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007553106681
更新日期：2000-03-01 00:00:00
abstract：:Leucine enkephalin (YGGFL) undergoes rapid degradation in sheep nasal mucosa to yield GGFL which is further degraded to FL. The activity of the nasal mucosal homogenate against YGGFL and GGFL (t1/2 12 and 7 min) was significantly greater than that observed with a nasal wash fluid (t1/2 40 and 13 min). The effect of cy...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018946829225
更新日期：1994-12-01 00:00:00
abstract：PURPOSE:The purpose of the present study is to explore whether a poly-L-arginine (poly-L-Arg)-induced increase in tight junctions (TJ) permeability of fluorescein isothiocyanate-labeled dextran (MW 4.4 kDa, FD-4) is associated with the Ca2+-dependent signaling and occurs following the phosphorylation/dephosphorylation ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000003383.86238.d1
更新日期：2003-11-01 00:00:00
abstract：:A new enteric-coated formulation of sodium ursodeoxycholate was prepared and administered to man. The barrier film disintegrates and releases the drug only at pH > or = 5.5. The sodium salt of glycoursodeoxycholate was also prepared and encapsulated like ursodeoxycholate. Serum levels of ursodeoxycholate and glycourso...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018907825281
更新日期：1994-05-01 00:00:00
abstract：PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011913723928
更新日期：1998-07-01 00:00:00
abstract：PURPOSE:To quantitatively compare in vitro dissolution data in biorelevant and compendial media, to investigate whether in vitro differences are reflected in the simulated plasma profile and to specify under which circumstances prediction of the plasma profile of orally administered lipophilic drugs can be achieved. M...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011071401306
更新日期：2001-03-01 00:00:00
abstract：PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016243706415
更新日期：1995-10-01 00:00:00
abstract：PURPOSE:The heparin-paclitaxel conjugates using amino acid as linker (HD2), with low anticoagulant activity, the similar anticancer activity as paclitaxel, offer great potential for further investigation. METHODS:Two types of heparin-paclitaxel conjugates (HD) have been developed, in which O-acetylated heparin as carr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9762-5
更新日期：2009-04-01 00:00:00
abstract：PURPOSE:Anticancer chemotherapy usually involves the administration of several anticancer drugs that differ in their action mechanisms. Here, we aimed to test whether the combination of omacetaxine mepesuccinate (OMT) and doxorubicin (DOX) could show synergism, and whether the liposomal co-delivery of these two drugs c...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1317-3
更新日期：2014-08-01 00:00:00
abstract：PURPOSE:Pulmonary antibiotic delivery is recommended as maintenance therapy for cystic fibrosis (CF) patients who experience chronic infections. However, abnormally thick and sticky mucus present in the respiratory tract of CF patients impairs mucus penetration and limits the efficacy of inhaled antibiotics. To overcom...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1921-5
更新日期：2016-08-01 00:00:00
abstract：PURPOSE:To describe the pharmacokinetics of SK&F 107647, a synthetic hematoregulatory peptide, in healthy volunteers and in patients with adenocarcinoma. METHODS:SK&F 107647 pharmacokinetics were evaluated in 2 dose-escalation studies. Volunteers received SK&F 107647 as single 15-minute iv infusion doses of 1, 10, 100...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007512617139
更新日期：2000-04-01 00:00:00
abstract：PURPOSE:The aim of the present study was to design a new mucosal drug delivery system composed of liposomes dispersed within a bioadhesive hydrogel containing methyl-beta-cyclodextrin (Me(beta)CD) for controlled drug release. METHODS:A hydrophilic model molecule, inulin, was encapsulated within positively charged and ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-4591-2
更新日期：2005-06-01 00:00:00
abstract：PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016051600828
更新日期：1996-05-01 00:00:00
abstract：:An alternative procedure for the simultaneous determination of trimethoprim and sulfamethoxazole in an intravenous pharmaceutical formulation is presented. Infrared spectra of 14 calibration and 6 validation samples were collected using Fourier transform-infrared/attenuated total reflectance (FT-IR/ATR). Partial least...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015957632242
更新日期：1989-07-01 00:00:00
abstract：PURPOSE:The major objectives of this study were to 1) develop a new mathematical model describing all phases of drug release from bioerodible microparticles; 2) evaluate the validity of the theory with experimental data; and 3) use the model to elucidate the release mechanisms in poly(lactide-co-glycolide acid)-based m...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1021457911533
更新日期：2002-12-01 00:00:00
abstract：PURPOSE:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GF...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016100715125
更新日期：2002-06-01 00:00:00
abstract：PURPOSE:We present a smart intradermal interface suitable for skin-attached drug delivery devices. Our solution enables injections or infusions that are less invasive compared to subcutaneous injections and are leakage-free at the location of penetration. METHODS:The intradermal interface is based on a 31-gauge cannul...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0319-z
更新日期：2011-03-01 00:00:00
abstract：:Interleukin-1 receptor antagonist (IL-1Ra) is a naturally occurring anti-inflammatory antagonist of interleukin-1 family of pro-inflammatory cytokines. The broad spectrum anti-inflammatory effects of IL-1Ra have been investigated against various auto-immune diseases such as diabetes mellitus, rheumatoid arthritis. Des...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-013-1118-0
更新日期：2013-11-01 00:00:00
abstract：PURPOSE:The purpose of this study was (i) to develop glancing angle x-ray powder diffractometry (XRD) as a method for profiling phase transformations as a function of tablet depth; and (ii) to apply this technique to (a) study indomethacin crystallization during dissolution of partially amorphous indomethacin tablets a...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000012163.89163.f8
更新日期：2004-01-01 00:00:00
