Abstract:
:Transient receptor potential vanilloid 1 (TRPV1) is primarily expressed in central and peripheral terminals of non-myelinated primary afferent neurons. We previously showed that AS1928370, a novel TRPV1 antagonist that can prevent ligand-induced activation but not proton-induced activation, ameliorates neuropathic pain in rats without hyperthermic effect. In this study, we investigated its analgesic profile in mice. AS1928370 showed good oral bioavailability and high penetration into the brain and spinal cord in mice. The mean plasma-to-brain and plasma-to-spinal cord ratios were 4.3 and 3.5, respectively. Pretreatment with AS1928370 significantly suppressed both capsaicin-induced acute pain and withdrawal response in hot plate test at 10-30 mg/kg per os (p.o.). At lower oral doses (0.3-1.0 mg/kg), AS1928370 improved mechanical allodynia in mice undergoing spinal nerve ligation. Intrathecal administration of AS1928370 (30 µg/body) also significantly suppressed mechanical allodynia. In addition, AS1928370 showed no effect on locomotor activity up to 30 mg/kg p.o. These results suggest that spinal TRPV1 has an important role in the transmission of neuropathic pain and that the central nervous system (CNS) penetrant TRPV1 receptor antagonist AS1928370 is a promising candidate for treating neuropathic pain.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Watabiki T,Kiso T,Tsukamoto M,Aoki T,Matsuoka Ndoi
10.1248/bpb.34.1105subject
Has Abstractpub_date
2011-01-01 00:00:00pages
1105-8issue
7eissn
0918-6158issn
1347-5215pii
JST.JSTAGE/bpb/34.1105journal_volume
34pub_type
杂志文章abstract::The tumor microenvironment is one of the key factors contributing to the efficiency of drug delivery to a tumor. It has been reported that lymphangiogenesis is induced in certain tumors. Because the lymphatic system functions as a drainage one, it is possible that tumor lymphatic vessels alter not only the tumor micro...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b17-00730
更新日期:2018-01-01 00:00:00
abstract::As one of the adverse effects of oxaliplatin, a key agent in colon cancer chemotherapy, a taste disorder is a severe issue in a clinical situation because it decreases the quality of life of patients. However, there is little information on the mechanism underlying the oxaliplatin-induced taste disorder. Here, we exam...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b15-00935
更新日期:2016-01-01 00:00:00
abstract::Cynanchum wilfordii is one of most widely used medicinal plants in Oriental medicine for the treatment of various conditions. In the present study, we isolated cynandione A (CA) from an extract of Cynanchum wilfordii roots (CWE) and investigated the effects of CA on the expression of inducible nitric oxide synthase (i...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b13-00939
更新日期:2014-01-01 00:00:00
abstract::The effects of aged garlic extract (AGE) on longevity and learning and memory performances were studied in the senescence accelerated mouse (SAM). A solid diet containing 2% (w/w) AGE was given to SAM from 2 months of age. The survival ratio of SAM P8, senescence accelerated animals, treated with AGE was significantly...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.1589
更新日期:1994-12-01 00:00:00
abstract::The aim of this work is to investigate the therapeutic efficacy of VP-343 ((N-[4-[[(2S,3aR)-2-hydroxy-2,3,3a,4-tetrahydropyrrolo[1,2-a]qunoxalin-5(1H)-yl]phenyl]-4'-methyl[1,1'-biphenyl]-2-carboxamide), a selective vasopressin V2 receptor antagonist, using the experimental SIADH (syndrome of inappropriate secretion of...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.23.1323
更新日期:2000-11-01 00:00:00
abstract::Twelve species of pyridobenzazoles and pyrimidobenzimidazole were examined as inhibitors of the replication of respiratory syncytial virus (RSV) in HeLa cells. From the pyridobenzazoles studied, 2-benzamido-4-cyano-1-oxo-1H,5H-pyrido[1,2-alpha]benzimidazol emerged as a potent inhibitor of the RSV. Based on its inhibit...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.18.1081
更新日期:1995-08-01 00:00:00
abstract::Using a validated high-performance liquid chromatographic (HPLC) method, the pharmacokinetics of multi-constituents in Huangqin-Tang decoction were simultaneously studied both in the compound prescription and in each single herb decoction. At different intervals (0, 1, 2, 4, 8, 12, 24, 36, 48 h) after oral administrat...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.26.911
更新日期:2003-07-01 00:00:00
abstract::The effects of a liquid nutritive and tonic drug (NTD) selected from a modification of the "Kai-xin-shou-yu-shen-qi-wan" prescription, on scopolamine-induced amnesia in mice were investigated using the passive avoidance and water-maze tasks. A popular NTD in Japan that contains 17 crude (natural) drug extracts togethe...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.1886
更新日期:2005-10-01 00:00:00
abstract::We established a highly sensitive method for evaluating P-glycoprotein activity in Caco-2 cells. Using time-lapse confocal laser-scanning microscopy, we measured the change in fluorescence of residual rhodamine 123 in Caco-2 cells. Horizontal fluorescence images of rhodamine 123 in the apical and central parts of thes...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.1238
更新日期:2010-01-01 00:00:00
abstract::The present study investigated whether or not Sho-saiko-to (crude powder extract, TJ-9) can suppress nitric oxide (NO) generation by endotoxin-activated J774A.1 cells in order to study the preventive mechanism of Sho-saiko-to against endotoxemia. In this experiment, we estimated the NO2- in the murine macrophage cell ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.18.621
更新日期:1995-04-01 00:00:00
abstract::A conditioned medium (CM) was prepared by culturing human sperm at 3.0 x 10(6) sperm/ml for 12 h. The fusion index increased significantly when the sperm penetration assay (SPA) was performed with CM (0.6 without CM to 2.0 with CM). The conditioned medium was also effective on the sperm from 11 patients who showed a l...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.18.5
更新日期:1995-01-01 00:00:00
abstract::It is well established that vesicular nucleotide transporter (VNUT) is responsible for vesicular storage of nucleotides such as ATP, and that VNUT-expressing cells can secrete nucleotides upon exocytosis, playing an important role in purinergic chemical transmission. In the present study, we show that VNUT is expresse...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b14-00275
更新日期:2014-01-01 00:00:00
abstract::Acori graminei Rhizoma is one of the best-known traditional herbal medicines frequently used for the treatment of cardiovascular symptoms in Asian countries. The anti-ischemic effect of Acori graminei Rhizoma on ischemia-induced isolated rat heart was investigated through analysis of changes in perfusion pressure, aor...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.483
更新日期:2006-03-01 00:00:00
abstract::Radiation induces an important inflammatory response in the irradiated organs, characterized by leukocyte infiltration and vascular changes. Since adhesion molecules play an important role in facilitating the immune response at the inflammation sites, interfering with the expression of these molecules may be an import...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.752
更新日期:2010-01-01 00:00:00
abstract::We investigated the gene expression of GAPDH, cytochrome P450 isoforms (CYP1A1, CYP1A2, CYP1B1, CYP2A6, CYP2E1, CYP3A4, CYP3A5, and CYP3A7), UGT-dependent glucuronosyl transferase isoforms (UGT1A6 and UGT1A9), and ABC transporter (ABCB1) after exposure to 0.1, 0.5, and 2.5% dimethyl sulfoxide (DMSO). GAPDH mRNA levels...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.26.1052
更新日期:2003-07-01 00:00:00
abstract::To explore the mechanism responsible for puromycin aminonucleoside induced-nephrotoxicity, metal content was preliminarily investigated in the kidneys of rats that had received a single subcutaneous injection of the agent (80 mg/kg body weight). In the group that received this agent, the renal content of Fe rose on da...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.871
更新日期:1994-06-01 00:00:00
abstract::Regorafenib is a small molecule inhibitor of tyrosine kinases, and has been shown to improve the outcomes of patients with advanced colorectal cancer and advanced gastrointestinal stromal tumors. The transport profiles of regorafenib by various transporters were evaluated. HEK293/organic anion transporting polypeptide...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b14-00740
更新日期:2015-01-01 00:00:00
abstract::Polyporus (P.) umbellatus, an endangered medicinal fungus in China, is distributed throughout most areas of the country. Thirty-seven natural P. umbellatus samples collected from 12 provinces in China were subjected to the inter-simple sequence repeat (ISSR) assay to investigate the genetic diversity within and among ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b15-00274
更新日期:2015-01-01 00:00:00
abstract::We previously reported the isolation of a novel cerebroside (1-O-(beta-D-glucopyranosyl)-(2S,3R,4E,8Z)-2-N-palmityloc tadecasphinga-4,8-diene; LCC) from the fruits of Lycium chinense MILL. (Solanaceae) which protected primary cultured rat hepatocytes from the toxicity induced by carbon tetrachloride (CCl4). The presen...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.873
更新日期:1999-08-01 00:00:00
abstract::In an acute treatment experiment, metformin (150, 300 mg/kg, per os (p.o.)) markedly reduced the consumption of a high-fat diet (HFD) (45 kcal% fat-containing diet) for 2 h after the HFD was given to the fasted male C57BL/6J (B6) mice. In addition, metformin at a higher dose increased plasma active glucagon-like pepti...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.963
更新日期:2010-01-01 00:00:00
abstract::The aim of the present study is to investigate the effects of long-term Hypericum perforatum treatment on spatial learning and memory in rats. Hypericum preparation (HP) standardized to 0.3% hypericin content was administered orally for 9 weeks in doses of 4.3 and 13 microg/kg corresponding to therapeutic dosages in h...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.25.1289
更新日期:2002-10-01 00:00:00
abstract::There are some highly cytotoxic anticancer compounds inducing differentiation of cancer cells to normal cells at below highly cytotoxic concentration. Naphthoquinone derivatives having cytotoxic effects on cancer cell were tested to learn whether they have differentiation inducing activity in human leukemia HL-60 cell...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.19.824
更新日期:1996-06-01 00:00:00
abstract::We recently suggested that the transferrin (Tf)-gallium-67 (67Ga) complex dissociated on the surface of the hepatocytes after partial hepatectomy and free 67Ga bound to heparan sulfate in the extracellular matrix. In the present study, we investigated whether the entering of indium-111 (111In) and iron-59 (59Fe) with ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.27.1193
更新日期:2004-08-01 00:00:00
abstract::The purpose of this study was to investigate the absorption behavior of an ophthalmic drug injected in rabbit periocular tissues. After intracapsular, retrobulbar and palpebral conjunctival injections of 150 microl and 50 microl fluorescein isothiocyanate dextran (FITC-dextran, average molecular weight 11000), leakage...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.956
更新日期:1999-09-01 00:00:00
abstract::Microvessels are composed of endothelial cells that cover the luminal surface and pericytes that wrap around and along endothelial cells. In the present study, we investigated the regulation of fibrinolysis in cultured human brain microvascular pericytes and endothelial cells after exposure to thrombin. It was found t...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.208
更新日期:2005-02-01 00:00:00
abstract::Pentosidine, a fluorescent cross-linking compound, accumulates in extracellular matrix, especially in the collagen, and is formed by the nonenzymatic process of advanced Maillard reaction. We developed a method of determination of pentosidine and tried to examine its level in urine and serum of elder patients. The met...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.21.1005
更新日期:1998-10-01 00:00:00
abstract::Liquid intraurethral prostaglandin E1 (PGE1) delivery system was developed using self-microemulsifying drug delivery system (SMEDDS). For this, pseudo-ternary phase diagrams were constructed and characterized. The viscosity of optimized formulation was increased gradually upon the addition of water and it was decrease...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.31.668
更新日期:2008-04-01 00:00:00
abstract::This study sought to investigate the ameliorating effects of soy 11S protein on the impacts of alcohol consumption in rat hepatocytes and in reducing total cholesterol levels and total lipid levels in the serum. Liver histology and the clinically important enzyme markers (Aspartate Aminotransferase: AST and Alanine Am...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.27.1636
更新日期:2004-10-01 00:00:00
abstract::The purpose of this study was to develop a method for the measurement of the cell kinetics of spleen lymphocytes using the ROSA 26 transgenic mouse ubiquitously expressing beta-galactosidase (beta-gal). Spleen lymphocytes were isolated from ROSA 26 mice and intravenously inoculated into C57BL/6 mice under normal condi...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.25.1378
更新日期:2002-10-01 00:00:00
abstract::Defining a quantitative and reliable relationship between in vitro drug release and in vivo absorption is highly desired for rational development, optimization, and evaluation of controlled-release dosage forms and manufacturing process. During the development of once daily extended-release (ER) tablet of glipizide, a...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.31.1946
更新日期:2008-10-01 00:00:00