Re-examining osteoarthritis therapy from a developmental biologist's perspective.

abstract：:A set of sulfamides designed, synthesized and evaluated against maximal electroshock seizure (MES) and pentilenetetrazol (PTZ) tests with promising results, were tested for their affinity for the benzodiazepine binding site of the GABA(A) receptor. The most active compounds, N,N'-dicyclohexylsulfamide (7) and N,N'-dip...

journal_title：Biochemical pharmacology

authors： Wasowski C,Gavernet L,Barrios IA,Villalba ML,Pastore V,Samaja G,Enrique A,Bruno-Blanch LE,Marder M

更新日期：2012-01-15 00:00:00

abstract：:A series of cytotoxic propenal (3-oxoprop-1-enyl) derivatives of pyrimidine bases and deoxynucleosides was evaluated for their ability to block thymidylate synthesis in intact and permeabilized murine leukemia L1210 cells. Several were potent inhibitors of this process, likely contributing to their cytotoxicity. The I...

journal_title：Biochemical pharmacology

authors： Kalman TI,Marinelli ER,Xu B,Reddy AR,Johnson F,Grollman AP

更新日期：1991-07-05 00:00:00

abstract：:Anticholinesterases (anti-ChE) have some effects on biological properties including behavior, vision, and electroencephalograms, which are often long lasting and which do not appear to be due to cholinesterase (ChE; EC 3.1.1.7) inhibition, but which may be due to alterations in the organization and/or functioning of t...

journal_title：Biochemical pharmacology

authors： Schupper H,Rosenberg P

更新日期：1991-09-12 00:00:00

abstract：:A new triazinoaminopiperidine derivative, Servier 9788 (S9788), was investigated for its ability to increase Adriamycin (ADR) accumulation and retention in two rodent (P388/ADR and DC-3F/AD) and three human (KB-A1, K562/R and COLO 320DM) cell lines displaying the P-glycoprotein (P-gp)-mediated multidrug resistance (MD...

journal_title：Biochemical pharmacology

authors： Léonce S,Pierré A,Anstett M,Pérez V,Genton A,Bizzari JP,Atassi G

更新日期：1992-11-03 00:00:00

abstract：:Phentermine was shown in the 1970s to inhibit the metabolism of serotonin by monoamine oxidase (MAO), but never was labeled as an MAO inhibitor; hence, it was widely used in combination with fenfluramine, and continues to be used, in violation of their labels, with other serotonin uptake blockers. We examined the effe...

journal_title：Biochemical pharmacology

authors： Ulus IH,Maher TJ,Wurtman RJ

更新日期：2000-06-15 00:00:00

abstract：:The oxidation of 14C-pyruvate by isolated rat pancreatic islets was inhibited competitively and in a concentration-dependent manner by alpha-cyano-4-hydroxycinnamate. A similar, though less marked inhibition was observed of U-14C-glucose oxidation, although oxidation of 1-14C-glucose was slightly enhanced in the prese...

journal_title：Biochemical pharmacology

authors： Best L,Tomlinson S

更新日期：1988-05-15 00:00:00

abstract：:To determine whether alpha,alpha-dideutero substitution in the side chain of the tryptamine molecule can exert primary isotope effects and enhance its bioavailability, equimolar mixtures of tryptamine (T) and either alpha,alpha-dideutero-tryptamine (alpha,alpha-[2H2]T) or beta,beta-dideutero-tryptamine (beta,beta-[2H2...

journal_title：Biochemical pharmacology

authors： Dyck LE,Boulton AA

更新日期：1986-09-01 00:00:00

abstract：:The actions of alkylating pindolol (N8-bromoacetyl-N1-3'-(4-indolyloxy)-2'-hydroxypropyl[z]-1,8- diamino-p-menthane; BIM) have been examined on beta-adrenoceptors in guinea-pig left atria and trachea. In organ bath experiments, addition of BIM (greater than or equal to 0.1 microM), followed by washout, produced concen...

journal_title：Biochemical pharmacology

authors： Molenaar P,Russell F,Pitha J,Summers R

更新日期：1988-10-01 00:00:00

abstract：:Although it is generally believed that thiazolidinediones ameliorate insulin resistance by lowering circulating free fatty acids, direct effects of these drugs in skeletal muscle may also contribute to their antidiabetic action. We report that troglitazone administration to mice for 1 day increased the protein express...

journal_title：Biochemical pharmacology

authors： Planavila A,Alegret M,Sánchez RM,Rodríguez-Calvo R,Laguna JC,Vázquez-Carrera M

更新日期：2005-04-15 00:00:00

abstract：:Tumor necrosis factor (TNF) is a pleiotropic cytokine that mediates different cellular responses including cytotoxicity, cytostasis, proliferation, differentiation and expression of specific genes. Recent studies have demonstrated that chemotherapeutic drugs that inhibit the nuclear enzyme DNA topoisomerase II synergi...

journal_title：Biochemical pharmacology

authors： Valenti M,Cimoli G,Mariani GL,Conte PF,Parodi S,Russo P

更新日期：1993-10-05 00:00:00

abstract：:A comparison between the effects of schisandrin B (Sch B) and butylated hydroxytoluene (BHT) treatments on hepatic antioxidant status was made to identify the critical antioxidant action of Sch B involved in hepatoprotection in mice. Whereas Sch B treatment (3 mmol/kg/day x 3, p.o.) increased the hepatic mitochondrial...

journal_title：Biochemical pharmacology

authors： Ip SP,Ko KM

更新日期：1996-12-13 00:00:00

abstract：:We have recently reported evidence that a simple beta-linked alkylated mannose reversibly increased the magnitude of GABA(A) receptor currents evoked in cultured rat pyramidal neurons whilst concomitantly reducing the incidence of spontaneous synaptic activity. In this present study, the effects of the simple beta-lin...

journal_title：Biochemical pharmacology

authors： Rezai N,Duggan C,Cairns D,Lees G,Chazot PL

更新日期：2003-02-15 00:00:00

abstract：:In this study we examined the metabolism of hypoxanthine in fibroblast growth factor (FGF)-stimulated porcine aortic endothelial cells (PAEC). Our previous report indicated that hypoxanthine in fetal bovine serum (FBS) was an essential component for both basal and FGF-dependent growth of PAEC (Hayashi et al., Exp Cell...

journal_title：Biochemical pharmacology

authors： Hirai S,Hayashi Y,Koizumi T,Nakanishi N,Fukui T,Ichikawa A

更新日期：1993-04-22 00:00:00

abstract：:A growing body of evidence suggests that mitochondria take up calcium upon receptor (agonist) stimulation and that this contributes to the dynamics of spatiotemporal calcium signaling. We have previously shown that engagement of the high-affinity receptor for immunoglobulin E (FcepsilonRI) stimulates mitochondrial cal...

journal_title：Biochemical pharmacology

authors： Suzuki Y,Yoshimaru T,Inoue T,Nunomura S,Ra C

更新日期：2008-04-01 00:00:00

abstract：:The localization of the low-affinity adenosine binding protein adenotin-1 with respect to distribution in rat organs and subcellular compartments was investigated. Adenotin-1 was characterized by 5'-N-ethylcarboxamido[2,8-3H]adenosine ([3H]NECA) binding and Western blotting. Cytosolic as well as membrane fractions of ...

journal_title：Biochemical pharmacology

authors： Lorenzen A,Engelhardt J,Kerst B,Schwabe U

更新日期：1998-02-15 00:00:00

abstract：:The microsomal brush-border fraction of rat renal tissue contains enzymatic activity, optimally active at pH 9, that is capable of degrading human myelin basic protein (BP) peptide 43-88. In the present study, this degradation and the effect on it of selected drugs and hormones were examined further. Of the substances...

journal_title：Biochemical pharmacology

authors： Trestman RL,Heinemann MA,Whitaker JN,Seyer JM

更新日期：1985-04-15 00:00:00

abstract：:The inhibitory effects of anion channel blockers were evaluated on aggregation, intracellular Ca2+ rises, and the production of arachidonic acid metabolites in human platelets. Inhibitors included five anion channel blockers: phloretin, probenecid, pyridoxal phosphate, 4,4'-diisothiocyano-2,2'-disulfonic acid stilbene...

journal_title：Biochemical pharmacology

authors： Ozaki Y,Matsumoto Y,Yatomi Y,Higashihara M,Kariya T,Shoji K

更新日期：1989-07-01 00:00:00

abstract：:In the present study the inability of 1,4-benzoquinone to support NADPH-cytochrome reductase catalysed redox cycling was investigated. The results obtained demonstrate that NADPH-cytochrome reductase is able to initiate a rapid two-electron reduction of 1,4-benzoquinone resulting in formation of the hydroquinone. The ...

journal_title：Biochemical pharmacology

authors： Boersma MG,Balvers WG,Boeren S,Vervoort J,Rietjens IM

更新日期：1994-06-01 00:00:00

abstract：:Ethyl 2[5(4-chlorophenyl)pentyl]oxirane-2-carboxylate (POCA) is strongly hypoglycaemic in fasted normal and diabetic rats [H. P. O. Wolf, K. Eistetter and G. Ludwig, Diabetologia 22, 456 (1982)]. POCA was fed for 12 weeks to rats on a standard low-fat (3%) diet at levels of 0.05% and 0.2% to give daily intakes of abou...

journal_title：Biochemical pharmacology

authors： Koundakjian PP,Turnbull DM,Bone AJ,Rogers MP,Younan SI,Sherratt HS

更新日期：1984-02-01 00:00:00

abstract：:Here we report that organic copper complexes can potently and selectively inhibit the chymotrypsin-like activity of the proteasome in vitro and in vivo. Several copper compounds, such as NCI-109268 and bis-8-hydroxyquinoline copper(II) [Cu(8-OHQ)(2)], can inhibit the chymotrypsin-like activity of purified 20S proteaso...

journal_title：Biochemical pharmacology

authors： Daniel KG,Gupta P,Harbach RH,Guida WC,Dou QP

更新日期：2004-03-15 00:00:00

abstract：:Smoking during pregnancy is the largest modifiable risk factor for pregnancy-related morbidity and mortality. The success of bupropion for smoking cessation warrants its investigation for the treatment of pregnant patients. Nevertheless, the use of bupropion for the treatment of pregnant smokers requires additional da...

journal_title：Biochemical pharmacology

authors： Wang X,Abdelrahman DR,Zharikova OL,Patrikeeva SL,Hankins GD,Ahmed MS,Nanovskaya TN

更新日期：2010-06-01 00:00:00

abstract：:It has become apparent of late that even in tamoxifen and/or aromatase resistant breast cancers, ERα remains a bona fide therapeutic target. Not surprisingly, therefore, there has been considerable interest in developing Selective ER Degraders (SERDs), compounds that target the receptor for degradation. Currently, ICI...

journal_title：Biochemical pharmacology

authors： Wardell SE,Marks JR,McDonnell DP

更新日期：2011-07-15 00:00:00

abstract：:Epothilones constitute a novel class of antitubulin agents that are active in patients who relapse after treatment with other chemotherapeutics. This study investigated the molecular mechanisms leading to the onset of epothilone-B (patupilone) resistance in ovarian cancer. Results demonstrated that the Gli family of t...

journal_title：Biochemical pharmacology

authors： Mozzetti S,Martinelli E,Raspaglio G,Prislei S,De Donato M,Filippetti F,Shahabi S,Scambia G,Ferlini C

更新日期：2012-12-01 00:00:00

abstract：:Epoxyeicosatrienoic acids (EETs), a family of cytochrome P450 epoxygenase metabolites of arachidonic acid, are believed to have an autocrine or paracrine role in the regulation of neurons or neuroendocrine cells. The effects of 14,15-EET on ionic currents were investigated in rat pituitary GH(3) cells. In the whole-ce...

journal_title：Biochemical pharmacology

authors： Wu SN,Li HF,Chiang HT

更新日期：2000-07-15 00:00:00

abstract：:The immunosuppressive and cytostatic agent 15-deoxyspergualin (DSG) binds to the Hsc70 class of molecular chaperones with a K(D) = 4 microM. Because Hsc70s represent a diverse group of cellular effectors and because Hsc70 function frequently requires a DnaJ molecular chaperone, the specificity of DSG for different Hsc...

journal_title：Biochemical pharmacology

authors： Brodsky JL

更新日期：1999-04-15 00:00:00

abstract：:P-450-male is a male specific form of cytochrome P-450 in rat liver microsomes. Cytochrome P-450 crossreactive with anti-P-450-male antibodies was purified to an electrophoretical homogeneity from liver microsomes of male beagle dogs. The specific content of the purified cytochrome P-450 (P-450-D1) was 16.9 nmol/mg pr...

journal_title：Biochemical pharmacology

authors： Komori M,Shimada H,Miura T,Kamataki T

更新日期：1989-01-15 00:00:00

abstract：:Macrophages are key inflammatory cells in chronic obstructive pulmonary disease (COPD). The pathophysiology of cigarette smoke-induced lung emphysema is complex but there is a clear role for reactive oxygen species (ROS, such as peroxynitrite), tumor necrosis factor (TNF-alpha) and interleukin (IL)-8. We investigated ...

journal_title：Biochemical pharmacology

authors： Sarir H,Mortaz E,Janse WT,Givi ME,Nijkamp FP,Folkerts G

更新日期：2010-03-01 00:00:00

abstract：:GABAB receptors assemble from GABAB1 and GABAB2 subunits. GABAB2 additionally associates with auxiliary KCTD subunits (named after their K(+) channel tetramerization-domain). GABAB receptors couple to heterotrimeric G-proteins and activate inwardly-rectifying K(+) channels through the βγ subunits released from the G-p...

journal_title：Biochemical pharmacology

authors： Adelfinger L,Turecek R,Ivankova K,Jensen AA,Moss SJ,Gassmann M,Bettler B

更新日期：2014-10-01 00:00:00

abstract：:Phomopsins comprise a family of peptide mycotoxins containing a 13-membered ring formed by an ether bridge, produced by the fungus Phomopsis leptostromiformis, the causal agent in lupin poisoning (lupinosis). The biochemical actions of two naturally occurring phomopsins, phomopsin A and B, and the chemical derivatives...

journal_title：Biochemical pharmacology

authors： Lacey E,Edgar JA,Culvenor CC

更新日期：1987-07-01 00:00:00

abstract：:The nuclear receptors liver X receptor (LXR) alpha and LXRbeta serve as oxysterol receptors and play an important role in the regulation of lipid metabolism. We investigated the potential effects of LXRs on pathways of colon carcinogenesis and found that LXR activation suppresses the transactivation activity of beta-c...

journal_title：Biochemical pharmacology

authors： Uno S,Endo K,Jeong Y,Kawana K,Miyachi H,Hashimoto Y,Makishima M

更新日期：2009-01-15 00:00:00