Stimulation and inhibition of adenylyl cyclase by distinct 5-hydroxytryptamine receptors.

abstract：:With the aid of a chiral derivatizing reagent and a sensitive and specific nitrogen-phosphorus gas chromatographic assay, metabolism of para-chloroamphetamine (PCA) enantiomers has been studied following incubation of racemic (RS)-, R(-)- and S(+)-PCA with rabbit liver microsomal preparations. Significant metabolism o...

journal_title：Biochemical pharmacology

authors： Ames MM,Frank SK

更新日期：1982-01-01 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：: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：:Improved syntheses, based on Lewis acid-catalyzed nucleosidation, are described for the preparation of 5-alkyl-2'-deoxyuridines. These were converted to their 5'-phosphates with the use of wheat shoot phosphotransferase. The dUMP analogues, 5-ethyl-dUMP and 5-propyl-dUMP, were competitive vs dUMP inhibitors of thymidy...

journal_title：Biochemical pharmacology

authors： Rode W,Kulikowski T,Kedzierska B,Jastreboff M,Shugar D

更新日期：1984-09-01 00:00:00

abstract：:Rat, rabbit and human serum albumins were immobilized on an HPLC stationary phase, and the resulting phases were tested for their abilities to determine the extent and enantioselectivity of ligand binding to the respective albumins. A series of achiral and chiral compounds were chromatographed on the phases including ...

journal_title：Biochemical pharmacology

authors： Massolini G,Aubry AF,McGann A,Wainer IW

更新日期：1993-10-05 00:00:00

abstract：:Tumor-induced neoangiogenesis is an essential event for solid tumor growth. Therefore, a compound able to block angiogenesis-promoting factors could have antitumor activity. The polysulfonated naphthylurea suramin is hypothesized to have this mode of action. A series of sulfonated distamycin A derivatives have been sy...

journal_title：Biochemical pharmacology

authors： Ciomei M,Pastori W,Mariani M,Sola F,Grandi M,Mongelli N

更新日期：1994-01-20 00:00:00

abstract：:[3H]Morphine, PL-017[prolyl-3,4-3H,D-prolyl,3,4-3H] ([3H]PL-017) and enkephalin-(2-D-penicillamine,5-D-penicillamine)[tyrosyl-2,6-3H] ([3H]DPDPE) were directly cross-linked to mouse brain opiate receptors by an ultraviolet (254 nm) irradiation procedure. [3H]Morphine preferentially and specifically labeled a 58 kDa pr...

journal_title：Biochemical pharmacology

authors： Nagamatsu K,Tagawa Y,Uchida S,Hasegawa A

更新日期：1993-10-05 00:00:00

abstract：:Products derived from arachidonic acid (AA) via both the cyclo-oxygenase and lipoxygenase pathways play a role in inflammation: prostaglandins (PGs), particularly PGE2, contribute to the formation of oedema, erythema and hyperalgesia whereas leukotriene B4 (LTB4), a product of the 5' lipoxygenase, may modulate the rec...

journal_title：Biochemical pharmacology

authors： Terano T,Salmon JA,Higgs GA,Moncada S

更新日期：1986-03-01 00:00:00

abstract：:The effect of the adenosine deaminase (ADA) inhibitor 2'-deoxycoformycin (dCF) on the development of insulin-dependent diabetes mellitus (IDDM) was assessed in the BB Wistar rat. Sixty-one male rats were treated from days 30 to 120 with 0, 0.5, 1.0 or 1.5 mg dCF/kg/week. The incidence of IDDM was 78% in the controls a...

journal_title：Biochemical pharmacology

authors： Thliveris JA,Begleiter A,Kobrinsky NL,Verburg L,Dean HJ,Johnston JB

更新日期：1993-09-14 00:00:00

abstract：:Quinones are ubiquitously present in mammals and their environment. They are involved in physiologic functions such as electron transport but are also toxic compounds. In particular, quinone-quinol redox cycles may lead to oxidative stress, and arylating quinones have been demonstrated to activate endoplasmic reticulu...

journal_title：Biochemical pharmacology

authors： Bock KW

更新日期：2012-04-01 00:00:00

abstract：:MRP1 overexpression in multidrug-resistant cancer cells has been shown to be responsible for collateral sensitivity to some flavonoids that stimulate a huge MRP1-mediated GSH efflux. This massive GSH depletion triggers the death of these cancer cells. We describe here that bivalent flavonoid dimers strikingly stimulat...

journal_title：Biochemical pharmacology

authors： Dury L,Nasr R,Lorendeau D,Comsa E,Wong I,Zhu X,Chan KF,Chan TH,Chow L,Falson P,Di Pietro A,Baubichon-Cortay H

更新日期：2017-01-15 00:00:00

abstract：:"Are new neurons added in the adult mammalian brain?" "Do neural stem cells activate following CNS diseases?" "How can we modulate their activation to promote recovery?" Recent findings in the field provide novel insights for addressing these questions from a new perspective. In this review, we will summarize the curr...

journal_title：Biochemical pharmacology

authors： Pino A,Fumagalli G,Bifari F,Decimo I

更新日期：2017-10-01 00:00:00

abstract：:Hemin is a potential cytolytic agent. To test the effect of vitamin E on hemin-mediated permeability in cell membranes, sheep erythrocytes were chosen as an appropriate model to study hemolysis induced by hemin. Hemin-induced hemolysis but did not elicit lipid peroxidation in sheep erythrocytes. Vitamin E was effectiv...

journal_title：Biochemical pharmacology

authors： Wang F,Wang T,Lai J,Li M,Zou C

更新日期：2006-03-14 00:00:00

abstract：:3'-Phosphoadenosine 5'-phosphosulfate (PAPS) is the high-energy "sulfate donor" for reactions catalyzed by sulfotransferase (SULT) enzymes. The strict requirement of SULTs for PAPS suggests that PAPS synthesis might influence the rate of sulfate conjugation. In humans, PAPS is synthesized from ATP and SO(4)(2-) by two...

journal_title：Biochemical pharmacology

authors： Xu ZH,Thomae BA,Eckloff BW,Wieben ED,Weinshilboum RM

更新日期：2003-06-01 00:00:00

abstract：:Tannic acid (TA) is a naturally occurring phenol, which has been found to display an antipromotion effect on mouse skin carcinogenesis. In order to explore the molecular mechanism, we have examined the process of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced protein kinase C (PKC) activation, including phorbol es...

journal_title：Biochemical pharmacology

authors： Kuo ML,Wu WS,Lee KC,Lin JK

更新日期：1993-10-19 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：:Site-specific DNA cleavage in the presence of Cu(II) complexes of podophyllotoxin derivatives was investigated with a modified Sanger sequencing method. Cu(II) complexes of 4'-demethylepipodophyllotoxin (DEPD) and syringic acid (SA) cleaved M13mp18 single-strand DNA site-specifically at both cytosine (C) and guanine (...

journal_title：Biochemical pharmacology

authors： Yamashita A,Tawa R,Imakura Y,Lee KH,Sakurai H

更新日期：1994-05-18 00:00:00

abstract：:The human α7 neuronal nicotinic acetylcholine receptor gene (CHRNA7) is a candidate gene for schizophrenia and an important drug target for cognitive deficits in the disorder. Activation of the α7*nAChR, results in opening of the channel and entry of mono- and divalent cations, including Ca(2+), that presynaptically p...

journal_title：Biochemical pharmacology

authors： Araud T,Graw S,Berger R,Lee M,Neveu E,Bertrand D,Leonard S

更新日期：2011-10-15 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：: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：:Isolated rat liver mitochondria have been incubated in the presence of the general anesthetic 2,6-diisopropylphenol (0-100 microM) and the efficiency of oxidative phosphorylation has been evaluated by measuring the respiratory rates, the rates of ATP synthesis or hydrolysis and the magnitude of the transmembrane elect...

journal_title：Biochemical pharmacology

authors： Branca D,Roberti MS,Lorenzin P,Vincenti E,Scutari G

更新日期：1991-06-21 00:00:00

abstract：:The interaction of dicumarol derivatives and protriptyline with respect to the binding to alpha 1-acid glycoprotein (AGP) has been investigated by circular dichroism (CD), equilibrium dialysis and ultrafiltration. Investigation of the induced CD spectra of dicumarol derivatives bound to AGP indicated that the conforma...

journal_title：Biochemical pharmacology

authors： Miyoshi T,Yamamichi R,Maruyama T,Takadate A,Otagiri M

更新日期：1992-05-28 00:00:00

abstract：:The possible role of fluroacetate in the toxicity and antitumour activity of the fluroethylnitrosoureas, BFNU and FCNU has been studied in CBA mice bearing the TLX5 lymphoma either sensitive (TLXS) or resistant (TLXRT) to nitrosoureas. Treatment of mice bearing either TLXS or TLXRT tumours with either BFNU or FCNU cau...

journal_title：Biochemical pharmacology

authors： Tisdale MJ,Brennan RA

更新日期：1985-09-15 00:00:00

abstract：:Prostacyclin and beraprost sodium (beraprost), a stable analogue of prostacyclin, increased cyclic AMP (cAMP) levels of cultured human umbilical vein endothelial cells (HUVEC) in a concentration-dependent manner. The elevation of cAMP by beraprost was sustained longer than that by prostacyclin. The expression of throm...

journal_title：Biochemical pharmacology

authors： Kainoh M,Maruyama I,Nishio S,Nakadate T

更新日期：1991-04-15 00:00:00

abstract：:Minocycline is a semisynthetic tetracycline derivative; it has anti-inflammatory and anti-cancer effects distinct from its antimicrobial function. However, the molecular mechanism of minocycline-induced cytotoxicity in non-small cell lung cancer (NSCLC) cells has not been identified. Rad51 plays a central role in homo...

journal_title：Biochemical pharmacology

authors： Ko JC,Wang TJ,Chang PY,Syu JJ,Chen JC,Chen CY,Jian YT,Jian YJ,Zheng HY,Chen WC,Lin YW

更新日期：2015-10-01 00:00:00

abstract：:beta-Antiadrenergic properties are part of the pharmacological characteristics of amiodarone. In the present study, the action of amiodarone on rat-heart beta-adrenoceptors was investigated. [125I]Cyanopindolol (CYP) was used to label beta-adrenoceptors in crude rat-heart microsomes. In competition binding experiments...

journal_title：Biochemical pharmacology

authors： Nokin P,Clinet M,Schoenfeld P

更新日期：1983-09-01 00:00:00

abstract：:Tetranitromethane (TNM) is a reagent which reacts with the tyrosine and cysteine residues of proteins. Chemical modification of partially purified human platelet alpha 2-adrenoceptors with TNM resulted in an irreversible loss of binding activity. Typically, an 80-90% decrease in binding activity occurred with a 60-min...

journal_title：Biochemical pharmacology

authors： Nakata H,Regan JW,Lefkowitz RJ

更新日期：1986-11-15 00:00:00

abstract：:Inflammation, especially chronic inflammation, is directly involvement in the pathogenesis of many diseases including cancer. An effective approach for managing inflammation is to employ chemicals to block activation of nuclear factor-κB (NF-κB), a key regulator for inflammatory processes. Piperlongumine (piplartine, ...

journal_title：Biochemical pharmacology

authors： Sun LD,Wang F,Dai F,Wang YH,Lin D,Zhou B

更新日期：2015-06-01 00:00:00

abstract：:The effects of cetaben and clofibric acid were compared on the activities of peroxisomal enzymes in the liver and kidney of male Wistar rats. Cetaben at 200 mg/kg body wt increased the activities of all of the enzymes in the liver that were studied two to eight times, whereas the changes induced by the same dose of cl...

journal_title：Biochemical pharmacology

authors： Chandoga J,Rojeková I,Hampl L,Hocman G

更新日期：1994-02-09 00:00:00

abstract：:The DNA-topoisomerase I (Topo I) inhibitor, camptothecin (CPT), is a plant alkaloid with an important antitumor activity. In order to investigate the cellular mechanism leading to the development of the resistance to this agent, we have established by progressive adaptation a P388 subline resistant to CPT. After 5 mon...

journal_title：Biochemical pharmacology

authors： Madelaine I,Prost S,Naudin A,Riou G,Lavelle F,Riou JF

更新日期：1993-01-26 00:00:00