alpha-Fluoromethylhistidine. Kinetics of uptake and inhibition of histamine synthesis in basophil (2H3) cell cultures.

abstract：:The endogenous bronchodilator, S-nitrosoglutathione (GSNO), increases expression, maturation, and function of both the wild-type and the DeltaF508 mutant of the cystic fibrosis transmembrane conductance regulatory protein (CFTR). Though transcriptional mechanisms of action have been identified, GSNO seems also to have...

journal_title：Molecular pharmacology

authors： Zaman K,Carraro S,Doherty J,Henderson EM,Lendermon E,Liu L,Verghese G,Zigler M,Ross M,Park E,Palmer LA,Doctor A,Stamler JS,Gaston B

更新日期：2006-10-01 00:00:00

abstract：:In the present study, we have elucidated the functional characteristics and mechanism of action of methaqualone (2-methyl-3-o-tolyl-4(3H)-quinazolinone, Quaalude), an infamous sedative-hypnotic and recreational drug from the 1960s-1970s. Methaqualone was demonstrated to be a positive allosteric modulator at human α1,2...

journal_title：Molecular pharmacology

authors： Hammer H,Bader BM,Ehnert C,Bundgaard C,Bunch L,Hoestgaard-Jensen K,Schroeder OH,Bastlund JF,Gramowski-Voß A,Jensen AA

更新日期：2015-08-01 00:00:00

abstract：:The precise mechanism by which the broad-spectrum anti-RNA virus agent ribavirin elicits its in vitro antiviral effect has remained a matter of debate. We have demonstrated that inhibition of cellular inosine monophosphate dehydrogenase (IMPDH) activity, and thus depletion of intracellular GTP pools, is the predominan...

journal_title：Molecular pharmacology

authors： Leyssen P,De Clercq E,Neyts J

更新日期：2006-04-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs) act in concert to regulate cell growth, proliferation, survival, and migration. Metabotropic GABAB receptor (GABABR) is the GPCR for the main inhibitory neurotransmitter GABA in the central nervous system. Increased expression of GABABR has been ...

journal_title：Molecular pharmacology

authors： Xia S,He C,Zhu Y,Wang S,Li H,Zhang Z,Jiang X,Liu J

更新日期：2017-09-01 00:00:00

abstract：:Recent clinical studies reveal that selective agonists of group II metabotropic glutamate (mGlu) receptors have robust efficacy in treating positive and negative symptoms in patients with schizophrenia. Group II mGlu receptor agonists also modulate the in vivo activity of psychotomimetic drugs and reduce the ability o...

journal_title：Molecular pharmacology

authors： Benneyworth MA,Xiang Z,Smith RL,Garcia EE,Conn PJ,Sanders-Bush E

更新日期：2007-08-01 00:00:00

abstract：:Gemcitabine and pemetrexed are effective agents in the treatment of non-small-cell lung cancer (NSCLC), and the present study investigates cellular and genetic aspects of their interaction against A549, Calu-1, and Calu-6 cells. Cells were treated with pemetrexed and gemcitabine, and their interaction was assessed usi...

journal_title：Molecular pharmacology

authors： Giovannetti E,Mey V,Nannizzi S,Pasqualetti G,Marini L,Del Tacca M,Danesi R

更新日期：2005-07-01 00:00:00

abstract：:Tumor cell resistance to anthracyclines and epipodophyllotoxins can be due to reduced drug accumulation and/or alterations in the activity of topoisomerase II (TOPO II). HL-60 cells selected in 0.05 micrograms/ml doxorubicin (DOX) are 10-fold and > 20-fold resistant to DOX and etoposide (VP-16), respectively. The accu...

journal_title：Molecular pharmacology

authors： Ganapathi R,Constantinou A,Kamath N,Dubyak G,Grabowski D,Krivacic K

更新日期：1996-08-01 00:00:00

abstract：:Cadmium is a dangerous metal distributed widely in the environment. Members of our laboratory recently identified the ZIP8 transporter protein, encoded by the mouse Slc39a8 gene, to be responsible for genetic differences in response to cadmium damage of the testis. Stable retroviral infection of the ZIP8 cDNA in mouse...

journal_title：Molecular pharmacology

authors： He L,Girijashanker K,Dalton TP,Reed J,Li H,Soleimani M,Nebert DW

更新日期：2006-07-01 00:00:00

abstract：:Controlled inhibition of brain acetyl- and butyrylcholinesterases (AChE and BChE, respectively) and of monoamine oxidase-B (MAO-B) may slow neurodegeneration in Alzheimer's and Parkinson's diseases. It was postulated that certain carbamate esters would inhibit AChE and BChE with the concomitant release in the brain of...

journal_title：Molecular pharmacology

authors： Groner E,Ashani Y,Schorer-Apelbaum D,Sterling J,Herzig Y,Weinstock M

更新日期：2007-06-01 00:00:00

abstract：:Previous studies showed that lapatinib and obatoclax interact in a greater-than-additive fashion to cause cell death and do so through a toxic form of autophagy. The present studies sought to extend our analyses. Lapatinib and obatoclax killed multiple tumor cell types, and cells lacking phosphatase and tensin homolog...

journal_title：Molecular pharmacology

authors： Cruickshanks N,Tang Y,Booth L,Hamed H,Grant S,Dent P

更新日期：2012-12-01 00:00:00

abstract：:The use of classic antipsychotic drugs is limited by the occurrence of extrapyramidal motor symptoms, which are caused by dopamine (DA) receptor blockade in the neostriatum. We examined the impact of early-life stress on haloperidol-induced catalepsy using the rat model of prenatal restraint stress (PRS). Adult "PRS r...

journal_title：Molecular pharmacology

authors： Marrocco J,Mairesse J,Bucci D,Lionetto L,Battaglia G,Consolazione M,Ravasi L,Simmaco M,Morley-Fletcher S,Maccari S,Nicoletti F

更新日期：2013-08-01 00:00:00

abstract：:The aptamer mechanism of action involves the direct interaction of oligonucleotide with protein and is responsible for the biological effects of many pharmacologically active oligodeoxynucleotides. In the work reported here, we have determined the effects of aptamers on the secondary, tertiary, and quaternary structur...

journal_title：Molecular pharmacology

authors： Balasubramanian V,Nguyen LT,Balasubramanian SV,Ramanathan M

更新日期：1998-05-01 00:00:00

abstract：:In mammals, receptors for the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) are divided into three pharmacological classes, which are denoted GABAA, GABAB, and GABAC. GABAC receptors are defined by their insensitivity to the GABAA receptor antagonist bicuculline and the GABAB receptor agonist (-)-baclofen...

journal_title：Molecular pharmacology

authors： Ragozzino D,Woodward RM,Murata Y,Eusebi F,Overman LE,Miledi R

更新日期：1996-10-01 00:00:00

abstract：:Ubiquitination of the human kappa opioid receptor (hKOR) expressed in Chinese hamster ovary (CHO) cells was observed in the presence of the proteasomal inhibitor N-benzoyloxycarbonyl (Z)-Leu-Leu-leucinal (MG132) and enhanced by the agonists (-)(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidiny) cyclohexyl] benzeneaceta...

journal_title：Molecular pharmacology

authors： Li JG,Haines DS,Liu-Chen LY

更新日期：2008-04-01 00:00:00

abstract：:In isolated perfused rat livers, infusion of the sulfonylureas, glyburide (2.5 microM) and tolbutamide (0.5 mM), stimulated by 2-fold the rate of biliary glutathione secretion. This increase was mainly the result of an apparent increase in the rate of reduced glutathione release by the liver since oxidized glutathione...

journal_title：Molecular pharmacology

authors： Patel TB,Rashed HM,Dyson J,Waller FM

更新日期：1987-06-01 00:00:00

abstract：:TWIK-related K(+) 1 (TREK1) potassium channels are members of the two-pore domain potassium channel family and contribute to background potassium conductances in many cell types, where their activity can be regulated by a variety of physiologic and pharmacologic mediators. Fenamates such as FFA (flufenamic acid; 2-{[3...

journal_title：Molecular pharmacology

authors： Veale EL,Al-Moubarak E,Bajaria N,Omoto K,Cao L,Tucker SJ,Stevens EB,Mathie A

更新日期：2014-05-01 00:00:00

abstract：:Chick brain mRNA was isolated and injected into Xenopus oocytes. This led to the expression of gamma-aminobutyrate (GABA) channels easily accessible for current measurements using the voltage clamp technique. The effect of the anthelmintic natural product avermectin B1a on the GABA current was studied quantitatively. ...

journal_title：Molecular pharmacology

authors： Sigel E,Baur R

更新日期：1987-12-01 00:00:00

abstract：:Receptors for the serine protease thrombin and for lysophospholipids are coupled to G proteins and control a wide range of cellular functions, including mitogenesis. Activators of these receptors are present in blood, and can enter the brain during central nervous system (CNS) injury. Reactive astrogliosis, a prominen...

journal_title：Molecular pharmacology

authors： Sorensen SD,Nicole O,Peavy RD,Montoya LM,Lee CJ,Murphy TJ,Traynelis SF,Hepler JR

更新日期：2003-11-01 00:00:00

abstract：:We demonstrated previously that nonsteroidal anti-inflammatory drugs (NSAIDs) increased p27(Kip1) by inhibiting protein degradation to suppress the proliferation of human lung cancer cells. In this study, we elucidate the molecular mechanism by which NSAIDs modulate p27(Kip1) proteolysis. Immunoblotting and in vitro u...

journal_title：Molecular pharmacology

authors： Huang YC,Chuang LY,Hung WC

更新日期：2002-12-01 00:00:00

abstract：:Melanoma differentiation associated gene-7 (mda-7)/interleukin-24 (IL-24), a member of the IL-10 cytokine gene family, preferentially induces cell death in neoplastic epithelial cells types while sparing their normal counterparts. The effects of mda-7/IL-24 in acute myeloid leukemia (AML) cells have not been extensive...

journal_title：Molecular pharmacology

authors： Rahmani M,Mayo M,Dash R,Sokhi UK,Dmitriev IP,Sarkar D,Dent P,Curiel DT,Fisher PB,Grant S

更新日期：2010-12-01 00:00:00

abstract：:Noscapine, a microtubule-interfering agent, has been shown to arrest mitosis, to induce apoptosis, and to have potent antitumor activity. We report herein that two brominated derivatives of noscapine, 5-bromonoscapine (5-Br-nosc) and reduced 5-bromonoscapine (Rd 5-Br-nosc), have higher tubulin binding activity than no...

journal_title：Molecular pharmacology

authors： Zhou J,Gupta K,Aggarwal S,Aneja R,Chandra R,Panda D,Joshi HC

更新日期：2003-04-01 00:00:00

abstract：:Agonist stimulation of group III metabotropic glutamate receptors (mGluRs) induces an inhibition of neurotransmitter release from neurons. The group III mGluRs are pharmacologically defined by activation with the glutamate analog L-amino-4-phosphonobutyric acid (L-AP4). The affinities of these receptors for L-AP4 and ...

journal_title：Molecular pharmacology

authors： Rosemond E,Wang M,Yao Y,Storjohann L,Stormann T,Johnson EC,Hampson DR

更新日期：2004-10-01 00:00:00

abstract：:The GABA type A receptor (GABA(A)R) is the major inhibitory receptor in the mammalian central nervous system and the target of numerous pharmaceuticals. The alpha-subunit of these pentameric Cys-loop neurotransmitter-gated ion channels contributes to the binding of both GABA and allosteric modulators such as the benzo...

journal_title：Molecular pharmacology

authors： Hanek AP,Lester HA,Dougherty DA

更新日期：2010-07-01 00:00:00

abstract：:We identified a novel azaindole derivative, L-750,667, that has high affinity (Ki = 0.51 nM) and >2000-fold selectivity for D4 dopamine receptors compared with its activity at D2 and D3 dopamine receptors. L-750,667 had little affinity for rat D1/D5 dopamine receptors, sigma binding sites, or 5-hydroxytryptamine1A or ...

journal_title：Molecular pharmacology

authors： Patel S,Patel S,Marwood R,Emms F,Marston D,Leeson PD,Curtis NR,Kulagowski JJ,Freedman SB

更新日期：1996-12-01 00:00:00

abstract：:EM-652 (SCH 57068) is a new orally active antiestrogen that demonstrates pure antagonistic effects in the mammary gland and endometrium. In vivo studies have shown that EM-652 is primarily glucuronidated at the 7-hydroxy position in rats and that the metabolite is present in the plasma of female monkeys and human subj...

journal_title：Molecular pharmacology

authors： Barbier O,Albert C,Martineau I,Vallée M,High K,Labrie F,Hum DW,Labrie C,Bélanger A

更新日期：2001-03-01 00:00:00

abstract：:The isoprenoid donor for protein geranylgeranylation reactions, geranylgeranyl diphosphate (GGDP), is the product of the enzyme GGDP synthase (GGDPS) that condenses farnesyl diphosphate (FDP) and isopentenyl pyrophosphate. GGDPS inhibition is of interest from a therapeutic perspective for multiple myeloma because we h...

journal_title：Molecular pharmacology

authors： Allen C,Kortagere S,Tong H,Matthiesen RA,Metzger JI,Wiemer DF,Holstein SA

更新日期：2017-03-01 00:00:00

abstract：:The ligand recognition site of A2a-adenosine receptors in rabbit striatal membranes was probed using non-site-directed labeling reagents and specific affinity labels. Exposure of membranes to diethylpyrocarbonate at a concentration of 2.5 mM, followed by washing, was found to inhibit the binding of [3H]CGS 21680 and [...

journal_title：Molecular pharmacology

authors： Jacobson KA,Stiles GL,Ji XD

更新日期：1992-07-01 00:00:00

abstract：:The metabotropic glutamate 5 receptor and the cannabinoid type 1 receptor are G protein-coupled receptors that are widely expressed in the central nervous system. Metabotropic glutamate 5 receptors, present at the postsynaptic site, are coupled to Gαq/11 proteins and display an excitatory response upon activation, whe...

journal_title：Molecular pharmacology

authors： Olmo IG,Ferreira-Vieira TH,Ribeiro FM

更新日期：2016-11-01 00:00:00

abstract：:The purpose of these studies was to support the hypothesis that an undiscovered cannabinoid receptor exists in brain. [(35)S]GTP gamma S binding was stimulated by anandamide and WIN55212-2 in brain membranes from both CB(1)(+/+) and CB(1)(-/-) mice. In contrast, a wide variety of other compounds that are known to acti...

journal_title：Molecular pharmacology

authors： Breivogel CS,Griffin G,Di Marzo V,Martin BR

更新日期：2001-07-01 00:00:00

abstract：:Several 2-amino-3-benzoylthiophenes were found to increase the binding of [3H]N6-cyclohexyladenosine to A1 adenosine receptors in rat brain membranes. Concentration-response curves were bell-shaped, with up to 45% stimulation of binding at 10 microM followed by inhibition at higher concentrations. Because these compou...

journal_title：Molecular pharmacology

authors： Bruns RF,Fergus JH

更新日期：1990-12-01 00:00:00