Cannabinol enhancement of interleukin-2 (IL-2) expression by T cells is associated with an increase in IL-2 distal nuclear factor of activated T cell activity.

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：:The binding of [3H]Hspiroperidol to D2 dopaminergic receptors in rat striatum was compared to the binding of [3H]dopamine to its binding sites. Both radioligands labeled apparently homogeneous populations of high affinity, stereoselective, saturable sites, determined from analysis of saturation isotherms. [3H]Spiroper...

journal_title：Molecular pharmacology

authors： Hancock AA,Marsh CL

更新日期：1984-11-01 00:00:00

abstract：:Healing of gastrointestinal mucosal lesions occurs through two processes: an early one involving cell migration and a later one in which cell division replaces lost cells. Both processes require the presence of polyamines, but the mechanism of action of these compounds is unknown. In the present study, we examined the...

journal_title：Molecular pharmacology

authors： McCormack SA,Zimmerman BJ,Israel M,Blanner P,Johnson LR

更新日期：1995-10-01 00:00:00

abstract：:The epithelial sodium channel (ENaC) is believed to represent the rate-limiting step for sodium absorption in the renal collecting duct. Consequently, ENaC is a central effector affecting systemic blood volume and pressure. Sodium and water transport are dysregulated in diabetes mellitus. Peroxisome proliferator-activ...

journal_title：Molecular pharmacology

authors： Pavlov TS,Levchenko V,Karpushev AV,Vandewalle A,Staruschenko A

更新日期：2009-12-01 00:00:00

abstract：:In this study, we investigated the effects of single alanine substitutions of amino acid residues in the supposed ATP binding site of the human P2X3 receptor on the agonistic effect of nucleotide analogs. The wild-type and mutant receptors were expressed in HEK293 cells, and the nucleotide effects were measured by mea...

journal_title：Molecular pharmacology

authors： Riedel T,Wiese S,Leichsenring A,Illes P

更新日期：2012-07-01 00:00:00

abstract：:Organic anion transporting polypeptides (Oatp) mediate the transport of a wide variety of amphipathic organic substrates. Rat Oatp1b2 and human OATP1B3 are members of a liver-specific subfamily of Oatps/OATPs. We investigated whether prolactin (PRL) and growth hormone (GH) regulated Oatp1b2 and OATP1B3 gene expression...

journal_title：Molecular pharmacology

authors： Wood M,Ananthanarayanan M,Jones B,Wooton-Kee R,Hoffman T,Suchy FJ,Vore M

更新日期：2005-07-01 00:00:00

abstract：:Newly synthesized tocainide analogs were tested for their state-dependent affinity and use-dependent behavior on sodium currents (INa) of adult skeletal muscle fibers by means of the Vaseline-gap voltage clamp method. The drugs had the pharmacophore amino group constrained in position alpha [N-(2,6-dimethylphenyl)pyrr...

journal_title：Molecular pharmacology

authors： De Luca A,Talon S,De Bellis M,Desaphy JF,Lentini G,Corbo F,Scilimati A,Franchini C,Tortorella V,Camerino DC

更新日期：2003-10-01 00:00:00

abstract：:The P2Y(1) receptor is responsible for the initiation of platelet aggregation in response to ADP and plays a key role in thrombosis. Although this receptor is expressed early in the platelet lineage, the regulation of its expression during megakaryocyte differentiation is unknown. In the mouse megakaryocytic cell line...

journal_title：Molecular pharmacology

authors： Hechler B,Toselli P,Ravanat C,Gachet C,Ravid K

更新日期：2001-11-01 00:00:00

abstract：:Reuptake of glutamate in astrocytes, a critical mechanism involved in the maintenance of physiological excitatory amino acid neurotransmission, is inhibited by both arachidonic acid (AA) and reactive oxygen species (ROS), via incompletely defined molecular mechanisms. Because ROS are generated during AA metabolism and...

journal_title：Molecular pharmacology

authors： Volterra A,Trotti D,Racagni G

更新日期：1994-11-01 00:00:00

abstract：:Four piperazinoquinolone antibacterial drugs (norfloxacin, ciprofloxacin, enoxacin, and pipemidic acid), known to be gamma-aminobutyric acid (GABA) antagonists, fully reversed the inhibitory effect of GABA on [35S]t-butylbicyclophosphorothionate ([35S] TBPS) binding to rat brain membranes in vitro. Twelve indomethacin...

journal_title：Molecular pharmacology

authors： Squires RF,Saederup E

更新日期：1993-05-01 00:00:00

abstract：:Ethanol-inducible CYP2E1 is an enzyme of major toxicological interest because it metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. CYP2E1 has also been implicated in alcohol liver disease because of its contribution to oxidative stress. Previously, polymorphic alleles with mutations in i...

journal_title：Molecular pharmacology

authors： Hu Y,Oscarson M,Johansson I,Yue QY,Dahl ML,Tabone M,Arincò S,Albano E,Ingelman-Sundberg M

更新日期：1997-03-01 00:00:00

abstract：:alpha-Amidation is essential for the function of many peptides in intercellular communication. This C-terminal modification is mediated in a two-step process by the hydroxylase and lyase activities of the bifunctional enzyme, peptidylglycine alpha-amidating monooxygenase (PAM). The first step, catalyzed by peptidylgly...

journal_title：Molecular pharmacology

authors： Driscoll WJ,Mueller SA,Eipper BA,Mueller GP

更新日期：1999-06-01 00:00:00

abstract：:The membrane-permeable, noncompetitive inositol 1,4,5-trisphosphate (IP3)-receptor inhibitor 2-aminoethoxydiphenyl borane (2-APB) has been widely used to probe for IP3-receptor involvement in calcium signaling pathways. However, a number of recent studies in different cell types revealed other sites of action of 2-APB...

journal_title：Molecular pharmacology

authors： Braun FJ,Aziz O,Putney JW Jr

更新日期：2003-06-01 00:00:00

abstract：:The gonadotropin-releasing hormone receptor (GnRH-R) of the African catfish couples to phospholipase C and belongs to the large family of G protein-coupled receptors. We recently demonstrated that removal of the carboxyl-terminal tail (S331-Q379) from the catfish GnRH-R results in a loss of agonist binding; the curren...

journal_title：Molecular pharmacology

authors： Blomenröhr M,Heding A,Sellar R,Leurs R,Bogerd J,Eidne KA,Willars GB

更新日期：1999-12-01 00:00:00

abstract：:We have expanded previous studies with the 5-hydroxytryptamine (5-HT)(2) receptor agonist (+/-)-1-(2,5-dimethoxy-4-[(125)I]iodophenyl)-2-aminopropane [(+/-)-[(125)I]DOI] in human brain that had shown biphasic competition curves for several 5-HT(2A) receptor antagonists by using new selective antagonists of 5-HT(2A) (M...

journal_title：Molecular pharmacology

authors： López-Giménez JF,Villazón M,Brea J,Loza MI,Palacios JM,Mengod G,Vilaró MT

更新日期：2001-10-01 00:00:00

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：:Cytotoxic effects of quinones are thought to be mediated by redox cycles between quinones and quinols whereby reactive oxygen species are generated. The role of glucuronidation in preventing these toxic redox cycles was investigated by using benzo(a)pyrene-3,6-quinone and isolated rat hepatocytes or Reuber hepatoma ce...

journal_title：Molecular pharmacology

authors： Lilienblum W,Bock-Hennig BS,Bock KW

更新日期：1985-04-01 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：:Allosteric modulators of G-protein-coupled receptors can regulate conformational states involved in receptor activation ( Mol Pharmacol 58: 1412-1423, 2000 ). This hypothesis was investigated for the corticotropin-releasing factor type 1 (CRF(1)) receptor using a novel series of ligands with varying allosteric effect ...

journal_title：Molecular pharmacology

authors： Hoare SR,Fleck BA,Gross RS,Crowe PD,Williams JP,Grigoriadis DE

更新日期：2008-05-01 00:00:00

abstract：:Prior studies indicate that adenosine and the adenosine A2A receptor play a role in hepatic fibrosis by a mechanism that has been proposed to involve direct stimulation of hepatic stellate cells (HSCs). The objective of this study was to determine whether primary hepatic stellate cells produce collagen in response to ...

journal_title：Molecular pharmacology

authors： Che J,Chan ES,Cronstein BN

更新日期：2007-12-01 00:00:00

abstract：:Guanine nucleotides have been examined as to their effects on subclass-specific excitatory amino acid receptor-ligand interactions. Guanine nucleotides selectively inhibit L-[3H]glutamate binding to the N-methyl-D-aspartate (NMDA) recognition site while showing a lesser effect on [3H]kainate, [3H]alpha-amino-3-hydroxy...

journal_title：Molecular pharmacology

authors： Monahan JB,Hood WF,Michel J,Compton RP

更新日期：1988-08-01 00:00:00

abstract：:Previous analyses suggested that potent aryl hydrocarbon receptor (AhR) antagonists were planar, with a lateral electron-rich center. To further define structural requirements and mechanism for antagonism, ten additional flavone derivatives were synthesized. Based on their ability to 1) compete with 2,3,7, 8-tetrachlo...

journal_title：Molecular pharmacology

authors： Henry EC,Kende AS,Rucci G,Totleben MJ,Willey JJ,Dertinger SD,Pollenz RS,Jones JP,Gasiewicz TA

更新日期：1999-04-01 00:00:00

abstract：:Increasing data indicate that brain endocannabinoid system plays a role in the effects of antidepressant medications. Here we examined the effect of in vivo exposure to the selective serotonin uptake inhibitor fluoxetine on cannabinoid type 1 (CB(1)) receptor density and functionality in the rat prefrontal cortex (PFC...

journal_title：Molecular pharmacology

authors： Mato S,Vidal R,Castro E,Díaz A,Pazos A,Valdizán EM

更新日期：2010-03-01 00:00:00

abstract：:Voltage-gated potassium (Kv) channels regulate many physiological functions and represent important therapeutic targets in the treatment of several clinical disorders. Although some of these channels have been well-characterized, the study of others, such as Kv3 channels, has been hindered because of limited pharmacol...

journal_title：Molecular pharmacology

authors： Yan L,Herrington J,Goldberg E,Dulski PM,Bugianesi RM,Slaughter RS,Banerjee P,Brochu RM,Priest BT,Kaczorowski GJ,Rudy B,Garcia ML

更新日期：2005-05-01 00:00:00

abstract：:The highly conserved Arg in the so-called DRY motif (Asp-Arg-Tyr) at the intracellular end of transmembrane helix 3 is in general considered as an essential residue for G protein coupling in rhodopsin-like seven transmembrane (7TM) receptors. In the open reading frame 74 (ORF74) receptor encoded by equine herpesvirus ...

journal_title：Molecular pharmacology

authors： Rosenkilde MM,Kledal TN,Schwartz TW

更新日期：2005-07-01 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：:Macrophage production of growth factors for fibroblasts, in particular platelet-derived growth factor B [PDGF(B)] and transforming growth factor-beta (TGF-beta), is thought to be central to the pathogenesis of pulmonary fibrosis. In a search for anti-inflammatory agents that might prevent this process, we asked whethe...

journal_title：Molecular pharmacology

authors： Wangoo A,Haynes AR,Sutcliffe SP,Sorooshian M,Shaw RJ

更新日期：1992-10-01 00:00:00

abstract：:Tetrodotoxin-sensitive Na(+) currents have been extensively studied because they play a major role in neuronal firing and bursting. In this study, we showed that voltage-dependent Na(+) currents are regulated in a slow manner by oxotremorine (oxo-M) and angiotensin II in rat sympathetic neurons. We found that these cu...

journal_title：Molecular pharmacology

authors： Puente EI,De la Cruz L,Arenas I,Elias-Viñas D,Garcia DE

更新日期：2016-04-01 00:00:00

abstract：:The nonselective cation channel TRPA1 (ANKTM1, p120) is a potential mediator of pain, and selective pharmacological modulation of this channel may be analgesic. Although several TRPA1 activators exist, these tend to be either reactive or of low potency and/or selectivity. The aim of the present study, therefore, was t...

journal_title：Molecular pharmacology

authors： Maher M,Ao H,Banke T,Nasser N,Wu NT,Breitenbucher JG,Chaplan SR,Wickenden AD

更新日期：2008-04-01 00:00:00

abstract：:GPR139 is an orphan G-protein-coupled receptor expressed in the central nervous system. To identify its physiologic ligand, we measured GPR139 receptor activity from recombinant cells after treatment with amino acids, orphan ligands, serum, and tissue extracts. GPR139 activity was measured using guanosine 5'-O-(3-[(35...

journal_title：Molecular pharmacology

authors： Liu C,Bonaventure P,Lee G,Nepomuceno D,Kuei C,Wu J,Li Q,Joseph V,Sutton SW,Eckert W,Yao X,Yieh L,Dvorak C,Carruthers N,Coate H,Yun S,Dugovic C,Harrington A,Lovenberg TW

更新日期：2015-11-01 00:00:00