Hemodynamic Effects of Glutathione-Liganded Binuclear Dinitrosyl Iron Complex: Evidence for Nitroxyl Generation and Modulation by Plasma Albumin.

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：:The cannabinoid analog abnormal cannabidiol [abn-cbd; (-)-4-(3-3,4-trans-p-menthadien-[1,8]-yl)-olivetol] does not bind to CB(1) or CB(2) receptors, yet it acts as a full agonist in relaxing rat isolated mesenteric artery segments. Vasorelaxation by abn-cbd is endothelium-dependent, pertussis toxin-sensitive, and is i...

journal_title：Molecular pharmacology

authors： Offertáler L,Mo FM,Bátkai S,Liu J,Begg M,Razdan RK,Martin BR,Bukoski RD,Kunos G

更新日期：2003-03-01 00:00:00

abstract：:To study behavior of activated G(alpha)(s) in living cells, green fluorescent protein (GFP) was inserted within the internal amino acid sequence of G(alpha)(s) to generate a G(alpha)(s)-GFP fusion protein. The fusion protein maintained a bright green fluorescence and was identified by immunoblotting with antibodies ag...

journal_title：Molecular pharmacology

authors： Yu JZ,Rasenick MM

更新日期：2002-02-01 00:00:00

abstract：:Arrestins mediate G protein-coupled receptor desensitization, internalization, and signaling. Dopamine D(2) and D(3) receptors have similar structures but distinct characteristics of interaction with arrestins. The goals of this study were to compare arrestin-binding determinants in D(2) and D(3) receptors other than ...

journal_title：Molecular pharmacology

authors： Lan H,Liu Y,Bell MI,Gurevich VV,Neve KA

更新日期：2009-01-01 00:00:00

abstract：:We have, in the accompanying work, demonstrated the coexistence of M2 and M3 muscarinic receptors in the circular smooth muscle of canine colon. In the present study, the effects of muscarinic receptor stimulation on phosphoinositide turnover and adenylate cyclase activity were examined. In myo-[3H]inositol-labeled ci...

journal_title：Molecular pharmacology

authors： Zhang LB,Buxton IL

更新日期：1991-12-01 00:00:00

abstract：:Activation of synthesis-modulating dopamine autoreceptors by dopamine or its agonists has been shown to inhibit dopamine synthesis in the rat striatum. However, systemic administration of the direct-acting dopamine agonist apomorphine failed to inhibit dopamine synthesis in striata from rats that had received local un...

journal_title：Molecular pharmacology

authors： Bean AJ,Shepard PD,Bunney BS,Nestler EJ,Roth RH

更新日期：1988-12-01 00:00:00

abstract：:The constitutive androstane receptor (CAR) regulates mouse and human CYP2B genes through binding to the direct repeat-4 (DR4) motifs present in the phenobarbital-responsive enhancer module (PBREM). The preference of PBREM elements for nuclear receptors and the extent of cross-talk between CAR and other nuclear recepto...

journal_title：Molecular pharmacology

authors： Mäkinen J,Frank C,Jyrkkärinne J,Gynther J,Carlberg C,Honkakoski P

更新日期：2002-08-01 00:00:00

abstract：:Retina from 1-day-old chicks is a valuable tissue model for studying neuronal nicotinic receptors because it expresses a large number of the developmentally regulated high affinity [(3)H]epibatidine labeled nicotinic receptors. Most of these receptors contain the beta4 subunit associated with different alpha subunits....

journal_title：Molecular pharmacology

authors： Barabino B,Vailati S,Moretti M,McIntosh JM,Longhi R,Clementi F,Gotti C

更新日期：2001-06-01 00:00:00

abstract：:The human mu-opioid receptor (HmuOR) is a G-protein coupled receptor that mediates analgesia, euphoria and other important central and peripheral neurological functions. In this study, we found in a yeast two-hybrid screen that a protein kinase C-interacting protein (PKCI) specifically interacts with the C terminus of...

journal_title：Molecular pharmacology

authors： Guang W,Wang H,Su T,Weinstein IB,Wang JB

更新日期：2004-11-01 00:00:00

abstract：:The effect of relatively nontoxic levels of HgCl2 on semiconservative DNA synthesis and on DNA repair induced following treatment of intact cells with X-ray or ultraviolet (UV) light has been studied in cultured Chinese hamster ovary cells. In the presence of 1 microM HgCl2 the repair of DNA strand breaks induced by 4...

journal_title：Molecular pharmacology

authors： Christie NT,Cantoni O,Sugiyama M,Cattabeni F,Costa M

更新日期：1986-02-01 00:00:00

abstract：:Glyceryl trinitrate (GTN) is used in the treatment of angina pectoris and cardiac failure, but the rapid onset of GTN tolerance limits its clinical utility. Research suggests that a principal cause of tolerance is inhibition of an enzyme responsible for the production of physiologically active concentrations of NO fro...

journal_title：Molecular pharmacology

authors： DiFabio J,Ji Y,Vasiliou V,Thatcher GR,Bennett BM

更新日期：2003-11-01 00:00:00

abstract：:Stromal cell-derived factor-1 (SDF-1/CXCL-12) and vascular endothelial growth factor (VEGF), which can be secreted by hypoxic tumors, promote the generation of new blood vessels. These potent angiogenic factors stimulate endothelial cell migration via the activation of Rho GTPases and the phosphatidylinositol 3-kinase...

journal_title：Molecular pharmacology

authors： Carretero-Ortega J,Walsh CT,Hernández-García R,Reyes-Cruz G,Brown JH,Vázquez-Prado J

更新日期：2010-03-01 00:00:00

abstract：:Binding equilibria of 12 nonsteroidal, anti-inflammatory substances, salicylic acid, diflunisal, phenylbutazone, azapropazone, fenbufen, biphenylacetic acid, naproxen, flurbiprofen, ibuprofin, diclofenac, indomethacin, and benoxaprofen, to defatted human serum albumin has been investigated at 37 degrees, pH 7.4, in a ...

journal_title：Molecular pharmacology

authors： Honoré B,Brodersen R

更新日期：1984-01-01 00:00:00

abstract：:Previous biochemical studies have demonstrated that synergy between non-nucleoside reverse transcriptase (RT) inhibitors (NNRTI) and nucleoside RT inhibitors (NRTIs) is due to inhibition by the NNRTI of the rate at which HIV-1 RT facilitates ATP-mediated excision of NRTIs from chain-terminated template/primers (T/P). ...

journal_title：Molecular pharmacology

authors： Radzio J,Sluis-Cremer N

更新日期：2008-02-01 00:00:00

abstract：:We studied the mechanism by which the peptide omega-grammotoxin-SIA inhibits voltage-dependent calcium channels. Grammotoxin at concentrations of > 50 nM completely inhibited inward current carried by 2 mM barium through P-type channels in rat cerebellar Purkinje neurons when current was elicited by depolarizations up...

journal_title：Molecular pharmacology

authors： McDonough SI,Lampe RA,Keith RA,Bean BP

更新日期：1997-12-01 00:00:00

abstract：:Mammalian A2-adenosine receptor binding subunits (A2AR) can be visualized by covalent labeling with the photoaffinity crosslinking ligand 125I-2-[4-[2-[2-[(4-aminophenyl)methylcarbonylamino] ethylaminocarbonyl]ethyl]phenyl]ethylamino-5'-N-ethylcarboxamidoad enosine or directly with the azide derivative described in th...

journal_title：Molecular pharmacology

authors： Barrington WW,Jacobson KA,Stiles GL

更新日期：1990-08-01 00:00:00

abstract：:Matrix metalloproteinases (MMPs) are synthesized in response to diverse stimuli, including cytokines, growth factors, hormones, and oxidative stress. Here we show that the nitric oxide (NO) donor 2-(N,N-diethylamino)-diazenolate-2-oxide (DEA-NO) and NO from murine macrophages transcriptionally regulate MMP-13 expressi...

journal_title：Molecular pharmacology

authors： Zaragoza C,Soria E,López E,Browning D,Balbín M,López-Otín C,Lamas S

更新日期：2002-10-01 00:00:00

abstract：:Valproic acid (VPA) is a widely used antiepileptic agent that is undergoing clinical evaluation for anticancer therapy. We assessed the effects of VPA on angiogenesis in vitro and in vivo. In human umbilical vein endothelial cells, therapeutically relevant concentrations of VPA (0.25 to 1 mM) inhibited proliferation, ...

journal_title：Molecular pharmacology

authors： Michaelis M,Michaelis UR,Fleming I,Suhan T,Cinatl J,Blaheta RA,Hoffmann K,Kotchetkov R,Busse R,Nau H,Cinatl J Jr

更新日期：2004-03-01 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 effect of mercuric acetate on the activities of deoxyuridine triphosphate nucleotidohydrolase (dUTPase), DNA polymerase (alpha, beta), and uracil-DNA glycosylase has been studied in cultured human KB cells. There was a dose- and time-dependent inactivation of both dUTPase and DNA polymerase alpha activities by mer...

journal_title：Molecular pharmacology

authors： Williams MV,Winters T,Waddell KS

更新日期：1987-02-01 00:00:00

abstract：:Organic anion transporter-1 (OAT1) mediates the body disposition of a diverse array of clinically important drugs, including anti-HIV therapeutics, antitumor drugs, antibiotics, antihypertensives, and anti-inflammatories. Therefore, understanding the regulation of OAT1 has profound clinical significance. We previously...

journal_title：Molecular pharmacology

authors： Li S,Zhang Q,You G

更新日期：2013-07-01 00:00:00

abstract：:Using an oligonucleotide based on the sequence of a porcine brain muscarinic receptor cDNA, we recently cloned four distinct muscarinic receptors from the rat and human genomes. In the present study we transfected the rat homolog of the porcine brain muscarinic receptor cDNA into A9 L cells using a mammalian expressio...

journal_title：Molecular pharmacology

authors： Brann MR,Buckley NJ,Jones SV,Bonner TI

更新日期：1987-10-01 00:00:00

abstract：:By limiting unrestricted activation of intracellular effectors, compartmentalised signalling of cyclic nucleotides confers specificity to extracellular stimuli and is critical for the development and health of cells and organisms. Dissecting the molecular mechanisms that allow local control of cyclic nucleotide signal...

journal_title：Molecular pharmacology

authors： Schleicher K,Zaccolo M

更新日期：2020-02-28 00:00:00

abstract：:A central axiom of ligand-receptor theory is that agonists bind more tightly to active than to inactive receptors. However, measuring agonist affinity in inactive receptors is confounded by concomitant activation. We identified a cysteine substituted mutant γ-aminobutyric acid type A (GABAA) receptor with unique chara...

journal_title：Molecular pharmacology

authors： Stewart DS,Hotta M,Desai R,Forman SA

更新日期：2013-06-01 00:00:00

abstract：:We examined the effects on allosteric modulation and ligand binding of the mutation of amino acid residues of the human A(3) adenosine receptor (A(3)AR) that are hypothesized to be near one of three loci: the putative sodium binding site, the putative ligand binding site, and the DRY motif in transmembrane helical dom...

journal_title：Molecular pharmacology

authors： Gao ZG,Kim SK,Gross AS,Chen A,Blaustein JB,Jacobson KA

更新日期：2003-05-01 00:00:00

abstract：:The initial event upon binding of insulin-like growth factor 1 to the insulin-like growth factor type-I receptor (IGF-1R) is auto-phosphorylation of tyrosine residues within the activation loop of the kinase domain followed by phosphorylation of other receptor tyrosine residues and the subsequent activation of the int...

journal_title：Molecular pharmacology

authors： Vasilcanu R,Vasilcanu D,Sehat B,Yin S,Girnita A,Axelson M,Girnita L

更新日期：2008-03-01 00:00:00

abstract：:The interaction of hormones acting via the mobilization of calcium and stimulation of cAMP levels in cells was examined by determining the effects of carbachol and forskolin on cAMP and cGMP accumulation in mouse parotid gland. Treatment of isolated acini with either carbachol (0.01 to 20 microM) or forskolin (1 micro...

journal_title：Molecular pharmacology

authors： Watson EL,Singh JC,McPhee C,Beavo J,Jacobson KL

更新日期：1990-10-01 00:00:00

abstract：:mRNA levels for the protooncogene c-fos, measured by Northern blot analysis, were greatly increased in brains of mice undergoing ethanol withdrawal seizures. This increase was transient (levels were increased at the time of the seizure and returned to normal by 24 hr or less after seizure) and was larger in hippocampu...

journal_title：Molecular pharmacology

authors： Dave JR,Tabakoff B,Hoffman PL

更新日期：1990-03-01 00:00:00

abstract：:Stimulation of beta2-adrenoceptors with the selective beta2 agonist procaterol caused a biphasic decrease in cell surface M2 muscarinic receptor number in human embryonic lung 299 cells when measured with the hydrophilic antagonist [3H]N-methylscopolamine. In contrast, total muscarinic receptor number, measured with t...

journal_title：Molecular pharmacology

authors： Rousell J,Haddad EB,Mak JC,Webb BL,Giembycz MA,Barnes PJ

更新日期：1996-04-01 00:00:00

abstract：:Carbachol is 100 times more potent for inhibiting cyclic AMP formation than for stimulating phosphoinositide (PI) hydrolysis in chick heart cells. To determine whether this reflects differences in agonist affinity of the receptor(s) coupled to the two responses, we measured these functional responses following removal...

journal_title：Molecular pharmacology

authors： Brown JH,Goldstein D

更新日期：1986-12-01 00:00:00