Stimulation of biliary glutathione secretion by sulfonylureas.

abstract：:AM1710 (3-(1,1-dimethyl-heptyl)-1-hydroxy-9-methoxy-benzo(c) chromen-6-one), a cannabilactone cannabinoid receptor 2 (CB2) agonist, suppresses chemotherapy-induced neuropathic pain in rodents without producing tolerance or unwanted side effects associated with CB1 receptors; however, the signaling profile of AM1710 re...

journal_title：Molecular pharmacology

authors： Li AL,Lin X,Dhopeshwarkar AS,Thomaz AC,Carey LM,Liu Y,Nikas SP,Makriyannis A,Mackie K,Hohmann AG

更新日期：2019-02-01 00:00:00

abstract：:A variety of direct and indirect techniques have revealed the existence of ATP-sensitive potassium (KATP) channels in the inner membranes of mitochondria. The molecular identity of these mitochondrial KATP (mitoKATP) channels remains unclear. We used a pharmacological approach to distinguish mitoKATP channels from cla...

journal_title：Molecular pharmacology

authors： Hu H,Sato T,Seharaseyon J,Liu Y,Johns DC,O'Rourke B,Marbán E

更新日期：1999-06-01 00:00:00

abstract：:Celecoxib (CE) is a nonsteroidal anti-inflammatory drug (NSAID) that is a specific inhibitor of cyclooxygenase 2 (COX2). It is indicated for a variety of chronic inflammatory conditions, including rheumatoid arthritis. Over the last few years, adverse cardiovascular effects and increased risk for heart attacks have be...

journal_title：Molecular pharmacology

authors： Alloza I,Baxter A,Chen Q,Matthiesen R,Vandenbroeck K

更新日期：2006-05-01 00:00:00

abstract：:The effect of the neuromuscular blocker alcuronium on the binding of N-[3H]-methylscopolamine [( 3H]NMS) and l-[3H]quinuclidinylbenzilate ([3H]QNB) to muscarinic binding sites in rat heart atria, longitudinal smooth muscle of the ileum, cerebral cortex, cerebellum, and submaxillary glands was measured using filtration...

journal_title：Molecular pharmacology

authors： Tucek S,Musílková J,Nedoma J,Proska J,Shelkovnikov S,Vorlícek J

更新日期：1990-11-01 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：:Potassium channels play fundamental roles in physiology. Chemically diverse drugs bind in the pore region of K+ channels. Here, we homology-modeled voltage- and Ca2+-gated K+ channel BK and voltage-gated Kv1.3 using the X-ray structures of MthK and Kv1.2, respectively, and simulated the binding of d-tubocurarine in th...

journal_title：Molecular pharmacology

authors： Rossokhin A,Teodorescu G,Grissmer S,Zhorov BS

更新日期：2006-04-01 00:00:00

abstract：:Three different cDNA clones, namely DM1-1, Dah1, and Dah2, encoding hepatic cytochrome P-450, were isolated from a cDNA library in lambda gt11 constructed from liver RNA of polychlorinated biphenyl-treated beagle dogs. DM1-1 was 1857 base pairs (bp) long and encoded a polypeptide of 457 residues. Dah1 was 2394 bp long...

journal_title：Molecular pharmacology

authors： Uchida T,Komori M,Kitada M,Kamataki T

更新日期：1990-11-01 00:00:00

abstract：:Thiopurine methyltransferase (TPMT) catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine. Levels of TPMT activity in human tissue are controlled by a common genetic polymorphism that is an important factor responsible for individual variation in thiopurine drug toxicity and therapeutic efficacy. Ou...

journal_title：Molecular pharmacology

authors： Honchel R,Aksoy IA,Szumlanski C,Wood TC,Otterness DM,Wieben ED,Weinshilboum RM

更新日期：1993-06-01 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：:The presence of DNA damage initiates signaling through the ataxia-telangiectasia mutated kinase (ATM) and the ATM- and the Rad3-related kinase (ATR), which phosphorylate, thus activating, the checkpoint kinases (Chk) 1 and 2, which leads to cell cycle arrest. The bifunctional DNA alkylator 1,3-bis(2-chloroethyl)-1-nit...

journal_title：Molecular pharmacology

authors： Cui B,Johnson SP,Bullock N,Ali-Osman F,Bigner DD,Friedman HS

更新日期：2009-06-01 00:00:00

abstract：:The ADP-sensitive and K+ -sensitive phosphorylated forms of Na,K-ATPase (E1P and E2P, respectively) are believed to be the main phosphorylated intermediates of Na,K-ATPase. In the presence of 100 mM Na+, E2P is the major component of the phosphorylated form in all native Na,K-ATPase preparations known, including the m...

journal_title：Molecular pharmacology

authors： Yoda A,Yoda S

更新日期：1982-11-01 00:00:00

abstract：:We searched for sites on the alpha-subunit of the fast Na(+) channel responsible for the difference in GTX (grayanotoxin) sensitivity of the skeletal- and cardiac-muscle Na(+) current. cDNA clones, encoding the skeletal or cardiac isoforms of the alpha-subunit, were inserted into a mammalian expression vector and tran...

journal_title：Molecular pharmacology

authors： Kimura T,Yamaoka K,Kinoshita E,Maejima H,Yuki T,Yakehiro M,Seyama I

更新日期：2001-10-01 00:00:00

abstract：:Aldehyde dehydrogenase-2 (ALDH2) catalyzes vascular bioactivation of the antianginal drug nitroglycerin (GTN) to yield nitric oxide (NO) or a related species that activates soluble guanylate cyclase (sGC), resulting in cGMP-mediated vasodilation. Accordingly, established ALDH2 inhibitors attenuate GTN-induced vasorela...

journal_title：Molecular pharmacology

authors： Neubauer R,Neubauer A,Wölkart G,Schwarzenegger C,Lang B,Schmidt K,Russwurm M,Koesling D,Gorren AC,Schrammel A,Mayer B

更新日期：2013-09-01 00:00:00

abstract：:We have investigated various nitric oxide (NO) synthase inhibitors for their affinity and selectivity toward the three human isoenzymes in radioligand binding experiments. Therefore, we developed the new radioligand [(3)H]2-amino-4-picoline to measure binding of these compounds to the three human NO synthase (NOS) iso...

journal_title：Molecular pharmacology

authors： Boer R,Ulrich WR,Klein T,Mirau B,Haas S,Baur I

更新日期：2000-11-01 00:00:00

abstract：:The intermediate-conductance Ca2+-activated K+ channel (KCa3.1) constitutes an attractive pharmacological target for immunosuppression, fibroproliferative disorders, atherosclerosis, and stroke. However, there currently is no available crystal structure of this medically relevant channel that could be used for structu...

journal_title：Molecular pharmacology

authors： Nguyen HM,Singh V,Pressly B,Jenkins DP,Wulff H,Yarov-Yarovoy V

更新日期：2017-04-01 00:00:00

abstract：:Multidrug resistance-associated protein 2 (MRP2) transports glutathione conjugates, glucuronide conjugates, and sulfated conjugates of bile acids. In the present study, we examined the role of charged amino acids in the transmembrane domains of rat Mrp2, conserved among MRP families, using the isolated membrane vesicl...

journal_title：Molecular pharmacology

authors： Ito K,Suzuki H,Sugiyama Y

更新日期：2001-05-01 00:00:00

abstract：:Cannabinoids have been implicated in the reduction of glioma growth. The present study investigated a possible relationship between the recently shown induction of cyclooxygenase (COX)-2 expression by the endocannabinoid analog R(+)methanandamide [R(+)-MA] and its effect on the viability of H4 human neuroglioma cells....

journal_title：Molecular pharmacology

authors： Hinz B,Ramer R,Eichele K,Weinzierl U,Brune K

更新日期：2004-12-01 00:00:00

abstract：:Pancreatic cancer is one of the most lethal types of tumors with no effective therapy available; is currently the third leading cause of cancer in developed countries; and is predicted to become the second deadliest cancer in the United States by 2030. Due to the marginal benefits of current standard chemotherapy, the...

journal_title：Molecular pharmacology

authors： Carozzo A,Yaneff A,Gómez N,Di Siervi N,Sahores A,Diez F,Attorresi AI,Rodríguez-González Á,Monczor F,Fernández N,Abba M,Shayo C,Davio C

更新日期：2019-07-01 00:00:00

abstract：:In cells expressing both the insulin receptor isoform A (IRA) and the insulin-like growth factor-1 receptor (IGF1R), the presence of hybrid receptors, made up of an alphabeta-IRA chain associated with an alphabeta-IGF1R chain, has been demonstrated. These heterodimers are found in normal cells, and they also seem to p...

journal_title：Molecular pharmacology

authors： Blanquart C,Gonzalez-Yanes C,Issad T

更新日期：2006-11-01 00:00:00

abstract：:GABAA receptors are modulated by a variety of compounds, including the neurosteroids and barbiturates. Although the effects of barbiturates on alphabetagamma isoforms, thought to dominate phasic (synaptic) GABAergic inhibition, have been extensively studied, the effects of pentobarbital on kinetic properties of alphab...

journal_title：Molecular pharmacology

authors： Feng HJ,Bianchi MT,Macdonald RL

更新日期：2004-10-01 00:00:00

abstract：:Nitric oxide (NO) possesses potent anti-inflammatory properties; however, an over-production of NO will promote inflammation and induce cell and tissue dysfunction. Thus, the ability to precisely regulate NO production could prove beneficial in controlling damage. In this study, advantage was taken of the well charact...

journal_title：Molecular pharmacology

authors： Bian K,Harari Y,Zhong M,Lai M,Castro G,Weisbrodt N,Murad F

更新日期：2001-04-01 00:00:00

abstract：:The 90-kDa heat shock family (HSP90) of protein and two-component histidine kinases, although quite distinct at the primary amino acid sequence level, share a common structural ATP-binding domain known as the Bergerat fold. The Bergerat fold is important for the ATPase activity and associated chaperone function of HSP...

journal_title：Molecular pharmacology

authors： Besant PG,Lasker MV,Bui CD,Turck CW

更新日期：2002-08-01 00:00:00

abstract：:delta-Opioid receptor (DOR) promoter exhibited a cell-type-specific expression pattern. Protein-DNA interactions in this promoter were identified by dimethyl sulfate in vivo footprinting analysis of NG108-15 cells, expressing endogenous DOR. Complete protection of the putative Sp1 cis-element and partial protection of...

journal_title：Molecular pharmacology

authors： Smirnov D,Im HJ,Loh HH

更新日期：2001-08-01 00:00:00

abstract：:Binding by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) to the Ah receptor leads to transcriptional activation of several genes and a toxicity syndrome that includes tumor promotion, wasting, hormonal and immune system dysfunction, and death. Recent findings indicate that TCDD may also affect cardiac function. Here, we ...

journal_title：Molecular pharmacology

authors： Canga L,Paroli L,Blanck TJ,Silver RB,Rifkind AB

更新日期：1993-12-01 00:00:00

abstract：:Recently we demonstrated that the effects of beta 2-adrenoceptor (AR) stimulation to augment Ca2+ current (ICa), cytosolic Ca2+ (Cai) transients, and contractility in rat ventricular myocytes are largely dissociated from its effect to increase cellular cAMP levels. This result suggested that beta 2ARs might be coupled...

journal_title：Molecular pharmacology

authors： Xiao RP,Ji X,Lakatta EG

更新日期：1995-02-01 00:00:00

abstract：:The ability of dopamine agonists and antagonists to compete with [3H]spiperone binding to rat striatal membrane preparations at 4, 15, 26, and 37 degrees varied markedly with temperature. Dopamine and the dopamine agonist 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene hydrobromide (ADTN) were more potent at lower...

journal_title：Molecular pharmacology

authors： Kilpatrick GJ,el Tayar N,Van de Waterbeemd H,Jenner P,Testa B,Marsden CD

更新日期：1986-09-01 00:00:00

abstract：:Understanding the structures of active and inactive agonist- and antagonist-bound receptor complexes is of great interest. In this work, we focus on position 30 of cholecystokinin (CCK) and its spatial approximation with the type A CCK receptor. For this, we developed two photoaffinity labeling probes, replacing the n...

journal_title：Molecular pharmacology

authors： Dong M,Hadac EM,Pinon DI,Miller LJ

更新日期：2005-06-01 00:00:00

abstract：:We show here that arsenite (As(3+)) elicits multiple effects on gene control, such as the interruption of cell cycle control by initiating G(2)/M arrest as well as inhibiting the aryl hydrocarbon (Ah) receptor-mediated 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-inducible expression of CYP1A1. This raises the question ...

journal_title：Molecular pharmacology

authors： Bonzo JA,Chen S,Galijatovic A,Tukey RH

更新日期：2005-04-01 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：:All five (m1-m5) muscarinic receptors are sensitive to allosteric regulation, but gallamine is considerably more potent in slowing the dissociation of N-[3H]methylscopolamine (NMS) from the m2 subtype than from the m3 or m5 subtypes. To study the structural basis for the preference of gallamine for the m2 subtype, we ...

journal_title：Molecular pharmacology

authors： Ellis J,Seidenberg M,Brann MR

更新日期：1993-09-01 00:00:00