Interaction of a benzomorphan opiate with acetylcholinesterase and the nicotinic acetylcholine receptor.

abstract：:The human CYP2C9 plays a crucial role in the metabolic clearance of a wide range of clinical therapeutics. The *2 allele is a prevalent genetic variation in CYP2C9 that is found in various populations. A marked reduction of catalytic activity toward many important drug substrates has been demonstrated by CYP2C9*2, whi...

journal_title：Molecular pharmacology

authors： Parikh SJ,Evans CM,Obi JO,Zhang Q,Maekawa K,Glass KC,Shah MB

更新日期：2020-11-01 00:00:00

abstract：:Interleukin 6 (IL-6), which is elevated in patients with congestive heart failure and acts as both a chronic marker of inflammation and an acute-phase reactant, is associated with myocardial damage. Circulating levels of arginine vasopressin (AVP) are elevated during cardiac stress and could be a factor for cardiac in...

journal_title：Molecular pharmacology

authors： Xu F,Sun S,Wang X,Ni E,Zhao L,Zhu W

更新日期：2017-09-01 00:00:00

abstract：:Neuronal cell degeneration was studied in vitro in primary rat brain neuronal cultures grown in serum-free, chemically defined, CDM R12 medium, by measuring lactate dehydrogenase (LDH) released in the culture medium. A Ca2+-dependent neuronal cell degeneration was observed after prolonged and transient exposure 30 mic...

journal_title：Molecular pharmacology

authors： Pauwels PJ,Van Assouw HP,Leysen JE,Janssen PA

更新日期：1989-10-01 00:00:00

abstract：:Adenosine acting via A2a receptors (A2aR) is a potent cerebral vasodilator that relaxes vascular smooth muscle cells (VSMCs) by a mechanism attributed to activation of cAMP-dependent protein kinase (cAK). We examined effects of adenosine and its mechanism of action on L-type Ca2+ channels in native VSMCs from rat basi...

journal_title：Molecular pharmacology

authors： Murphy K,Gerzanich V,Zhou H,Ivanova S,Dong Y,Hoffman G,West GA,Winn HR,Simard JM

更新日期：2003-09-01 00:00:00

abstract：:Lead (Pb(2+)) is a well-known inhibitor of voltage-dependent Ca(2+) channels in their native environments in several types of cells. However, its effects on discrete Ca(2+) channel phenotypes in isolation have not been well studied. We compared how specific subtypes of human neuronal high-voltage-activated Ca(2+) chan...

journal_title：Molecular pharmacology

authors： Peng S,Hajela RK,Atchison WD

更新日期：2002-12-01 00:00:00

abstract：:Histone deacetylase inhibitors (HDACis) are currently in trial or are in clinical use for the treatment of a number of tumor types. The clinical efficacy of HDACis can be partly attributed to the modulation of the cell cycle by the HDACis. Here, we have examined the effects of N-(2-aminophenyl)-4-((4-pyridin-3-ylpyrim...

journal_title：Molecular pharmacology

authors： Chia K,Beamish H,Jafferi K,Gabrielli B

更新日期：2010-09-01 00:00:00

abstract：:In this work, we evaluate the structural differences of transmembrane helix 3 in rhodopsin and the 5-hydroxytryptamine 1A (5-HT1A) receptor caused by their different amino acid sequence. Molecular dynamics simulations of helix 3 in the 5-HT1A receptor tends to bend toward helix 5, in sharp contrast to helix 3 in rhodo...

journal_title：Molecular pharmacology

authors： López-Rodríguez ML,Vicente B,Deupi X,Barrondo S,Olivella M,Morcillo MJ,Behamú B,Ballesteros JA,Sallés J,Pardo L

更新日期：2002-07-01 00:00:00

abstract：:We previously demonstrated that murine bone marrow stromal cells express high levels of cytochrome P4501B1 (CYP1B1) that metabolizes 7,12-dimethylbenza[a]anthracene (DMBA), and that DMBA activates the Ah receptor (AhR) in these cells in vitro. More recently, we reported that CYP1B1 is required for DMBA-induced lymphob...

journal_title：Molecular pharmacology

authors： Heidel SM,Holston K,Buters JT,Gonzalez FJ,Jefcoate CR,Czupyrynski CJ

更新日期：1999-12-01 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：:The action of tetrahydroaminoacridine (THA), a centrally active cholinesterase inhibitor that may provide symptomatic benefit in Alzheimer's disease, was studied on responses to the excitatory amino acid N-methyl-D-aspartate (NMDA) in cultured hippocampal neurons, using whole-cell voltage-clamp and single-channel reco...

journal_title：Molecular pharmacology

authors： Hershkowitz N,Rogawski MA

更新日期：1991-05-01 00:00:00

abstract：:A nonnaturally occurring L-configuration nucleoside analog, L-beta-5-bromovinyl-(2-hydroxymethyl)-1,3-(dioxolanyl)uracil (L-BVOddU) selectively inhibited varicella-zoster virus growth in human embryonic lung (HEL) 299 cell culture with an EC(50) of 0.055 microM, whereas no inhibition of CEM and HEL 299 cell growth or ...

journal_title：Molecular pharmacology

authors： Li L,Dutschman GE,Gullen EA,Tsujii E,Grill SP,Choi Y,Chu CK,Cheng YC

更新日期：2000-11-01 00:00:00

abstract：:5-Hydroxytryptamine3 (5-HT3) receptors are ligand-gated ion channels that mediate neurotransmission by serotonin in the central nervous system. Pharmacological inhibition of 5-HT3 receptor activity has therapeutic potential in several psychiatric diseases, including depression and anxiety. The recently approved multim...

journal_title：Molecular pharmacology

authors： Ladefoged LK,Munro L,Pedersen AJ,Lummis SCR,Bang-Andersen B,Balle T,Schiøtt B,Kristensen AS

更新日期：2018-12-01 00:00:00

abstract：:In an attempt to better understand the role of the cyclohexene ring (ring A) in the biochemical and pharmacological properties of anthracyclines related to doxorubicin and daunorubicin, we investigated the effects of introduction of a fluorine atom at position 8 of idarubicin (4-demethoxydaunorubicin) on drug molecula...

journal_title：Molecular pharmacology

authors： Animati F,Arcamone F,Bigioni M,Capranico G,Caserini C,De Cesare M,Lombardi P,Pratesi G,Salvatore C,Supino R,Zunino F

更新日期：1996-09-01 00:00:00

abstract：:Regulator of G protein signaling (RGS) proteins are a family of approximately 20 proteins that negatively regulate signaling through heterotrimeric G protein-coupled receptors. The RGS proteins act as GTPase-activating proteins (GAPs) for certain Galpha subunits and as effector antagonists for Gqalpha. Mouse RGS14 enc...

journal_title：Molecular pharmacology

authors： Cho H,Kozasa T,Takekoshi K,De Gunzburg J,Kehrl JH

更新日期：2000-09-01 00:00:00

abstract：:We reported previously that protein associated with Myc (PAM) interacts with the C2 domain of type V adenylyl cyclase (ACV-C2) and that purified PAM is a potent inhibitor of Galphas-stimulated ACV activity (J Biol Chem 276:47583-47589, 2001). The present study was conducted to identify the region in PAM that inhibits ...

journal_title：Molecular pharmacology

authors： Gao X,Patel TB

更新日期：2005-01-01 00:00:00

abstract：:The aryl hydrocarbon receptor (AHR) binds planar aromatic compounds and up-regulates the transcription of a battery of xenobiotic-metabolizing enzymes. To identify proteins involved in the biosynthesis of endogenous AHR ligands, we screened extracts of various mouse tissues for AHR signaling activity. We found heart e...

journal_title：Molecular pharmacology

authors： Bittinger MA,Nguyen LP,Bradfield CA

更新日期：2003-09-01 00:00:00

abstract：:Nafazatrom, an antithrombotic and antimetastatic agent containing a pyrazolone functionality, is a reducing substrate for the peroxidase activity of prostaglandin H (PGH) synthase. Nafazatrom inhibits the hydroperoxide-dependent oxidation of phenylbutazone, stimulates the reduction of 15-hydroperoxy-5,8,11,13-eicosate...

journal_title：Molecular pharmacology

authors： Marnett LJ,Siedlik PH,Ochs RC,Pagels WR,Das M,Honn KV,Warnock RH,Tainer BE,Eling TE

更新日期：1984-09-01 00:00:00

abstract：:Regulation of beta2-adrenergic receptor (beta2AR) levels by glucocorticoids is a physiologically important mechanism for altering beta2AR responsiveness. Glucocorticoids increase beta2AR density by increasing the rate of beta2AR gene transcription, but the cis-elements involved have not been well characterized. We now...

journal_title：Molecular pharmacology

authors： Cornett LE,Hiller FC,Jacobi SE,Cao W,McGraw DW

更新日期：1998-12-01 00:00:00

abstract：:Purified assembly-competent vimentin, an intermediate filament protein, was obtained from bovine lens in this study. The effects of withangulatin A on vimentin assembly with or without phosphorylation were examined by negative-stain electron microscopy. Soluble tetrameric vimentin was assembled into irregular fibrils ...

journal_title：Molecular pharmacology

authors： Perng MD,Cheng TJ,Chen CM,Lai YK

更新日期：1994-10-01 00:00:00

abstract：:15-Deoxy delta(12,14)-prostaglandin J(2) (15d-PGJ(2)), an activator of peroxisome proliferator-activated receptor (PPAR)-gamma and -delta, is a prostanoid metabolite with anti-inflammatory actions. In intrauterine tissues, proinflammatory cytokines and prostaglandins have been identified as playing key roles in the ma...

journal_title：Molecular pharmacology

authors： Berry EB,Keelan JA,Helliwell RJ,Gilmour RS,Mitchell MD

更新日期：2005-07-01 00:00:00

abstract：:Previous studies revealed that phenylhistamines and histaprodifens possess higher potency and affinity at guinea pig histamine H(1)-receptor (gpH(1)R) than at human histamine H(1)-receptor (hH(1)R). However, we recently identified an imidazolylpropylguanidine [N(1)-(3-cyclohexylbutanoyl)-N(2)-[3-(1H-imidazol-4-yl)-pro...

journal_title：Molecular pharmacology

authors： Strasser A,Wittmann HJ,Kunze M,Elz S,Seifert R

更新日期：2009-03-01 00:00:00

abstract：:Type II DNA topoisomerases are targets of acridine drugs. Nine mutations conferring resistance to acridines were obtained by forced molecular evolution, using methyl N-(4'-(9-acridinylamino)-3-methoxy-phenyl) methane sulfonamide (mAMSA), methyl N-(4'-(9-acridinylamino)-2-methoxy-phenyl) carbamate hydrochloride (mAMCA)...

journal_title：Molecular pharmacology

authors： Leontiou C,Watters GP,Gilroy KL,Heslop P,Cowell IG,Craig K,Lightowlers RN,Lakey JH,Austin CA

更新日期：2007-04-01 00:00:00

abstract：:Na+-d-glucose cotransporter 1 (SGLT1) is rate-limiting for glucose absorption in the small intestine. Shortly after intake of glucose-rich food, SGLT1 abundance in the luminal membrane of the small intestine is increased. This upregulation occurs via glucose-induced acceleration of the release of SGLT1-containing vesi...

journal_title：Molecular pharmacology

authors： Chintalapati C,Keller T,Mueller TD,Gorboulev V,Schäfer N,Zilkowski I,Veyhl-Wichmann M,Geiger D,Groll J,Koepsell H

更新日期：2016-11-01 00:00:00

abstract：:Targeted inhibition of oncogenes in tumor cells is a rational approach toward the development of cancer therapies based on RNA interference (RNAi). Tumors caused by human papillomavirus (HPV) infection are an ideal model system for RNAi-based cancer therapies because the oncogenes that cause cervical cancer, E6 and E7...

journal_title：Molecular pharmacology

authors： Putral LN,Bywater MJ,Gu W,Saunders NA,Gabrielli BG,Leggatt GR,McMillan NA

更新日期：2005-11-01 00:00:00

abstract：:Ovarian cancer is the leading cause of death from gynecological malignancy and has the worst prognosis of all gynecological cancers. Vascular endothelial growth factor (VEGF) plays an important role in ovarian cancer development. 9-beta-D-Arabinofuranosyl-2-fluoroadenine (Fara-A), a nucleotide analog, is frequently us...

journal_title：Molecular pharmacology

authors： Fang J,Cao Z,Chen YC,Reed E,Jiang BH

更新日期：2004-07-01 00:00:00

abstract：:The dopamine (DA) transporter (DAT) mediates the removal of released DA. DAT is the major molecular target responsible for the rewarding properties and abuse potential of the psychostimulant amphetamine (AMPH). AMPH has been shown to reduce the number of DATs at the cell surface, and this AMPH-induced cell surface DAT...

journal_title：Molecular pharmacology

authors： Kahlig KM,Lute BJ,Wei Y,Loland CJ,Gether U,Javitch JA,Galli A

更新日期：2006-08-01 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：:Prenatal exposure to diethylstilbestrol (DES) is known to cause an increased susceptibility to a wide array of clinical disorders in humans. Previous studies from our laboratory demonstrated that prenatal exposure to DES induces thymic atrophy and apoptosis in the thymus. In the current study, we investigated if such ...

journal_title：Molecular pharmacology

authors： Singh NP,Abbas IK,Menard M,Singh UP,Zhang J,Nagarkatti P,Nagarkatti M

更新日期：2015-05-01 00:00:00

abstract：:The renal outer medullary potassium channel (ROMK) is expressed in the kidney tubule and critically regulates sodium and potassium balance. The physiological functions of other inward rectifying K(+) (Kir) channels expressed in the nephron, such as Kir7.1, are less well understood in part due to the lack of selective ...

journal_title：Molecular pharmacology

authors： Lewis LM,Bhave G,Chauder BA,Banerjee S,Lornsen KA,Redha R,Fallen K,Lindsley CW,Weaver CD,Denton JS

更新日期：2009-11-01 00:00:00

abstract：:The blocking effects of guanethidine on electrically induced, neurally mediated, contractions of the guinea pig vas deferens in vitro could be markedly antagonized by the bee venom polypeptide apamin (20-60 nM), by 0.1 mM methylene blue, and (less regularly) by 0.1-0.15 mM quinine, three substances known to inhibit ca...

journal_title：Molecular pharmacology

authors： Stutzin A,Paravic F,Ormenño G,Orrego F

更新日期：1983-03-01 00:00:00