Evidence for a PCN-P450 enzyme in chickens and comparison of its development with that of other phenobarbital-inducible forms.

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：:To study the functional role of individual alpha1-adrenergic (AR) subtypes in blood pressure (BP) regulation, we used mice lacking the alpha1B-AR and/or alpha1D-AR with the same genetic background and further studied their hemodynamic and vasoconstrictive responses. Both the alpha1D-AR knockout and alpha1B-/alpha1D-AR...

journal_title：Molecular pharmacology

authors： Hosoda C,Koshimizu TA,Tanoue A,Nasa Y,Oikawa R,Tomabechi T,Fukuda S,Shinoura H,Oshikawa S,Takeo S,Kitamura T,Cotecchia S,Tsujimoto G

更新日期：2005-03-01 00:00:00

abstract：:Intracellular recordings of membrane potassium current were made from rat locus coeruleus in vitro. The effects of agonists at mu-opioid receptors were studied on neurons from rats that had been chronically treated with morphine; these were compared with actions on neurons from control rats. Tolerance to the opioid-in...

journal_title：Molecular pharmacology

authors： Christie MJ,Williams JT,North RA

更新日期：1987-11-01 00:00:00

abstract：:A high cytoplasmic Na(+) concentration may contribute to N-methyl-D-aspartate (NMDA)-induced excitotoxicity by promoting Ca(2+) influx via reverse operation of the Na(+)/Ca(2+) exchanger (NaCaX), but may simultaneously decrease the electrochemical Ca(2+) driving force by depolarizing the plasma membrane (PM). Digital ...

journal_title：Molecular pharmacology

authors： Kiedrowski L

更新日期：1999-09-01 00:00:00

abstract：:4-PIOL is a structural analog of GABA that has low efficacy at GABAA receptor CI- channels and activates a nondesensitizing CI- conductance in central neurons. We investigated the biophysical mechanisms of its low efficacy in embryonic olfactory bulb neurons, which express a limited number of GABAA receptor subunit tr...

journal_title：Molecular pharmacology

authors： Kristiansen U,Barker JL,Serafini R

更新日期：1995-08-01 00:00:00

abstract：:Previous studies have established that two Xbal polymorphic restriction fragments [11.5 and 44 kilobases (kb)] hydridizing to a full length debrisoquin hydroxylase cDNA are associated with two different mutant alleles for the debrisoquin hydroxylase gene (IID6). An independent allele, defined by Xbal 16- and 9-kb frag...

journal_title：Molecular pharmacology

authors： Evans WE,Relling MV

更新日期：1990-05-01 00:00:00

abstract：:Although ATP-sensitive K+ channels continue to be explored for their therapeutic potential, developments in high-affinity radioligands to investigate native and recombinant KATP channels have been less forthcoming. This study reports the identification and pharmacological characterization of a novel iodinated 1,4-dihy...

journal_title：Molecular pharmacology

authors： Davis-Taber R,Molinari EJ,Altenbach RJ,Whiteaker KL,Shieh CC,Rotert G,Buckner SA,Malysz J,Milicic I,McDermott JS,Gintant GA,Coghlan MJ,Carroll WA,Scott VE,Gopalakrishnan M

更新日期：2003-07-01 00:00:00

abstract：:Electrical recordings were made in Xenopus oocytes to study the modulatory effects of steroids on gamma-aminobutyric acid (GABA) receptors expressed by RNA from mammalian brain and retina. GABA responses expressed by rat cerebral cortex poly(A)+ RNA were bicuculline-sensitive Cl- currents mediated by GABAA receptors. ...

journal_title：Molecular pharmacology

authors： Woodward RM,Polenzani L,Miledi R

更新日期：1992-01-01 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：:In the search for 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives, we have found 6-benzyl-1-(ethoxymethyl)-5-isopropyl-uracil (MKC-442) to be a highly potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). The IC50 value of MKC-442 for HIV-1 RT was 8 nM....

journal_title：Molecular pharmacology

authors： Yuasa S,Sadakata Y,Takashima H,Sekiya K,Inouye N,Ubasawa M,Baba M

更新日期：1993-10-01 00:00:00

abstract：:Despite some blockbuster G protein-coupled receptor (GPCR) drugs, only a small fraction (∼ 15%) of the more than 390 nonodorant GPCRs have been successfully targeted by the pharmaceutical industry. One way that this issue might be addressed is via translation of recent deorphanization programs that have opened the pro...

journal_title：Molecular pharmacology

authors： Bolognini D,Tobin AB,Milligan G,Moss CE

更新日期：2016-03-01 00:00:00

abstract：:Studies in vertebrate neuromuscular synapses have revealed previously that ATP, via P2Y receptors, plays a critical role in regulating postsynaptic gene expressions. An equivalent regulatory role of ATP and its P2Y receptors would not necessarily be expected for the very different situation of the brain synapses, but ...

journal_title：Molecular pharmacology

authors： Siow NL,Choi RC,Xie HQ,Kong LW,Chu GK,Chan GK,Simon J,Barnard EA,Tsim KW

更新日期：2010-12-01 00:00:00

abstract：:In Rat-1 fibroblasts, endothelin-1 and a protein kinase C-stimulating phorbol ester stimulated extracellular signal-regulated kinase (ERK), whereas phenylephrine, acting at stably transfected human alpha1A-adrenoceptors, inhibited basal and endothelin-1- and phorbol ester-stimulated ERK. On the other hand, phenylephri...

journal_title：Molecular pharmacology

authors： Alexandrov A,Keffel S,Goepel M,Michel MC

更新日期：1998-11-01 00:00:00

abstract：:Previous studies indicated that activation of alpha 1-adrenergic receptors in BC3H-1 muscle cells (S. K. Ambler and P. Taylor, J. Biol. Chem. 261:5866-5871, 1986) and muscarinic receptors in 1321N1 astrocytoma cells (S. B. Masters, T. K. Harden, and J. H. Brown, Mol. Pharmacol. 27:325-332, 1985) resulted in the rapid ...

journal_title：Molecular pharmacology

authors： Ambler SK,Thompson B,Solski PA,Brown JH,Taylor P

更新日期：1987-09-01 00:00:00

abstract：:Anaplastic thyroid carcinoma (ATC) is among the most aggressive malignancies known and is characterized with rapid growth, early invasion, and complete refractoriness to current therapies. Here we report that triptolide, a small molecule from a Chinese herb, could potently inhibit proliferation in vitro, angiogenesis ...

journal_title：Molecular pharmacology

authors： Zhu W,Ou Y,Li Y,Xiao R,Shu M,Zhou Y,Xie J,He S,Qiu P,Yan G

更新日期：2009-04-01 00:00:00

abstract：:GABAA receptors are predominantly composed of alphabetagamma and alphabetadelta isoforms in the brain. It has been proposed that alphabetagamma receptors mediate phasic inhibition, whereas alphabetadelta receptors mediate tonic inhibition. Propofol (2,6-di-isopropylphenol), a widely used anesthetic drug, exerts its ef...

journal_title：Molecular pharmacology

authors： Feng HJ,Macdonald RL

更新日期：2004-12-01 00:00:00

abstract：:Previous studies have demonstrated that cotreatment with mitogen activated-protein kinase kinase (MEK) 1/2 inhibitors (e.g., PD184352) and the checkpoint abrogator 7-hydroxystaurosporine (UCN-01) dramatically induces apoptosis in a variety of human leukemia and multiple myeloma cell types. The purpose of this study wa...

journal_title：Molecular pharmacology

authors： Dai Y,Dent P,Grant S

更新日期：2003-12-01 00:00:00

abstract：:The structure-activity relationships for vasoactive intestinal peptide (VIP) receptor binding were studied using N-terminally modified VIP analogs. VIP fragments, and VIP receptor antagonists. Tissue sources included bovine coronary artery, rat mesenteric artery, rat pituitary, rat brain synaptosomes, and rat liver. E...

journal_title：Molecular pharmacology

authors： Rorstad OP,Wanke I,Coy DH,Fournier A,Huang M

更新日期：1990-06-01 00:00:00

abstract：:Autophagy is a response of cancer cells to various anticancer therapies. It is designated as programmed cell death type II and characterized by the formation of autophagic vacuoles in the cytoplasm. The Akt/mammalian target of rapamycin (mTOR)/p70 ribosomal protein S6 kinase (p70S6K) and the extracellular signal-regul...

journal_title：Molecular pharmacology

authors： Aoki H,Takada Y,Kondo S,Sawaya R,Aggarwal BB,Kondo Y

更新日期：2007-07-01 00:00:00

abstract：:Consequent to agonist exposure, many G protein-coupled receptors undergo sequestration or internalization. Results with receptors linked to adenylate cyclase, such as the beta 2-adrenergic receptor, or receptors linked to phospholipase C (PLC) have provided conflicting results regarding the role of second messenger-de...

journal_title：Molecular pharmacology

authors： Benya RV,Akeson M,Mrozinski J,Jensen RT,Battey JF

更新日期：1994-09-01 00:00:00

abstract：:The chemokine receptor CCR2 is a G protein-coupled receptor that is activated primarily by the endogenous CC chemokine ligand 2 (CCL2). Many different small-molecule antagonists have been developed to inhibit this receptor, as it is involved in a variety of diseases characterized by chronic inflammation. Unfortunately...

journal_title：Molecular pharmacology

authors： Zweemer AJ,Nederpelt I,Vrieling H,Hafith S,Doornbos ML,de Vries H,Abt J,Gross R,Stamos D,Saunders J,Smit MJ,Ijzerman AP,Heitman LH

更新日期：2013-10-01 00:00:00

abstract：:Glutathione-S-transferase-catalyzed conjugation of glutathione (GSH) to aflatoxin B1-8,9-epoxide plays an important role in preventing binding of this ultimate carcinogen to target macromolecules. Once formed, the aflatoxin B1-epoxide-GSH conjugates are actively extruded from the cell by an unidentified ATP-dependent ...

journal_title：Molecular pharmacology

authors： Loe DW,Stewart RK,Massey TE,Deeley RG,Cole SP

更新日期：1997-06-01 00:00:00

abstract：:The putative serotonin (5-HT) agonist RU 24969 [5-methoxy-3-1,2,3,6-tetrahydropyridin-4-yl)indole; 5-MeO-THPI] has been extensively used in the study and classification of 5-HT receptors. In order to study molecular determinants for recognition of THPIs at central 5-HT recognition sites, about 25 additional THPI deriv...

journal_title：Molecular pharmacology

authors： Taylor EW,Nikam SS,Lambert G,Martin AR,Nelson DL

更新日期：1988-07-01 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：:Norcocaine nitroxide and N-hydroxynorcocaine were found to stimulate hepatic microsomal lipid peroxidation in vitro, as measured by spin-trapping techniques using the spin trap alpha-[4-pyridyl-1-oxide]-N-tert-butylnitrone. It was determined that either norcocaine nitroxide or N-hydroxynorcocaine markedly enhanced the...

journal_title：Molecular pharmacology

authors： Rosen GM,Kloss MW,Rauckman EJ

更新日期：1982-11-01 00:00:00

abstract：:The effect of cyanomorpholinyldoxorubicin, morpholinyldoxorubicin, doxorubicin, and Actinomycin D were studied on purified mouse leukemia (L1210) DNA topoisomerases I and II. DNA unwinding and cross-linking were also studied. It was found that 1) morpholinyldoxorubicin, cyanomorpholinyldoxorubicin, and Actinomycin D (...

journal_title：Molecular pharmacology

authors： Wassermann K,Markovits J,Jaxel C,Capranico G,Kohn KW,Pommier Y

更新日期：1990-07-01 00:00:00

abstract：:Although G protein-coupled receptors are often categorized in terms of their primary coupling to a given type of Gα protein subunit, it is now well established that many show promiscuous coupling and activate multiple signaling pathways. Furthermore, some agonists selectively activate signaling pathways by promoting i...

journal_title：Molecular pharmacology

authors： Evans BA,Broxton N,Merlin J,Sato M,Hutchinson DS,Christopoulos A,Summers RJ

更新日期：2011-02-01 00:00:00

abstract：:Electron affinities, approximated by lowest unoccupied molecular orbital (LUMO) energies, were determined for an extensive group of nitrated polycyclic aromatic hydrocarbons by ab initio methods at the STO-3G level. Significant correlations were demonstrated between nitroarene LUMO energy and the corresponding mutagen...

journal_title：Molecular pharmacology

authors： Maynard AT,Pedersen LG,Posner HS,McKinney JD

更新日期：1986-06-01 00:00:00

abstract：:Circular RNAs (circRNAs) are a distinct category of single-stranded, covalently closed RNAs formed by backsplicing. The functions of circRNAs are incompletely known and are under active investigation. Here, we report that in addition to traditional linear mRNAs (linRNA), mouse, rat, and human opioid receptor genes gen...

journal_title：Molecular pharmacology

authors： Irie T,Shum R,Deni I,Hunkele A,Le Rouzic V,Xu J,Wilson R,Fischer GW,Pasternak GW,Pan YX

更新日期：2019-08-01 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