Purification and characterization of the major hepatic cannabinoid hydroxylase in the mouse: a possible member of the cytochrome P-450IIC subfamily.

abstract：:Bovine adrenal zona fasciculata (AZF) cells express a noninactivating K+ current (IAC) that sets the resting membrane potential and may mediate depolarization-dependent cortisol secretion. External ATP stimulates cortisol secretion through activation of a nucleotide receptor. In whole-cell patch clamp recordings from ...

journal_title：Molecular pharmacology

authors： Xu L,Enyeart JJ

更新日期：1999-02-01 00:00:00

abstract：:We have investigated the effect of chronic flurazepam HCl treatment on the gamma-aminobutyric acid (GABA)A receptor complex in cultured mammalian cortical neurons. Chronic flurazepam (1-5 microM, for 1-10 days) treatment did not produce any changes in the morphological appearance or the cell protein content of cortica...

journal_title：Molecular pharmacology

authors： Hu XJ,Ticku MK

更新日期：1994-04-01 00:00:00

abstract：:Histone deacetylase inhibitors (HDACi), which have emerged as a new class of anticancer agents, act by modulating expression of genes controlling apoptosis or cell proliferation. Here, we compared the effect of HDACi on transcriptional activation by estrogen or glucocorticoid receptors (ER and GR, respectively), two m...

journal_title：Molecular pharmacology

authors： Rocha W,Sanchez R,Deschênes J,Auger A,Hébert E,White JH,Mader S

更新日期：2005-12-01 00:00:00

abstract：:An 'epoxygenase' eicosanoid analog, 14, 15-cis-episulfide-eicosatrienoic acid, has several unique pharmacological effects on platelets. These include (i) inhibition of ionophore A23187- but not thrombin-induced activation, (ii) inhibition of thromboxane B2 biosynthesis derived from endogenous but not exogenous arachid...

journal_title：Molecular pharmacology

authors： Bernstrom K,Malcolm K,McGee J,Maclouf J,Levy-Toledano S,Falck JR,Fitzpatrick FA

更新日期：1991-02-01 00:00:00

abstract：:The X-ray and NMR structural study of 3-carbomethoxy rifamycin S5 was undertaken in order to determine whether its low antimicrobial activity was related to a conformation of the molecule which was unfavorable for interaction with bacterial DNA-dependent RNA polymerase. However, the molecule assumes a conformation sim...

journal_title：Molecular pharmacology

authors： Brufani M,Cellai L,Cerrini S,Fedeli W,Segre A,Vaciago A

更新日期：1982-03-01 00:00:00

abstract：:Tissue plasminogen activator (tPA), a serine protease, catalyzes the conversion of plasminogen to plasmin. In the present study, we investigated the role of the tPA-plasmin system in depolarization-evoked dopamine (DA) and acetylcholine (ACh) release in the nucleus accumbens (NAc) and hippocampus, respectively, of mic...

journal_title：Molecular pharmacology

authors： Ito M,Nagai T,Kamei H,Nakamichi N,Nabeshima T,Takuma K,Yamada K

更新日期：2006-11-01 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 successful synthesis of dolastatin 11, a depsipeptide originally isolated from the mollusk Dolabella auricularia, permitted us to study its effects on cells. The compound arrested cells at cytokinesis by causing a rapid and massive rearrangement of the cellular actin filament network. In a dose-and time-dependent ...

journal_title：Molecular pharmacology

authors： Bai R,Verdier-Pinard P,Gangwar S,Stessman CC,McClure KJ,Sausville EA,Pettit GR,Bates RB,Hamel E

更新日期：2001-03-01 00:00:00

abstract：:The aim of this study was to clarify the mechanism by which cytochrome P450 (P450)-mediated catalytic activity is decreased following interferon (IFN) administration. Microsomal steroid hydroxylation was assessed to test the hypothesis that IFN selectively decreases the activities of individual P450 isozymes in male r...

journal_title：Molecular pharmacology

authors： Craig PI,Mehta I,Murray M,McDonald D,Aström A,van der Meide PH,Farrell GC

更新日期：1990-09-01 00:00:00

abstract：:The powerful analgesic effects of opioid drugs have captivated the interest of physicians and scientists for millennia, and the ability of opioid drugs to produce serious undesired effects has been recognized for a similar period of time (Kieffer and Evans, 2009). Many of these develop progressively with prolonged or ...

journal_title：Molecular pharmacology

authors： Jullié D,Gondin AB,von Zastrow M,Canals M

更新日期：2020-10-01 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：:Chimeric receptors of the beta2-adrenergic receptor in which the extracellular loops were replaced with the corresponding amino acids of the alpha1a-adrenergic receptor were generated to measure changes in alpha1-antagonist affinity. Although no changes in alpha1-antagonist affinity were measured in the beta2/alpha1a ...

journal_title：Molecular pharmacology

authors： Zhao MM,Gaivin RJ,Perez DM

更新日期：1998-03-01 00:00:00

abstract：:G protein-coupled receptor kinases (GRKs) play a key role in the process of receptor homologous desensitization. In the present study, we address the question of whether a variety of receptors coupled to different G protein subtypes and naturally expressed on the same cell are selectively regulated by GRK2. The signal...

journal_title：Molecular pharmacology

authors： Iacovelli L,Franchetti R,Grisolia D,De Blasi A

更新日期：1999-08-01 00:00:00

abstract：:The interaction of quinidine with a cloned human cardiac potassium channel (HK2) expressed in a stable mouse L cell line was studied using the whole-cell tight-seal voltage-clamp technique. Quinidine (20 microM) did not affect the initial sigmoidal activation time course of the current. However, it reduced the peak cu...

journal_title：Molecular pharmacology

authors： Snyders J,Knoth KM,Roberds SL,Tamkun MM

更新日期：1992-02-01 00:00:00

abstract：:Previously, we reported the presence of dual promoters, referred to as distal (DP) and proximal, with a negative regulatory element between them in the mouse mu-opioid receptor (mor) gene. Here we have identified a positive regulatory element influencing mor DP transcription, which contains multiple consensus binding ...

journal_title：Molecular pharmacology

authors： Im HJ,Smirnov D,Yuhi T,Raghavan S,Olsson JE,Muscat GE,Koopman P,Loh HH

更新日期：2001-06-01 00:00:00

abstract：:The observations from Dunlap and Fischbach that transmitter-mediated shortening of the duration of action potentials could be caused by a decrease in calcium conductance led to numerous studies of the mechanisms of modulation of voltage-dependent calcium channels. Calcium channels are well known targets for inhibition...

journal_title：Molecular pharmacology

authors： Strock J,Diversé-Pierluissi MA

更新日期：2004-11-01 00:00:00

abstract：:Glioma cells with stem cell properties, termed glioma stem-like cells (GSCs), have been linked to tumor formation, maintenance, and progression and are responsible for the failure of chemotherapy and radiotherapy. Because conventional glioma treatments often fail to eliminate GSCs completely, residual surviving GSCs a...

journal_title：Molecular pharmacology

authors： Kim RK,Kim MJ,Yoon CH,Lim EJ,Yoo KC,Lee GH,Kim YH,Kim H,Jin YB,Lee YJ,Cho CG,Oh YS,Gye MC,Suh Y,Lee SJ

更新日期：2012-09-01 00:00:00

abstract：:Differential display reverse transcription-polymerase chain reaction was used to identify mRNAs that are differentially expressed in the brain of rats treated chronically with the reference tricyclic antidepressant, imipramine, in comparison with control rats. The gene encoding for a mutation suppressor for Sec4-8 yea...

journal_title：Molecular pharmacology

authors： Andriamampandry C,Muller C,Schmidt-Mutter C,Gobaille S,Spedding M,Aunis D,Maitre M

更新日期：2002-12-01 00:00:00

abstract：:Several reports have been published recently demonstrating a beneficial effect of epidermal growth factor receptor (EGFR) inhibitors in improving pathologic and behavioral conditions in neurodegenerative diseases (NDDs) such as Alzheimer's disease and Amyotrophic Lateral Sclerosis (ALS) as well as the brain and spinal...

journal_title：Molecular pharmacology

authors： Tavassoly O,Sato T,Tavassoly I

更新日期：2020-07-01 00:00:00

abstract：:The μ-opioid receptor gene undergoes extensive alternative splicing to generate an array of splice variants. One group of splice variants excludes the first transmembrane (TM) domain and contains six TM domains. These 6TM variants are essential for the action of a novel class of analgesic drugs, including 3-iodobenzoy...

journal_title：Molecular pharmacology

authors： Zhang T,Xu J,Pan YX

更新日期：2020-10-01 00:00:00

abstract：:Neuronal cell lines provide a source of pure populations of neurons and allow the properties of many neurotransmitter receptors to be studied. However, none of these cells have been reported to express functional gamma-aminobutyric acid (GABA)A receptors. Indeed, there have been no reports of cell lines expressing fun...

journal_title：Molecular pharmacology

authors： Hales TG,Kim H,Longoni B,Olsen RW,Tobin AJ

更新日期：1992-08-01 00:00:00

abstract：:A method was developed to measure the formation of glutathione adducts of 1-chloro-2,4-dinitrobenzene (CDNB) and 2,4-dichloro-1-nitrobenzene (DCNB) in periportal and pericentral regions of the liver lobule in the isolated perfused rat liver by surface reflectance spectrophotometry. Conjugates of DCNB and CDNB are rele...

journal_title：Molecular pharmacology

authors： Harris C,Thurman RG

更新日期：1986-01-01 00:00:00

abstract：:Large-conductance Ca(2+)-activated K(+) (BK(Ca)) channels encoded by the Slo1 gene are ubiquitously expressed, and they play a role in regulation of many cell types. In excitable cells, BK(Ca) channels and voltage-activated Ca(2+) channels often form functional complexes that allow the cytoplasmic domains of BK(Ca) ch...

journal_title：Molecular pharmacology

authors： Zou S,Jha S,Kim EY,Dryer SE

更新日期：2008-02-01 00:00:00

abstract：:Advances in proteomic methodologies based on quantitative mass spectrometry are now transforming pharmacology and experimental biology more broadly. The present review will discuss several examples, based on work in the author's laboratory that focuses on delineating relationships between GPCR signaling and traffickin...

journal_title：Molecular pharmacology

authors： von Zastrow M

更新日期：2020-12-22 00:00:00

abstract：:We examined the role of putative trafficking sequences in two GABA(A) receptor subunits: α4 and δ. These subunits assemble with a β subunit to form a subtype of GABA(A) receptor involved in generating the "tonic" outward current. Both α4 and δ subunits contain dibasic retention motifs in homologous positions. When bas...

journal_title：Molecular pharmacology

authors： Bracamontes JR,Li P,Akk G,Steinbach JH

更新日期：2014-07-01 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：:Opioid drugs, such as morphine, and the endogenous opioid peptides, namely the enkephalins, endorphins, and dynorphins, exert a wide spectrum of physiological and behavioral effects, including effects on pain perception, mood, motor control, and autonomic functions. These effects are mediated via membrane-bound recept...

journal_title：Molecular pharmacology

authors： Raynor K,Kong H,Chen Y,Yasuda K,Yu L,Bell GI,Reisine T

更新日期：1994-02-01 00:00:00

abstract：:bTREK-1 K(+) channels set the resting membrane potential of bovine adrenal zona fasciculata (AZF) cells and function pivotally in the physiology of cortisol secretion. Adrenocorticotropic hormone controls the function and expression of bTREK-1 channels through signaling mechanisms that may involve cAMP and downstream ...

journal_title：Molecular pharmacology

authors： Enyeart JA,Liu H,Enyeart JJ

更新日期：2010-03-01 00:00:00

abstract：:EM-652 (SCH 57068) is a new orally active antiestrogen that demonstrates pure antagonistic effects in the mammary gland and endometrium. In vivo studies have shown that EM-652 is primarily glucuronidated at the 7-hydroxy position in rats and that the metabolite is present in the plasma of female monkeys and human subj...

journal_title：Molecular pharmacology

authors： Barbier O,Albert C,Martineau I,Vallée M,High K,Labrie F,Hum DW,Labrie C,Bélanger A

更新日期：2001-03-01 00:00:00

abstract：:GH3 cells show spontaneous activity characterized by bursts of action potentials and oscillations in [Ca 2+]i. This activity is modulated by the activation of exogenously expressed opioid receptors. In GH3 cells expressing only micro receptors (GH3MOR cells), the micro receptor-specific ligand [D-Ala2,N-Me-Phe4,Gly5-o...

journal_title：Molecular pharmacology

authors： Charles AC,Mostovskaya N,Asas K,Evans CJ,Dankovich ML,Hales TG

更新日期：2003-01-01 00:00:00