9-beta-D-arabinofuranosyl-2-fluoroadenine inhibits expression of vascular endothelial growth factor through hypoxia-inducible factor-1 in human ovarian cancer cells.

abstract：:Vasopressin receptor subtype(s) responsible for stimulation of insulin release from pancreatic beta cells were investigated by using subtype-selective antagonists and mice that were genetically lacking either V1a or V1b receptors. Arginine vasopressin (AVP) increased insulin release from isolated mouse islet cells in ...

journal_title：Molecular pharmacology

authors： Oshikawa S,Tanoue A,Koshimizu TA,Kitagawa Y,Tsujimoto G

更新日期：2004-03-01 00:00:00

abstract：:The possibility that vasoactive intestinal polypeptide (VIP) may facilitate the nicotine-mediated induction of adrenal medullary tyrosine hydroxylase (TH) was investigated with primary cultures (5-7 days in vitro) of bovine adrenal chromaffin (BAC) cells. Exposure of BAC cells to 100 microM nicotine led to only a marg...

journal_title：Molecular pharmacology

authors： Olasmaa M,Guidotti A,Costa E

更新日期：1992-03-01 00:00:00

abstract：:Upon sustained insult, kinins are released and many kinin responses, such as inflammatory pain, adapt from a B2 receptor (B2R) type in the acute phase to a B1 receptor (B1R) type in the chronic phase. In this study, we show that kinins modulate receptor endocytosis to rapidly decrease B2R and increase B1R on the cell ...

journal_title：Molecular pharmacology

authors： Enquist J,Skröder C,Whistler JL,Leeb-Lundberg LM

更新日期：2007-02-01 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：: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：:Melanocortins (MCs) have various physiological actions on the brain. The recent cloning of neural MC receptors opened new avenues to study the effects of these neuropeptides on the nervous system. Here we investigated the structure-activity relationships (SARs) of peptides derived from adrenocorticotropic hormone (ACT...

journal_title：Molecular pharmacology

authors： Adan RA,Cone RD,Burbach JP,Gispen WH

更新日期：1994-12-01 00:00:00

abstract：:The effect of lysosomotropic agents and secretory inhibitors were compared with verapamil for their effect on the activity of doxorubicin (DOX) in multiple drug-resistant (MDR) P388 leukemia cells (P388R) and in blocking anthracycline efflux from these cells. Agents known to interact with the plasma membrane did not p...

journal_title：Molecular pharmacology

authors： Klohs WD,Steinkampf RW

更新日期：1988-08-01 00:00:00

abstract：:The regulation of cellular responsiveness to dopamine via the D2 dopamine receptor was investigated in mouse fibroblast Ltk-cells stably expressing the rat D2-short receptor [Nature (Lond.) 336:783-787 (1988)]. Dopamine inhibited forskolin-stimulated cAMP levels in these cells (half-maximal inhibition at 3.9 +/- 1.1 n...

journal_title：Molecular pharmacology

authors： Bates MD,Senogles SE,Bunzow JR,Liggett SB,Civelli O,Caron MG

更新日期：1991-01-01 00:00:00

abstract：:A Walker 256 rat carcinoma cell line (WR) has been shown to be resistant to a broad spectrum of bifunctional nitrogen mustards (NM) in cell culture. The parent cell line (WS) from which the WR cells were selected retains marked sensitivity to this class of drugs. Karyotype analysis showed that the parent WS had a chro...

journal_title：Molecular pharmacology

authors： Tew KD,Wang AL

更新日期：1982-05-01 00:00:00

abstract：:We examined the subtype-selective binding site of the beta-adrenergic receptors (betaARs). The beta(1)/beta(2)-chimeric receptors showed the importance of the second and seventh transmembrane domains (TM2 and TM7) of the beta(2)AR for the binding of the beta(2)-selective agonists such as formoterol and procaterol. Ala...

journal_title：Molecular pharmacology

authors： Isogaya M,Sugimoto Y,Tanimura R,Tanaka R,Kikkawa H,Nagao T,Kurose H

更新日期：1999-11-01 00:00:00

abstract：:Opioid analgesics are used extensively in the management of pain. Although the clinically effective opioids bind with high affinity to the mu-opioid receptor, studies have suggested that the delta-opioid agonists might represent more ideal analgesic agents, with fewer side effects. A limitation to opiate effectiveness...

journal_title：Molecular pharmacology

authors： Bot G,Blake AD,Li S,Reisine T

更新日期：1997-08-01 00:00:00

abstract：:The interaction of [3H]acetylcholine ([3H]AcCh) with the muscarinic receptor was studied in seven distinct rat brain regions and in heart atrium by employing 10 microM atropine to define specific binding. The specific binding exhibited by the labeled neurotransmitter was found to be sensitive to muscarinic but not to ...

journal_title：Molecular pharmacology

authors： Gurwitz D,Kloog Y,Sokolovsky M

更新日期：1985-09-01 00:00:00

abstract：:Many cellular signaling pathways share regulation by protein phosphatase-2A (PP2A), a widely expressed serine/threonine phosphatase, and the heterotrimeric G protein Galpha(12). PP2A activity is altered in carcinogenesis and in some neurodegenerative diseases. We have identified binding of Galpha(12) with the Aalpha s...

journal_title：Molecular pharmacology

authors： Zhu D,Tate RI,Ruediger R,Meigs TE,Denker BM

更新日期：2007-05-01 00:00:00

abstract：:Propofol, etomidate, and barbiturate anesthetics are allosteric coagonists at pentameric α1β3γ2 GABAA receptors, modulating channel activation via four biochemically established intersubunit transmembrane pockets. Etomidate selectively occupies the two β+/α- pockets, the barbiturate photolabel R-5-allyl-1-methyl-5-(m-...

journal_title：Molecular pharmacology

authors： Szabo A,Nourmahnad A,Halpin E,Forman SA

更新日期：2019-04-01 00:00:00

abstract：:Systematic series of monoamines, diamines, and triamines were used to define the structural requirements for interaction at the polyamine recognition site of the N-methyl-D-aspartate receptor complex. Effects of amines on binding of [3H]MK-801 to washed synaptic plasma membranes were measured in the presence of L-glut...

journal_title：Molecular pharmacology

authors： Romano C,Williams K,DePriest S,Seshadri R,Marshall GR,Israel M,Molinoff PB

更新日期：1992-04-01 00:00:00

abstract：:Dantrolene was recently identified as a novel inhibitor of the plasmodial surface anion channel (PSAC), an unusual ion channel on Plasmodium falciparum-infected human red blood cells. Because dantrolene is used clinically, has a high therapeutic index, and has desirable chemical synthetic properties, it may be a lead ...

journal_title：Molecular pharmacology

authors： Kang M,Lisk G,Hollingworth S,Baylor SM,Desai SA

更新日期：2005-07-01 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：:The Gαi/o-coupled dopamine D2-like receptor family comprises three subtypes: the D2 receptor (D2R), with short and long isoform variants (D2SR and D2LR), D3 receptor (D3R), and D4 receptor (D4R), with several polymorphic variants. The common overlap of norepinephrine innervation and D2-like receptor expression pattern...

journal_title：Molecular pharmacology

authors： Sánchez-Soto M,Bonifazi A,Cai NS,Ellenberger MP,Newman AH,Ferré S,Yano H

更新日期：2016-04-01 00:00:00

abstract：:The effect of endocytosis inhibitors on 5-hydroxytryptamine(2A) (5-HT(2A)) receptor desensitization and resensitization was examined in transiently transfected human embryonic kidney (HEK) 293 cells and in C6 glioma cells that endogenously express 5-HT(2A) receptors. In HEK-293 cells, 5-HT(2A) receptor desensitization...

journal_title：Molecular pharmacology

authors： Gray JA,Sheffler DJ,Bhatnagar A,Woods JA,Hufeisen SJ,Benovic JL,Roth BL

更新日期：2001-11-01 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：:SC-54628 [1-(2-methylphenyl)-4-butyl-1,3-dihydro-3-[[6-[2-(1H- tetrazol-5-yl)phenyl]-3-pyridinyl]methyl]-2H-imidazol-2-one] and its 1-(2,6-dimethylphenyl)-2H-imidazol-2-one derivative SC-54629 were potent inhibitors of 125I-angiotensin II (125I-AII) binding to rat adrenal cortex angiotensin type 1 (AT1) receptors. SC-...

journal_title：Molecular pharmacology

authors： Olins GM,Chen ST,McMahon EG,Palomo MA,Reitz DB

更新日期：1995-01-01 00:00:00

abstract：:(6R)-5,6,7,8-Tetrahydrobiopterin (BH4), which is synthesized intracellularly from GTP, caused a concentration-dependent increase in rat pheochromocytoma (PC12) cell proliferation when added exogenously. Incubation with sepiapterin, which is converted enzymatically to BH4 within cells, also increased PC12 cell prolifer...

journal_title：Molecular pharmacology

authors： Anastasiadis PZ,States JC,Imerman BA,Louie MC,Kuhn DM,Levine RA

更新日期：1996-01-01 00:00:00

abstract：:Neuroactive steroids bind to a unique site on the gamma-aminobutyric acidA (GABAA) receptor complex and allosterically modulate the binding of convulsant ([35S]t-butylbicyclophosphorothionate, [35S]TBPS), GABA ([3H]muscimol), and benzodiazepine ([3H]flunitrazepam) site ligands. In rat cortical membranes, 3 alpha-hydro...

journal_title：Molecular pharmacology

authors： Hawkinson JE,Drewe JA,Kimbrough CL,Chen JS,Hogenkamp DJ,Lan NC,Gee KW,Shen KZ,Whittemore ER,Woodward RM

更新日期：1996-05-01 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：: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：: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：:Pyrethroid insecticides are synthetic neurotoxins patterned after the naturally occurring pyrethrins. Their mechanism of action is thought to involve effects primarily at the voltage-sensitive sodium channel of both insect and mammalian neurons, although recent studies have raised the possibility that these compounds ...

journal_title：Molecular pharmacology

authors： Brown GB,Gaupp JE,Olsen RW

更新日期：1988-07-01 00:00:00

abstract：:High-affinity glycine transport in neurons and glial cells is a primary means of inactivating synaptic glycine. We have synthesized a potent selective inhibitor of glycine transporter 1 (GlyT1), and characterized its activity using a quail fibroblast cell line (QT6). The glycine transporters GlyT1A, GlyT1B, GlyT1C, an...

journal_title：Molecular pharmacology

authors： Atkinson BN,Bell SC,De Vivo M,Kowalski LR,Lechner SM,Ognyanov VI,Tham CS,Tsai C,Jia J,Ashton D,Klitenick MA

更新日期：2001-12-01 00:00:00

abstract：:Voltage-gated sodium channels (Navs) are promising targets for analgesic and antiepileptic therapies. Although specificity between Nav subtypes may be desirable to target specific neural types, such as nociceptors in pain, many broadly acting Nav inhibitors are clinically beneficial in neuropathic pain and epilepsy. H...

journal_title：Molecular pharmacology

authors： Hinckley CA,Kuryshev Y,Sers A,Barre A,Buisson B,Naik H,Hajos M

更新日期：2021-01-01 00:00:00

abstract：:Immune-mediated drug hypersensitivity reactions (IDHRs) represent a significant problem due to their unpredictable and severe nature, as well as the lack of understanding of the pathogenesis. Sulfamethoxazole (SMX), a widely used antibiotic, has been used as a model compound to investigate the underlying mechanism of ...

journal_title：Molecular pharmacology

authors： Cheng L,Stewart BJ,You Q,Petersen DR,Ware JA,Piccotti JR,Kawabata TT,Ju C

更新日期：2008-06-01 00:00:00