The rat homologue of the bovine alpha 1c-adrenergic receptor shows the pharmacological properties of the classical alpha 1A subtype.

abstract：:We reported previously the formation of a glutathionyl conjugate of the active metabolite (AM) of clopidogrel and the covalent modification of a cysteinyl residue of human cytochrome P450 2B6 in a reconstituted system (Mol Pharmacol 80:839-847, 2011). In this work, we extended our studies of the metabolism of clopidog...

journal_title：Molecular pharmacology

authors： Zhang H,Lau WC,Hollenberg PF

更新日期：2012-08-01 00:00:00

abstract：:Stimulatory effects of spermine at heteromeric N-methyl-D-aspartate (NMDA) receptors expressed from cloned subunits were studied by voltage-clamp recording in Xenopus oocytes. At NR1A/NR2B receptors, in the presence of a saturating concentration of glycine, the magnitude of spermine stimulation was dependent on the co...

journal_title：Molecular pharmacology

authors： Williams K

更新日期：1994-07-01 00:00:00

abstract：:Previous studies have shown that the transcription factor signal transducer and activator of transcription-3 (STAT3) in podocytes plays an important role in progression of HIV nephropathy and in collapsing forms of glomerulonephritis. Here, we have observed that application of 100 nM angiotensin II (Ang II) to culture...

journal_title：Molecular pharmacology

authors： Abkhezr M,Dryer SE

更新日期：2014-08-01 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：:Wild-type p53 is frequently mutated in late-stage ovarian cancer and has been proposed as a determinant of cisplatin chemosensitivity. We have therefore established a human ovarian cancer cell line differing only in p53 status and characterized its response after treatment with different platinum complexes. The wild-t...

journal_title：Molecular pharmacology

authors： Pestell KE,Hobbs SM,Titley JC,Kelland LR,Walton MI

更新日期：2000-03-01 00:00:00

abstract：:To investigate the roles of individual transmembrane segments (TM) of the human D3 dopamine receptor in its ligand-receptor interactions, we generated chimeric receptors in which its TMs were replaced, one at a time, partially or entirely, by the corresponding TM of the homologous human D1 receptor. Ligand binding pro...

journal_title：Molecular pharmacology

authors： Alberts GL,Pregenzer JF,Im WB

更新日期：1998-08-01 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：:The mouse adrenocortical Y-1 cell line has been found to express high affinity binding sites for neuropeptide Y (NPY). Pharmacological studies have shown that these NPY binding sites are of the Y1 type. Reverse transcription-polymerase chain reaction using primers specific for the rat Y1 receptor revealed that the NPY...

journal_title：Molecular pharmacology

authors： Weng G,Yee F,Michl P,Reis D,Wahlestedt C

更新日期：1995-07-01 00:00:00

abstract：:Airway smooth muscle (ASM) cells can act as effector cells in the initiation and/or perpetuation of airway inflammation in asthma by producing various inflammatory chemokines or cytokines. Previous studies from our laboratory and others showed that the combination of tumor necrosis factor-alpha (TNFalpha) and interfer...

journal_title：Molecular pharmacology

authors： Keslacy S,Tliba O,Baidouri H,Amrani Y

更新日期：2007-02-01 00:00:00

abstract：:Lysosomes degrade cellular proteins and organelles and regulate cell signaling by providing a surface for the formation of critical protein complexes, notably molecular target of rapamycin (mTOR) complex 1 (mTORC1). Striking differences in the lysosomes of cancer versus normal cells suggest that they could be targets ...

journal_title：Molecular pharmacology

authors： Sironi J,Aranda E,Nordstrøm LU,Schwartz EL

更新日期：2019-01-01 00:00:00

abstract：:Trypanosoma brucei encodes a relatively high number of genes of the equilibrative nucleoside transporter (ENT) family. We report here the cloning and in-depth characterization of one T. brucei brucei ENT member, TbNT9/AT-D. This transporter was expressed in Saccharomyces cerevisiae and displayed a uniquely high affini...

journal_title：Molecular pharmacology

authors： Al-Salabi MI,Wallace LJ,Lüscher A,Mäser P,Candlish D,Rodenko B,Gould MK,Jabeen I,Ajith SN,de Koning HP

更新日期：2007-03-01 00:00:00

abstract：:We examined the influence of the molecular structure of four novel adamantane derivatives on their ability to block the channels of nicotinic acetylcholine (ACh) and N-methyl-D-aspartate (NMDA) receptors. The structure of the drugs is Ad-CH2-N+H2-(CH2)5-R, where Ad is adamantane and R was varied from ammonium (IEM-175...

journal_title：Molecular pharmacology

authors： Antonov SM,Johnson JW,Lukomskaya NY,Potapyeva NN,Gmiro VE,Magazanik LG

更新日期：1995-03-01 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：:Nicotine can enhance working memory and attention. Activation of both alpha7 and beta2(*) nicotinic acetylcholine receptors (nAChRs) in the prefrontal cortex (PFC) has been implicated in these processes. The ability of presynaptic nAChRs to modulate neurotransmitter release, notably glutamate release, is postulated to...

journal_title：Molecular pharmacology

authors： Dickinson JA,Kew JN,Wonnacott S

更新日期：2008-08-01 00:00:00

abstract：:The P2Y(1) receptor is responsible for the initiation of platelet aggregation in response to ADP and plays a key role in thrombosis. Although this receptor is expressed early in the platelet lineage, the regulation of its expression during megakaryocyte differentiation is unknown. In the mouse megakaryocytic cell line...

journal_title：Molecular pharmacology

authors： Hechler B,Toselli P,Ravanat C,Gachet C,Ravid K

更新日期：2001-11-01 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：: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：:α-Conotoxins are subtype-selective nicotinic acetylcholine receptor (nAChR) antagonists. Although potent α3β2 nAChR-selective α-conotoxins have been identified, currently characterized α-conotoxins show no or only weak affinity for α4β2 nAChRs, which are, besides α7 receptors, the most abundant nAChRs in the mammalian...

journal_title：Molecular pharmacology

authors： Beissner M,Dutertre S,Schemm R,Danker T,Sporning A,Grubmüller H,Nicke A

更新日期：2012-10-01 00:00:00

abstract：:We describe the nucleic acid sequence encoding a human 5-hydroxytryptamine1D (5-HT1D) serotonin receptor and some of the functional characteristics of the gene product. The receptor gene was isolated by hybridization to a probe based on a canine thyroid cDNA (called RDC4) previously isolated by others and believed to ...

journal_title：Molecular pharmacology

authors： Hamblin MW,Metcalf MA

更新日期：1991-08-01 00:00:00

abstract：:A series of isoflavone and tyrphostin compounds were found to inhibit the degradation of cAMP by several cyclic nucleotide phosphodiesterase (PDE) isozymes. Specific hydroxyl groups on the isoflavone structure were critical for PDE isozyme-selective inhibition. Replacement of the C-7 hydroxyl group of the isoflavone w...

journal_title：Molecular pharmacology

authors： Nichols MR,Morimoto BH

更新日期：2000-04-01 00:00:00

abstract：:Glucocorticoid-induced tumor necrosis factor receptor-related (GITR) protein is a costimulatory molecule that plays a role in inflammation so that GITR-Fc fusion protein can exert an anti-inflammatory effect. To investigate the mechanism by which GITR-Fc exerts its effects, we first used GITR knock-out (GITR(-/-)) mic...

journal_title：Molecular pharmacology

authors： Nocentini G,Cuzzocrea S,Genovese T,Bianchini R,Mazzon E,Ronchetti S,Esposito E,Rosanna DP,Bramanti P,Riccardi C

更新日期：2008-06-01 00:00:00

abstract：:We have identified four new mu-opiod receptor (MOR)-1 exons, indicating that the gene now contains at least nine exons spanning more than 200 kilobases. Replacement of exon 4 by combinations of the new exons yields three new receptors. When expressed in Chinese hamster ovary cells, all three variants displayed high af...

journal_title：Molecular pharmacology

authors： Pan YX,Xu J,Bolan E,Abbadie C,Chang A,Zuckerman A,Rossi G,Pasternak GW

更新日期：1999-08-01 00:00:00

abstract：:Human serum butyrylcholinesterase (Hu BChE) is a promising therapeutic against the toxicity of chemical warfare nerve agents. We have showed previously that recombinant (r) Hu BChE can be expressed at very high levels, 400 to 600 U/ml in mouse blood, by delivering the Hu BChE gene using adenovirus (Ad). Here, we repor...

journal_title：Molecular pharmacology

authors： Chilukuri N,Duysen EG,Parikh K,diTargiani R,Doctor BP,Lockridge O,Saxena A

更新日期：2009-09-01 00:00:00

abstract：:P2X receptors are trimeric membrane proteins. When they bind extracellular ATP, a conformational change occurs that opens a transmembrane ion channel. The ATP-binding pocket is formed in a cleft between two subunits, and a critical amino acid residue for ATP contact is Lys⁶⁹ (P2X2 numbering). In the present work, we s...

journal_title：Molecular pharmacology

authors： Stelmashenko O,Lalo U,Yang Y,Bragg L,North RA,Compan V

更新日期：2012-10-01 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：:It has long been believed that the cortical actin cytoskeleton plays an important role in regulating the secretion of hormones and neurotransmitters. In this study, we investigated the control of actin dynamics in primary neuroendocrine cells and determined the relationship of actin dynamics to various components of t...

journal_title：Molecular pharmacology

authors： Bittner MA,Holz RW

更新日期：2005-04-01 00:00:00

abstract：:This study identifies signaling pathways activated by the beta(2)-/beta(3)-adrenoceptor (AR) agonist zinterol, the selective beta(3)-AR agonist L755507, and the selective beta(3)-AR antagonist L748337 in CHO-K1 cells expressing human beta(3)-adrenoceptors. Zinterol and L755507 caused a robust concentration-dependent i...

journal_title：Molecular pharmacology

authors： Sato M,Hutchinson DS,Evans BA,Summers RJ

更新日期：2008-11-01 00:00:00

abstract：:Tetrodotoxin-sensitive Na(+) currents have been extensively studied because they play a major role in neuronal firing and bursting. In this study, we showed that voltage-dependent Na(+) currents are regulated in a slow manner by oxotremorine (oxo-M) and angiotensin II in rat sympathetic neurons. We found that these cu...

journal_title：Molecular pharmacology

authors： Puente EI,De la Cruz L,Arenas I,Elias-Viñas D,Garcia DE

更新日期：2016-04-01 00:00:00

abstract：:Analysis of the distribution of mRNA encoding the serotonin (5-hydroxytryptamine) 5-HT(2A) receptor and the mu opioid peptide receptor in rat brain demonstrated their coexpression in neurons in several distinct regions. These regions included the periaqueductal gray, an area that plays an important role in morphine-in...

journal_title：Molecular pharmacology

authors： Lopez-Gimenez JF,Vilaró MT,Milligan G

更新日期：2008-11-01 00:00:00

abstract：:Aldosterone synthase (AS) regulates blood volume by synthesizing the mineralocorticoid aldosterone. Overproduction of aldosterone in the adrenal gland can lead to hypertension, a major cause of heart disease and stroke. Aldosterone production depends upon stimulation of AS expression by the renin-angiotensin system, w...

journal_title：Molecular pharmacology

authors： Adams BP,Bose HS

更新日期：2012-03-01 00:00:00