Adenovirus-transduced human butyrylcholinesterase in mouse blood functions as a bioscavenger of chemical warfare nerve agents.

abstract：:Isoproterenol increases and decreases contractile force at low and high concentrations, respectively, through beta(2)-adrenoceptors overexpressed in transgenic mouse heart (TG4), consistent with activation of both G(s) and G(i) proteins. Using TG4 hearts, we demonstrated that epinephrine behaves like isoproterenol, bu...

journal_title：Molecular pharmacology

authors： Heubach JF,Ravens U,Kaumann AJ

更新日期：2004-05-01 00:00:00

abstract：:The pharmacological effects of angiotensin II (AII) are potently inhibited by several peptide and recently synthesized nonpeptide AII receptor antagonists. The interaction of sarcosine1, isoleucine8-AII (sarile), sarcosine1,O-methyltyrosine4-AII (sarmesin), and the nonpeptide AII antagonists 2-n-butyl-4-chloro-5- hydr...

journal_title：Molecular pharmacology

authors： Wienen W,Mauz AB,Van Meel JC,Entzeroth M

更新日期：1992-06-01 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：:The gamma-aminobutyric acid-A (GABA(A)) receptor complex is allosterically modulated by a variety of substances, some of clinical importance. Barbiturates and neurosteroids augment GABA-currents and also directly gate the channel. A variety of gamma-butyrolactone analogues also modulate GABA-induced currents, with som...

journal_title：Molecular pharmacology

authors： Williams KL,Tucker JB,White G,Weiss DS,Ferrendelli JA,Covey DF,Krause JE,Rothman SM

更新日期：1997-07-01 00:00:00

abstract：:Neuroactive steroids are efficacious potentiators of GABA-A receptors. Recent work has identified a site in the alpha1 subunit of the GABA-A receptor, that is essential for potentiation by steroids. However, each receptor contains two copies of the alpha1 subunit. We generated concatemers of subunits so that the alpha...

journal_title：Molecular pharmacology

authors： Bracamontes JR,Steinbach JH

更新日期：2009-04-01 00:00:00

abstract：:Adenosine receptors of the A1 and A2 subtypes were characterized in membranes from DDT1 MF-2 smooth muscle cells. These cells possess a high density of A1 adenosine receptors (Bmax = 0.8-0.9 pmol/mg of protein), as measured by both agonist and antagonist radioligands. Agonists compete for [125I]N6-[2-(4-amino-3-iodoph...

journal_title：Molecular pharmacology

authors： Ramkumar V,Barrington WW,Jacobson KA,Stiles GL

更新日期：1990-02-01 00:00:00

abstract：:The inflammatory response is necessary for the host's defense against pathogens; however, uncontrolled or unregulated production of eicosanoids has been associated with several types of chronic inflammatory diseases. Thus, it is not surprising that enzymes implicated in the production of eicosanoids have been strategi...

journal_title：Molecular pharmacology

authors： Doucet MS,Jougleux JL,Poirier SJ,Cormier M,Léger JL,Surette ME,Pichaud N,Touaibia M,Boudreau LH

更新日期：2019-01-01 00:00:00

abstract：:Thyrotropin-releasing hormone (TRH) receptors were solubilized from a rat pituitary tumor cell line, GH4C1, with digitonin. Convenient assays were developed based on the ability of hydroxylapatite and polyethyleneimine-soaked glass fiber filters to adsorb the solubilized [3H]methyl-TRH-receptor complex but not free [3...

journal_title：Molecular pharmacology

authors： Phillips WJ,Hinkle PM

更新日期：1989-04-01 00:00:00

abstract：:The aliphatic adenine analogues, D-eritadenine, L-eritadenine, L-threoeritadenine, and 9-(S)-(2,3-dihydroxypropyl)adenine [(S)DHPA] function as inhibitors/inactivators of purified S-adenosylhomocysteine (AdoHcy) hydrolase, but these compounds did not induce reduction of enzyme-bound NAD+. D-Eritadenine, L-eritadenine,...

journal_title：Molecular pharmacology

authors： Schanche JS,Schanche T,Ueland PM,Holý A,Votruba I

更新日期：1984-11-01 00:00:00

abstract：:Several structural subclasses of ligands bind to the benzodiazepine (BZD) binding site of the GABA(A) receptor. Previous studies from this laboratory have suggested that imidazobenzodiazepines (i-BZDs, e.g., Ro 15-1788) require domains in the BZD binding site for high-affinity binding that are distinct from the requir...

journal_title：Molecular pharmacology

authors： Kucken AM,Teissére JA,Seffinga-Clark J,Wagner DA,Czajkowski C

更新日期：2003-02-01 00:00:00

abstract：:Ribavirin used in therapies against hepatitis C virus (HCV) is potentially efficient against other viruses but presents a high cytotoxicity. Several ribavirin triphosphate analogs modified on the ribose moiety were synthesized and tested in vitro on the RNA polymerases of HCV, phage T7, and HIV-1 reverse transcriptase...

journal_title：Molecular pharmacology

authors： Gallois-Montbrun S,Chen Y,Dutartre H,Sophys M,Morera S,Guerreiro C,Schneider B,Mulard L,Janin J,Veron M,Deville-Bonne D,Canard B

更新日期：2003-03-01 00:00:00

abstract：:Microglia, as phagocytes and antigen-presenting cells in the central nervous system, are activated in such disease processes as stroke and multiple sclerosis. Because peripheral macrophages are capable of producing endocannabinoids, we have examined endocannabinoid production in a macrophage-colony stimulating factor ...

journal_title：Molecular pharmacology

authors： Carrier EJ,Kearn CS,Barkmeier AJ,Breese NM,Yang W,Nithipatikom K,Pfister SL,Campbell WB,Hillard CJ

更新日期：2004-04-01 00:00:00

abstract：:Voltage-gated sodium (Na(V)1) channels play a critical role in modulating the excitability of sensory neurons, and human genetic evidence points to Na(V)1.7 as an essential contributor to pain signaling. Human loss-of-function mutations in SCN9A, the gene encoding Na(V)1.7, cause channelopathy-associated indifference ...

journal_title：Molecular pharmacology

authors： Schmalhofer WA,Calhoun J,Burrows R,Bailey T,Kohler MG,Weinglass AB,Kaczorowski GJ,Garcia ML,Koltzenburg M,Priest BT

更新日期：2008-11-01 00:00:00

abstract：:Glutathione-liganded binuclear dinitrosyl iron complex (glut-BDNIC) has been proposed to be a donor of nitric oxide (NO). This study was undertaken to investigate the mechanisms of vasoactivity, systemic hemodynamic effects, and pharmacokinetics of glut-BDNIC. To test the hypothesis that glut-BDNICs vasodilate by rele...

journal_title：Molecular pharmacology

authors： Liu T,Zhang M,Terry MH,Schroeder H,Wilson SM,Power GG,Li Q,Tipple TE,Borchardt D,Blood AB

更新日期：2018-05-01 00:00:00

abstract：:Retina from 1-day-old chicks is a valuable tissue model for studying neuronal nicotinic receptors because it expresses a large number of the developmentally regulated high affinity [(3)H]epibatidine labeled nicotinic receptors. Most of these receptors contain the beta4 subunit associated with different alpha subunits....

journal_title：Molecular pharmacology

authors： Barabino B,Vailati S,Moretti M,McIntosh JM,Longhi R,Clementi F,Gotti C

更新日期：2001-06-01 00:00:00

abstract：:The exchange of tritium into water from saxitoxin molecules that were radiolabeled at the C-11 methylene position was measured at 37 degrees in solution and in suspensions of brain membranes. High concentrations of membrane receptors were used to assure that more than 80% of the total saxitoxin (STX) present was speci...

journal_title：Molecular pharmacology

authors： Strichartz G

更新日期：1982-03-01 00:00:00

abstract：:The two G protein-coupled receptors (GPCRs) C-X-C chemokine receptor type 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are part of the class A chemokine GPCR family and represent important drug targets for human immunodeficiency virus (HIV) infection, cancer, and inflammation diseases. CXCR4 is one of only thre...

journal_title：Molecular pharmacology

authors： Adlere I,Caspar B,Arimont M,Dekkers S,Visser K,Stuijt J,de Graaf C,Stocks M,Kellam B,Briddon S,Wijtmans M,de Esch I,Hill S,Leurs R

更新日期：2019-12-01 00:00:00

abstract：:Agonist stimulation of group III metabotropic glutamate receptors (mGluRs) induces an inhibition of neurotransmitter release from neurons. The group III mGluRs are pharmacologically defined by activation with the glutamate analog L-amino-4-phosphonobutyric acid (L-AP4). The affinities of these receptors for L-AP4 and ...

journal_title：Molecular pharmacology

authors： Rosemond E,Wang M,Yao Y,Storjohann L,Stormann T,Johnson EC,Hampson DR

更新日期：2004-10-01 00:00:00

abstract：:The Integrated Stress Response (ISR) is a signaling program that enables cellular adaptation to stressful conditions like hypoxia and nutrient deprivation in the tumor microenvironment. An important effector of the ISR is activating transcription factor 4 (ATF4), a transcription factor that regulates genes involved in...

journal_title：Molecular pharmacology

authors： Sayers CM,Papandreou I,Guttmann DM,Maas NL,Diehl JA,Witze ES,Koong AC,Koumenis C

更新日期：2013-03-01 00:00:00

abstract：:The insecticide imidacloprid and structurally related neonicotinoids act selectively on insect nicotinic acetylcholine receptors (nAChRs). To investigate the mechanism of neonicotinoid selectivity, we have examined the effects of mutations to basic amino acid residues in loop D of the nAChR acetylcholine (ACh) binding...

journal_title：Molecular pharmacology

authors： Shimomura M,Yokota M,Ihara M,Akamatsu M,Sattelle DB,Matsuda K

更新日期：2006-10-01 00:00:00

abstract：:The decrease in mu-opioid receptor activity after chronic agonist exposure (1 microM [D-Ala(2),N-MePhe(4),Gly-ol(5)]-enkephalin) is largely due to kinase-mediated phosphorylation of intracellular receptor domains. We have recently shown that the substitution of two putative Ca(2+)/calmodulin-dependent protein kinase I...

journal_title：Molecular pharmacology

authors： Koch T,Kroslak T,Averbeck M,Mayer P,Schröder H,Raulf E,Höllt V

更新日期：2000-08-01 00:00:00

abstract：:Telomerase activity is expressed in most types of cancer cells but not in normal somatic cells, suggesting that telomerase may be an important target for cancer chemotherapy. Inhibition of telomerase results in telomere erosion, leading to the subsequent growth arrest of cancer cells followed by senescence or cell dea...

journal_title：Molecular pharmacology

authors： Kim JH,Kim JH,Lee GE,Lee JE,Chung IK

更新日期：2003-05-01 00:00:00

abstract：:Aflatrem, a mycotoxin from Aspergillus flavus, potentiates the gamma-aminobutyric acid (GABA)-induced chloride current. This positive allosteric regulatory action of aflatrem was quantitatively studied on the GABAA receptor channel expressed in Xenopus oocytes after injection with chick brain mRNA under voltage-clamp ...

journal_title：Molecular pharmacology

authors： Yao Y,Peter AB,Baur R,Sigel E

更新日期：1989-03-01 00:00:00

abstract：:The benzomorphan opiate, (-)N-allynormetazocine [(-)ANMC, (-)SKF10047], has been shown previously to bind two distinct sites on acetylcholine receptor (AChR)-rich membranes from Torpedo electroplaque. The low affinity site seems to correspond to the site for noncompetitive blockers on the AChR. The high affinity site,...

journal_title：Molecular pharmacology

authors： Coleman BA,Michel L,Oswald R

更新日期：1987-10-01 00:00:00

abstract：:The lymphocyte potassium channel Kv1.3 is widely regarded as a promising new target for immunosuppression. To identify a potent small-molecule Kv1.3 blocker, we synthesized a series of 5-phenylalkoxypsoralens and tested them by whole-cell patch clamp. The most potent compound of this series, 5-(4-phenylbutoxy)psoralen...

journal_title：Molecular pharmacology

authors： Vennekamp J,Wulff H,Beeton C,Calabresi PA,Grissmer S,Hänsel W,Chandy KG

更新日期：2004-06-01 00:00:00

abstract：:Avermectins are a family of potent broad-spectrum anthelmintic compounds, which bind with high affinity to membranes isolated from the free-living nematode Caenorhabditis elegans. Binding of avermectins is thought to modulate chloride channel activity, but the exact mechanism for anthelmintic activity remains to be de...

journal_title：Molecular pharmacology

authors： Arena JP,Liu KK,Paress PS,Cully DF

更新日期：1991-09-01 00:00:00

abstract：:Microglial activation is an invariant feature of Alzheimer's disease (AD). It is noteworthy that cannabinoids are neuroprotective by preventing β-amyloid (Aβ)-induced microglial activation both in vitro and in vivo. On the other hand, the phytocannabinoid cannabidiol (CBD) has shown anti-inflammatory properties in dif...

journal_title：Molecular pharmacology

authors： Martín-Moreno AM,Reigada D,Ramírez BG,Mechoulam R,Innamorato N,Cuadrado A,de Ceballos ML

更新日期：2011-06-01 00:00:00

abstract：:The catestatin fragment of chromogranin A is an endogenous inhibitor of nicotinic cholinergic transmission, functioning in negative feedback control of catecholamine secretion. We explored naturally occurring polymorphisms in the amino acid sequence of catestatin. Three human variants were identified: Gly364Ser, Pro37...

journal_title：Molecular pharmacology

authors： Mahata SK,Mahata M,Wen G,Wong WB,Mahapatra NR,Hamilton BA,O'Connor DT

更新日期：2004-11-01 00:00:00

abstract：:A novel cloned polymorphism of the human concentrative nucleoside transporter hCNT3 was described and functionally characterized. This variant consists of a T/C transition leading to the substitution of cysteine 602 by an arginine residue in the core of transmembrane domain 13. The resulting hCNT3(C602R) protein has t...

journal_title：Molecular pharmacology

authors： Errasti-Murugarren E,Cano-Soldado P,Pastor-Anglada M,Casado FJ

更新日期：2008-02-01 00:00:00

abstract：:Cyclic nucleotide analogs were used to study relaxation of pig coronary arteries and guinea pig tracheal smooth muscle in an attempt to determine the roles of cAMP- and cGMP-dependent protein kinases (cA-K and cG-K). In pig coronary artery strips, cGMP analogs were generally more effective than cAMP analogs in promoti...

journal_title：Molecular pharmacology

authors： Francis SH,Noblett BD,Todd BW,Wells JN,Corbin JD

更新日期：1988-10-01 00:00:00