Alteration of intracellular cAMP levels and beating rates of cultured chick cardiac cells by Bordetella pertussis adenylate cyclase.

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：:The interactions between beta-adrenergic receptor (beta AR) antagonists and the beta(2)AR were studied with the use of photoaffinity labels. A proteolytic map of the receptor was made and confirmed through amino-terminal amino acid sequencing by locating sites of derivatization. [125I]Iodoazidothiophenylalprenolol (IA...

journal_title：Molecular pharmacology

authors： Hockerman GH,Girvin ME,Malbon CC,Ruoho AE

更新日期：1996-06-01 00:00:00

abstract：:Selegiline, a selective monoamine oxidase type B inhibitor, is beneficial in the treatment of Parkinson's disease. However, this beneficial effect is only transient, and patients must ultimately resort to treatment with standard levodopa therapy. We studied the effects of chronic selegiline treatment on the rat nigros...

journal_title：Molecular pharmacology

authors： Vrana SL,Azzaro AJ,Vrana KE

更新日期：1992-05-01 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：:Macrophage production of growth factors for fibroblasts, in particular platelet-derived growth factor B [PDGF(B)] and transforming growth factor-beta (TGF-beta), is thought to be central to the pathogenesis of pulmonary fibrosis. In a search for anti-inflammatory agents that might prevent this process, we asked whethe...

journal_title：Molecular pharmacology

authors： Wangoo A,Haynes AR,Sutcliffe SP,Sorooshian M,Shaw RJ

更新日期：1992-10-01 00:00:00

abstract：:Although the thiopurine drugs 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) are well established agents for the treatment of leukemia, controversies remain regarding their main mode of action. Previous evidence has suggested that although 6-TG exerts a cytotoxic effect through incorporation of 6-thioguanine nucleot...

journal_title：Molecular pharmacology

authors： Coulthard SA,Hogarth LA,Little M,Matheson EC,Redfern CP,Minto L,Hall AG

更新日期：2002-07-01 00:00:00

abstract：:15-Deoxy-Delta(12,14)-prostaglandin J(2) (15d-PGJ(2)) is a cyclopentenonic prostaglandin endowed with powerful anti-inflammatory activities, as shown in animal models of inflammatory/autoimmune diseases, where pharmacological administration of this prostanoid can ameliorate inflammation and local tissue damage via act...

journal_title：Molecular pharmacology

authors： Fionda C,Nappi F,Piccoli M,Frati L,Santoni A,Cippitelli M

更新日期：2007-11-01 00:00:00

abstract：:ATP-gated purinergic receptors (P2XRs) are a family of cation-permeable channels that conduct Ca(2+) and facilitate voltage-sensitive Ca(2+) entry in excitable cells. To study Ca(2+) signaling by P2XRs and its dependence on voltage-sensitive Ca(2+) influx, we expressed eight cloned P2XR subtypes individually in gonado...

journal_title：Molecular pharmacology

authors： Koshimizu TA,Van Goor F,Tomić M,Wong AO,Tanoue A,Tsujimoto G,Stojilkovic SS

更新日期：2000-11-01 00:00:00

abstract：:The levels of hepatic mRNAs for several enzymes involved in drug metabolism were measured following administration to rats of either phenobarbitone or 2-allyl-2-isopropylacetamide. There was a substantial elevation in the mRNA levels for cytochromes P450 IIB1, IIB2, and IIIA1, epoxide hydrolase, glutathione-S-transfer...

journal_title：Molecular pharmacology

authors： Srivastava G,Hansen AJ,Bawden MJ,May BK

更新日期：1990-10-01 00:00:00

abstract：:The heptadecapeptide orphanin FQ (OFQ) has been identified as the endogenous ligand for a G protein-coupled receptor (OFQ-R), which, despite its high degree of sequence similarity to opioid receptors, fails to bind opioid ligands. We developed two radioligands for the OFQ-R: a tritiated native OFQ peptide ([3H]OFQ) an...

journal_title：Molecular pharmacology

authors： Ardati A,Henningsen RA,Higelin J,Reinscheid RK,Civelli O,Monsma FJ Jr

更新日期：1997-05-01 00:00:00

abstract：:Multidrug resistance protein 1 (MRP1) is a member of the "C" branch of the ATP-binding cassette transporter superfamily. The NH(2)-proximal nucleotide-binding domain (NBD1) of MRP1 differs functionally from its COOH-proximal domain (NBD2). NBD1 displays intrinsic high-affinity ATP binding and little ATPase activity. I...

journal_title：Molecular pharmacology

authors： Payen L,Gao M,Westlake C,Theis A,Cole SP,Deeley RG

更新日期：2005-06-01 00:00:00

abstract：:The role of mitogen-activated protein kinase signaling and the transcription factor c-Jun in epidermal growth factor (EGF)-induced expression of 12-lipoxygenase in human epidermoid carcinoma A431 cells was studied. EGF increased the activation of extracellular signal-regulated kinase (ERK) and c-Jun amino terminal kin...

journal_title：Molecular pharmacology

authors： Chen BK,Kung HC,Tsai TY,Chang WC

更新日期：2000-01-01 00:00:00

abstract：:For several GPCRs, discrimination between agonism and antagonism is possible on the basis of thermodynamics parameters, such as binding enthalpy and entropy. In this study, we analyze whether agonists and antagonists can also be discriminated thermodynamically at the histamine H(1) receptor (H(1)R). Because previous s...

journal_title：Molecular pharmacology

authors： Wittmann HJ,Seifert R,Strasser A

更新日期：2009-07-01 00:00:00

abstract：:The human dopamine and norepinephrine transporters (hDAT and hNET, respectively) control neurotransmitter levels within the synaptic cleft and are the site of action for amphetamine (AMPH) and cocaine. We investigated the role of a threonine residue within the highly conserved and putative phosphorylation sequence RET...

journal_title：Molecular pharmacology

authors： Guptaroy B,Fraser R,Desai A,Zhang M,Gnegy ME

更新日期：2011-03-01 00:00:00

abstract：:The chemical reaction of 1,4-benzoquinone with glutathione results in the formation of adducts that exhibit increasing degrees of glutathione substitution. Purification of these adducts and analysis by 1H and 13C nuclear magnetic resonance spectroscopy revealed the products of the reaction to be 2-(glutathion-S-yl)hyd...

journal_title：Molecular pharmacology

authors： Lau SS,Hill BA,Highet RJ,Monks TJ

更新日期：1988-12-01 00:00:00

abstract：:Two different mechanisms leading to increased current have been described for the small-molecule human ether-à-go-go-related gene (herg) activator NS1643 [1,3-bis-(2-hydroxy-5-trifluoromethylphenyl)-urea]. On herg1a channels expressed in Xenopus laevis oocytes, it mainly acts via attenuation of inactivation and for ra...

journal_title：Molecular pharmacology

authors： Schuster AM,Glassmeier G,Bauer CK

更新日期：2011-11-01 00:00:00

abstract：:The transient receptor potential cation channel subfamily V member 1 (TRPV1) is known as a thermosensor and integrator of inflammation-induced hyperalgesia. TRPV1 is expressed in a subpopulation of primary afferent neurons that express several different neurotransmitters. The role of the TRPV1 channel in the developme...

journal_title：Molecular pharmacology

authors： Rogoz K,Andersen HH,Kullander K,Lagerström MC

更新日期：2014-02-01 00:00:00

abstract：:Styrylquinoline derivatives (SQ) efficiently inhibit the 3'-processing activity of integrase (IN) with IC50 values of between 0.5 and 5 microM. We studied the mechanism of action of these compounds in vitro. First, we used steady-state fluorescence anisotropy to assay the effects of the SQ derivatives on the formation...

journal_title：Molecular pharmacology

authors： Deprez E,Barbe S,Kolaski M,Leh H,Zouhiri F,Auclair C,Brochon JC,Le Bret M,Mouscadet JF

更新日期：2004-01-01 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：:The human caudate and putamen contain two high affinity binding sites for [3H]spiroperidol. Both of these affinity states exhibit dopaminergic selectivity. Ascorbic acid, at 0.1 mM, induces a slow loss of the low affinity component of [3H]spiroperidol binding in these tissues. The addition of guanyl nucleotides to the...

journal_title：Molecular pharmacology

authors： Andorn AC,Bacon BR,Nguyen-Hunh AT,Parlato SJ,Stitts JA

更新日期：1988-02-01 00:00:00

abstract：:Mitochondrial disorders are devastating genetic diseases for which efficacious therapies are still an unmet need. Recent studies report that increased availability of intracellular NAD obtained by inhibition of the NAD-consuming enzyme poly(ADP-ribose) polymerase (PARP)-1 or supplementation with the NAD-precursor nico...

journal_title：Molecular pharmacology

authors： Felici R,Lapucci A,Cavone L,Pratesi S,Berlinguer-Palmini R,Chiarugi A

更新日期：2015-06-01 00:00:00

abstract：:The recent molecular cloning of the genes encoding three somatostatin (SRIF) receptor subtypes has allowed for the individual expression of these receptors in mammalian cells and characterization of their respective pharmacological profiles. In the present study, we have investigated the affinities of a battery of SRI...

journal_title：Molecular pharmacology

authors： Raynor K,Murphy WA,Coy DH,Taylor JE,Moreau JP,Yasuda K,Bell GI,Reisine T

更新日期：1993-06-01 00:00:00

abstract：:Receptors have well-conserved regions that are recognized and activated by hormones and neurotransmitters. Most drugs bind to these sites and mimic or block the action of the native ligands. Using a high-throughput functional screen, we identified a potent and selective M(1) muscarinic receptor agonist from a novel st...

journal_title：Molecular pharmacology

authors： Spalding TA,Trotter C,Skjaerbaek N,Messier TL,Currier EA,Burstein ES,Li D,Hacksell U,Brann MR

更新日期：2002-06-01 00:00:00

abstract：:The UGT1 locus is felt to be highly conserved between species, as is evident from the characterization of the locus in rodents and humans. In rabbits, cDNAs encoding proteins homologous to human UGT1A4, UGT1A6, and UGT1A7 have previously been identified. Here we demonstrate by Southern blot analysis, using exon 1 dive...

journal_title：Molecular pharmacology

authors： Li Q,Lamb G,Tukey RH

更新日期：2000-07-01 00:00:00

abstract：:The organic anions picrate (2,4,6-trinitrophenol) and niflumate (2-[[3-(trifluoromethyl)phenyl]-amino]-3-pyridinecarboxylate) were examined for their effects on radioligand binding to the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex. Neither organic anion produced the enhancement of [35S] t-butylbicy...

journal_title：Molecular pharmacology

authors： Evoniuk G,Skolnick P

更新日期：1988-12-01 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：:Dynamin is a GTPase enzyme involved in membrane constriction and fission during endocytosis. Phospholipid binding via its pleckstrin homology domain maximally stimulates dynamin activity. We developed a series of surface-active small-molecule inhibitors, such as myristyl trimethyl ammonium bromide (MiTMAB) and octadec...

journal_title：Molecular pharmacology

authors： Quan A,McGeachie AB,Keating DJ,van Dam EM,Rusak J,Chau N,Malladi CS,Chen C,McCluskey A,Cousin MA,Robinson PJ

更新日期：2007-12-01 00:00:00

abstract：:The tetrapeptide Arg-Leu-Tyr-Glu (RLYE), a vascular endothelial growth factor (VEGF) receptor-2 antagonist, has been used previously either alone or in combination with chemotherapeutic drugs for treating colorectal cancer in a mouse model. We analyzed the half-life of the peptide and found that because of degradation...

journal_title：Molecular pharmacology

authors： Yun JA,Kim J,Baek YY,Park W,Park M,Kim S,Kim T,Choi S,Jeoung D,Lee H,Won MH,Kim JY,Ha KS,Kwon YG,Kim YM

更新日期：2019-12-01 00:00:00

abstract：:The nucleoside analog 5-azacytidine is an archetypical drug for epigenetic cancer therapy, and its clinical effectiveness has been demonstrated in the treatment of myelodysplastic syndromes (MDS) and acute myelogenous leukemia (AML). However, therapy resistance in patients with MDS/AML remains a challenging issue. Mem...

journal_title：Molecular pharmacology

authors： Hummel-Eisenbeiss J,Hascher A,Hals PA,Sandvold ML,Müller-Tidow C,Lyko F,Rius M

更新日期：2013-09-01 00:00:00

abstract：:Phosphodiesterase-9 (PDE9) inhibitors have been studied as potential therapeutics for treatment of central nervous system diseases and diabetes. Here, we report the discovery of a new category of PDE9 inhibitors by rational design on the basis of the crystal structures. The best compound, (S)-6-((1-(4-chlorophenyl)eth...

journal_title：Molecular pharmacology

authors： Huang M,Shao Y,Hou J,Cui W,Liang B,Huang Y,Li Z,Wu Y,Zhu X,Liu P,Wan Y,Ke H,Luo HB

更新日期：2015-11-01 00:00:00