Megakaryocytic Smad4 Regulates Platelet Function through Syk and ROCK2 Expression.

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：:Lead (Pb(2+)) is a well-known inhibitor of voltage-dependent Ca(2+) channels in their native environments in several types of cells. However, its effects on discrete Ca(2+) channel phenotypes in isolation have not been well studied. We compared how specific subtypes of human neuronal high-voltage-activated Ca(2+) chan...

journal_title：Molecular pharmacology

authors： Peng S,Hajela RK,Atchison WD

更新日期：2002-12-01 00:00:00

abstract：:Binding by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) to the Ah receptor leads to transcriptional activation of several genes and a toxicity syndrome that includes tumor promotion, wasting, hormonal and immune system dysfunction, and death. Recent findings indicate that TCDD may also affect cardiac function. Here, we ...

journal_title：Molecular pharmacology

authors： Canga L,Paroli L,Blanck TJ,Silver RB,Rifkind AB

更新日期：1993-12-01 00:00:00

abstract：:Unlike the majority of G protein-coupled receptors, the prostaglandin E(2) (PGE(2)) E-prostanoid 3 (EP3) receptor binds agonist with high affinity that is insensitive to the presence of guanosine 5[prime]-O-(3-thio)triphosphate (GTPγS). We report the identification of mutations that confer GTPγS sensitivity to agonist...

journal_title：Molecular pharmacology

authors： Natarajan C,Hata AN,Hamm HE,Zent R,Breyer RM

更新日期：2013-01-01 00:00:00

abstract：:The mechanism underlying the crosstalk between multiple G protein-coupled receptors remains poorly understood. We previously reported that prostaglandin E receptor EP1 facilitates dopamine D1 receptor signaling in striatal slices and promotes behavioral responses induced by D1 receptor agonists. Here, using human embr...

journal_title：Molecular pharmacology

authors： Ehrlich AT,Furuyashiki T,Kitaoka S,Kakizuka A,Narumiya S

更新日期：2013-09-01 00:00:00

abstract：:Depolarization-induced 86Rb efflux, an index of K+ efflux, was developed by using mammalian cultured spinal cord neurons to study the effect of gamma aminobutyric acid (GABAB) receptor activation on Ca2(+)-activated K(+)-channels. The Ca2(+)-activated 86Rb efflux was obtained by using two methods. The first method uti...

journal_title：Molecular pharmacology

authors： Kamatchi GL,Ticku MK

更新日期：1990-09-01 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：:Multiple lines of evidence indicate that the platinum-containing cancer drugs enter cells, are distributed to various subcellular compartments, and are exported from cells via transporters that evolved to manage copper homeostasis. The cytotoxicity of the platinum drugs is directly related to how much drug enters the ...

journal_title：Molecular pharmacology

authors： Howell SB,Safaei R,Larson CA,Sailor MJ

更新日期：2010-06-01 00:00:00

abstract：:Expression of the angiotensin II type 1 receptor (AT1-R) mRNA in vascular smooth muscle cells (VSMC) is down-regulated by a variety of agonists, including growth factors, agonists of Galphaq protein-coupled receptors, and activators of adenylyl cyclase. To determine whether cAMP-dependent protein kinases (PKA) partici...

journal_title：Molecular pharmacology

authors： Wang X,Murphy TJ

更新日期：1998-09-01 00:00:00

abstract：:Two peptides, which have no significant homology with known protein structures, were obtained by microsequencing of a mu-opioid binding protein purified to homogeneity from bovine striatal membranes. Polyclonal antibodies generated against portions of these peptides immunoprecipitated up to 65% of radiolabeled purifie...

journal_title：Molecular pharmacology

authors： Gioannini TL,Yao YH,Hiller JM,Taylor LP,Simon EJ

更新日期：1993-10-01 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：:Bufuralol 1'-hydroxylation is a prototypical reaction catalyzed by cytochrome P450 (P450) 2D6, an enzyme known to show debrisoquine/sparteine-type genetic polymorphism in humans. In the present study we further examined the roles of several human P450 enzymes, as well as P450 2D6, in the hydroxylation of (+/-)-bufural...

journal_title：Molecular pharmacology

authors： Yamazaki H,Guo Z,Persmark M,Mimura M,Inoue K,Guengerich FP,Shimada T

更新日期：1994-09-01 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

abstract：:SR33557 belongs to a new class of molecules (indolizinsulfones) that act on the same receptor complex that has been characterized for other classical calcium channel effectors. The main binding properties of SR33557 to rabbit skeletal muscle are as follows. (i) Unlabeled SR33557 completely inhibits the specific bindin...

journal_title：Molecular pharmacology

authors： Schmid A,Romey G,Barhanin J,Lazdunski M

更新日期：1989-06-01 00:00:00

abstract：:Using [3H]leukotriene C4 (LTC4) and radioligand-binding techniques, specific leukotriene C4 binding sites have been identified in membranes derived from guinea pig ventricular myocardium. High performance liquid chromatography analyses indicated that, in the presence of the gamma-glutamyl transpeptidase inhibitor L-se...

journal_title：Molecular pharmacology

authors： Hogaboom GK,Mong S,Stadel JM,Crooke ST

更新日期：1985-02-01 00:00:00

abstract：:Diltiazem is a widely prescribed Ca2+ antagonist drug for cardiac arrhythmia, hypertension, and angina pectoris. Using the ancestral CaV channel construct CaVAb as a molecular model for X-ray crystallographic analysis, we show here that diltiazem targets the central cavity of the voltage-gated Ca2+ channel underneath ...

journal_title：Molecular pharmacology

authors： Tang L,Gamal El-Din TM,Lenaeus MJ,Zheng N,Catterall WA

更新日期：2019-10-01 00:00:00

abstract：:Microinjection, but not extracellular application, of cytidine-5'-diphosphate-D-glucose (CDPG) has been shown to elicit Ca(2+)-dependent currents in Xenopus laevis oocytes. These responses were comparable to those of inositol-1,4,5-trisphosphate (InsP3) in being both rapid and dose dependent. For example, maximal ampl...

journal_title：Molecular pharmacology

authors： Kim HY,Thomas D,Hanley MR

更新日期：1996-02-01 00:00:00

abstract：:In order to elucidate the key atoms and/or stereostructures necessary for the inhibitory emergence of aldose reductase, crystal structure determinations were carried out for 11 oxazolecarbamate analogues, which have similar chemical and physicochemical properties but different inhibitory activities. The molecular conf...

journal_title：Molecular pharmacology

authors： Ishida T,In Y,Ohishi H,Yamamoto D,Inoue M,Tanaka C,Ueno Y,Ohmomo Y,Kanda N,Tanaka A

更新日期：1988-09-01 00:00:00

abstract：:Two forms of the multisubunit gamma-aminobutyric acid (GABA)A receptor were expressed in Xenopus oocytes by injecting mRNA encoding the bovine GABAA receptor subunit cDNAs for alpha 1 beta 1 gamma 2L and alpha 3 beta 1 gamma 2L. The properties of these two combinations were examined by electrophysiological recording o...

journal_title：Molecular pharmacology

authors： Wafford KA,Whiting PJ,Kemp JA

更新日期：1993-02-01 00:00:00

abstract：:To study the functional role of individual alpha1-adrenergic (AR) subtypes in blood pressure (BP) regulation, we used mice lacking the alpha1B-AR and/or alpha1D-AR with the same genetic background and further studied their hemodynamic and vasoconstrictive responses. Both the alpha1D-AR knockout and alpha1B-/alpha1D-AR...

journal_title：Molecular pharmacology

authors： Hosoda C,Koshimizu TA,Tanoue A,Nasa Y,Oikawa R,Tomabechi T,Fukuda S,Shinoura H,Oshikawa S,Takeo S,Kitamura T,Cotecchia S,Tsujimoto G

更新日期：2005-03-01 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：:Batrachotoxin (BTX), from South American frogs of the genus Phyllobates, irreversibly activates voltage-gated sodium channels. Previous work demonstrated that a phenylalanine residue approximately halfway through pore-lining transmembrane segment IVS6 is a critical determinant of channel sensitivity to BTX. In this st...

journal_title：Molecular pharmacology

authors： Li HL,Hadid D,Ragsdale DS

更新日期：2002-04-01 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：:We reported previously that protein associated with Myc (PAM) interacts with the C2 domain of type V adenylyl cyclase (ACV-C2) and that purified PAM is a potent inhibitor of Galphas-stimulated ACV activity (J Biol Chem 276:47583-47589, 2001). The present study was conducted to identify the region in PAM that inhibits ...

journal_title：Molecular pharmacology

authors： Gao X,Patel TB

更新日期：2005-01-01 00:00:00

abstract：:Melanoma differentiation associated gene-7 (mda-7)/interleukin-24 (IL-24), a member of the IL-10 cytokine gene family, preferentially induces cell death in neoplastic epithelial cells types while sparing their normal counterparts. The effects of mda-7/IL-24 in acute myeloid leukemia (AML) cells have not been extensive...

journal_title：Molecular pharmacology

authors： Rahmani M,Mayo M,Dash R,Sokhi UK,Dmitriev IP,Sarkar D,Dent P,Curiel DT,Fisher PB,Grant S

更新日期：2010-12-01 00:00:00

abstract：:A conjugate molecule was synthesized by linking the DNA-intercalative antitumor drug 4'-(9-acridinylamino)methanesulfon-manisidide (mAMSA) via a 4-carboxamide side chain to a dipyrrolecarboxamide moiety structurally related to the minor groove-binding antibiotic netropsin. The molecule (netropsin/ mAMSA) behaves as a ...

journal_title：Molecular pharmacology

authors： Henichart JP,Waring MJ,Riou JF,Denny WA,Bailly C

更新日期：1997-03-01 00:00:00

abstract：:K201 (JTV-519) may prevent abnormal Ca(2+) leak from the sarcoplasmic reticulum (SR) in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors (RyRs; RyR1 and RyR2, respectively). We tested direct modulation of the SR Ca(2+)-stimulated ATPase (SERCA) and RyRs by K201. In isolated cardiac a...

journal_title：Molecular pharmacology

authors： Darcy YL,Diaz-Sylvester PL,Copello JA

更新日期：2016-08-01 00:00:00

abstract：:We determined the effect of flufenamic acid (FFA) and related derivatives on gap junction channel currents, applying the dual whole-cell patch-clamp technique to pairs of N2A neuroblastoma cells transfected with various connexins. FFA reduced gap junction channel currents in a reversible and concentration-dependent ma...

journal_title：Molecular pharmacology

authors： Srinivas M,Spray DC

更新日期：2003-06-01 00:00:00

abstract：:Pharmacological studies suggest a role for CB1 cannabinoid receptors (CB1R) in regulating neurogenesis in the adult brain. To investigate this possibility, we measured neurogenesis by intraperitoneal injection of bromodeoxyuridine (BrdU), which labels newborn neurons, in wild-type and CB1R-knockout (CB1R-KO) mice. CB1...

journal_title：Molecular pharmacology

authors： Jin K,Xie L,Kim SH,Parmentier-Batteur S,Sun Y,Mao XO,Childs J,Greenberg DA

更新日期：2004-08-01 00:00:00

abstract：:3H-Neurokinin A (3H-NKA) with high specific activity (75 Ci/mmol) was synthesized to study NKA (NK-2)-binding sites on membrane preparations of various tissues in the rat, including brain, spinal cord, duodenum, vas deferens, and ileum. The binding capacity of 3H-NKA (0.9 nM) was very low in membrane preparations of d...

journal_title：Molecular pharmacology

authors： Bergström L,Beaujouan JC,Torrens Y,Saffroy M,Glowinski J,Lavielle S,Chassaing G,Marquet A,D'Orleans-Juste P,Dion S

更新日期：1987-12-01 00:00:00