Mss4 gene is up-regulated in rat brain after chronic treatment with antidepressant and down-regulated when rats are anhedonic.

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：:Increasing data indicate that brain endocannabinoid system plays a role in the effects of antidepressant medications. Here we examined the effect of in vivo exposure to the selective serotonin uptake inhibitor fluoxetine on cannabinoid type 1 (CB(1)) receptor density and functionality in the rat prefrontal cortex (PFC...

journal_title：Molecular pharmacology

authors： Mato S,Vidal R,Castro E,Díaz A,Pazos A,Valdizán EM

更新日期：2010-03-01 00:00:00

abstract：:The functional significance of the conserved amino acids within transmembrane regions II and VII of the human 5-hydroxytryptamine (5-HT)1A receptor was analyzed by oligonucleotide-directed mutagenesis followed by transient expression of the mutated receptor genes in COS-1 cells. The substitution of a conserved asparag...

journal_title：Molecular pharmacology

authors： Chanda PK,Minchin MC,Davis AR,Greenberg L,Reilly Y,McGregor WH,Bhat R,Lubeck MD,Mizutani S,Hung PP

更新日期：1993-04-01 00:00:00

abstract：:A quantum chemical study of adenosine, formycin, and their 2-NH2 and 2-F derivatives is performed. The tautomerism of neutral and protonated species as well as the protonation of adenosine, formycin, and their derivatives are theoretically studied using semiempirical MNDO and AM1, as well as ab initio STO-3G methods. ...

journal_title：Molecular pharmacology

authors： Orozco M,Canela EI,Franco R

更新日期：1989-02-01 00:00:00

abstract：:Understanding the structures of active and inactive agonist- and antagonist-bound receptor complexes is of great interest. In this work, we focus on position 30 of cholecystokinin (CCK) and its spatial approximation with the type A CCK receptor. For this, we developed two photoaffinity labeling probes, replacing the n...

journal_title：Molecular pharmacology

authors： Dong M,Hadac EM,Pinon DI,Miller LJ

更新日期：2005-06-01 00:00:00

abstract：:Fusion proteins between the human 5-hydroxytryptamine (5-HT)(1A) receptor and either wild type or certain pertussis toxin-resistant forms of G(o1)alpha and G(i1)alpha display constitutive GTPase activity that can be inhibited by the inverse agonist spiperone. Addition of recombinant regulator of G protein signaling (R...

journal_title：Molecular pharmacology

authors： Welsby PJ,Kellett E,Wilkinson G,Milligan G

更新日期：2002-05-01 00:00:00

abstract：:Expression vectors were designed and constructed to achieve optimum production of two different isozymes of rat glutathione S-transferase (GST) (EC 2.5.1.18) in COS cells, for studies of drug resistance. Promoter-enhancer elements from the simian virus 40 (SV40) early-region or the mouse alpha 2(I)-collagen gene, GST ...

journal_title：Molecular pharmacology

authors： Manoharan TH,Welch PJ,Gulick AM,Puchalski RB,Lathrop AL,Fahl WE

更新日期：1991-04-01 00:00:00

abstract：:Adult guinea pig hippocampal membranes contain two 5-hydroxytryptamine (5-HT) receptors positively coupled with an adenylate cyclase. One is a typical 5-HT1A receptor and the second is a nonclassical 5-HT receptor that we previously proposed to call 5-HT4. Here, we show that 4-amino-5-chlor-2-methoxy-benzamide derivat...

journal_title：Molecular pharmacology

authors： Bockaert J,Sebben M,Dumuis A

更新日期：1990-03-01 00:00:00

abstract：:High-throughput screening has led to the identification of small-molecule blockers of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel, but the structural basis of blocker binding remains to be defined. We developed molecular models of the CFTR channel on the basis of homology to the bac...

journal_title：Molecular pharmacology

authors： Norimatsu Y,Ivetac A,Alexander C,O'Donnell N,Frye L,Sansom MS,Dawson DC

更新日期：2012-12-01 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：:Activation of alpha 1-adrenergic receptors (alpha 1-AR) increases Na+/H+ exchange (NHE) in proximal tubule. NHE mediates the majority of active Na+ absorption in the proximal tubule. Three alpha 1-AR subtypes have been detected in kidney by molecular and binding techniques. We detected message for all three alpha 1-AR...

journal_title：Molecular pharmacology

authors： Liu F,Nesbitt T,Drezner MK,Friedman PA,Gesek FA

更新日期：1997-12-01 00:00:00

abstract：:Histone deacetylase inhibitors (HDACi), which have emerged as a new class of anticancer agents, act by modulating expression of genes controlling apoptosis or cell proliferation. Here, we compared the effect of HDACi on transcriptional activation by estrogen or glucocorticoid receptors (ER and GR, respectively), two m...

journal_title：Molecular pharmacology

authors： Rocha W,Sanchez R,Deschênes J,Auger A,Hébert E,White JH,Mader S

更新日期：2005-12-01 00:00:00

abstract：:Prostate cancer is a highly heterogenous disease in which a patient-tailored care program is much desired. Central to this goal is the development of novel targeted pharmacological interventions. To develop these treatment strategies, an understanding of the integration of cellular pathways involved in both tumorigene...

journal_title：Molecular pharmacology

authors： Assinder SJ,Dong Q,Mangs H,Richardson DR

更新日期：2009-03-01 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：:Phosphorylation of tau protein promotes stability of the axonal cytoskeleton; aberrant tau phosphorylation is implicated in the biogenesis of paired helical filaments (PHF) seen in Alzheimer's disease. Protein kinases and phosphatases that modulate tau phosphorylation have been identified using in vitro techniques; ho...

journal_title：Molecular pharmacology

authors： Garver TD,Kincaid RL,Conn RA,Billingsley ML

更新日期：1999-04-01 00:00:00

abstract：:Previous studies have shown that neural stimulation of brown adipose tissue (BAT) reorganizes the expression and activity of signaling proteins in the beta-adrenergic adenylyl cyclase pathway. Cold stress increases neural stimulation of BAT and increases alpha1-adrenergic receptor number; however, the alpha1 receptor ...

journal_title：Molecular pharmacology

authors： Granneman JG,Zhai Y,Lahners KN

更新日期：1997-04-01 00:00:00

abstract：:Beta-L-dioxolane-cytidine (L-OddC, BCH-4556, Troxacitabine), a novel L-configuration deoxycytidine analog, is under phase III clinical trial for cancer treatment. We showed that human apurinic/apyrimidinic endonuclease (APE-1) has exonuclease activity for preferentially removing L-OddC and other L-configuration nucleo...

journal_title：Molecular pharmacology

authors： Lam W,Park SY,Leung CH,Cheng YC

更新日期：2006-05-01 00:00:00

abstract：:The protease-activated receptors (PAR1 and PAR2) are unusual G protein-coupled receptors that are activated by distinct serine proteases and are coexpressed in many different cell types. Limited recent evidence suggests these closely related receptors regulate different physiological outputs in the same cell, although...

journal_title：Molecular pharmacology

authors： McCoy KL,Traynelis SF,Hepler JR

更新日期：2010-06-01 00:00:00

abstract：:Using an oligonucleotide based on the sequence of a porcine brain muscarinic receptor cDNA, we recently cloned four distinct muscarinic receptors from the rat and human genomes. In the present study we transfected the rat homolog of the porcine brain muscarinic receptor cDNA into A9 L cells using a mammalian expressio...

journal_title：Molecular pharmacology

authors： Brann MR,Buckley NJ,Jones SV,Bonner TI

更新日期：1987-10-01 00:00:00

abstract：:NAD(P):quinone acceptor oxidoreductase (quinone reductase) (DT-diaphorase, EC 1.6.99.2) is involved in the process of reductive activation of cytotoxic antitumor quinones and nitrobenzenes. In this study, we initially examined the relative abilities of mouse, rat, and human quinone reductases to reduce two prodrugs, C...

journal_title：Molecular pharmacology

authors： Chen S,Knox R,Lewis AD,Friedlos F,Workman P,Deng PS,Fung M,Ebenstein D,Wu K,Tsai TM

更新日期：1995-05-01 00:00:00

abstract：:ORKAMBI, a combination of the corrector, lumacaftor, and the potentiator, ivacaftor, partially rescues the defective processing and anion channel activity conferred by the major cystic fibrosis-causing mutation, F508del, in in vitro studies. Clinically, the improvement in lung function after ORKAMBI treatment is modes...

journal_title：Molecular pharmacology

authors： Wu YS,Jiang J,Ahmadi S,Lew A,Laselva O,Xia S,Bartlett C,Ip W,Wellhauser L,Ouyang H,Gonska T,Moraes TJ,Bear CE

更新日期：2019-10-01 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：:Glioma cells with stem cell properties, termed glioma stem-like cells (GSCs), have been linked to tumor formation, maintenance, and progression and are responsible for the failure of chemotherapy and radiotherapy. Because conventional glioma treatments often fail to eliminate GSCs completely, residual surviving GSCs a...

journal_title：Molecular pharmacology

authors： Kim RK,Kim MJ,Yoon CH,Lim EJ,Yoo KC,Lee GH,Kim YH,Kim H,Jin YB,Lee YJ,Cho CG,Oh YS,Gye MC,Suh Y,Lee SJ

更新日期：2012-09-01 00:00:00

abstract：:Smad4, a key transcription factor in the transforming growth factor-β signaling pathway, is involved in a variety of cell physiologic and pathologic processes. Here, we characterized megakaryocyte/platelet-specific Smad4 deficiency in mice to elucidate its effect on platelet function. We found that megakaryocyte/plate...

journal_title：Molecular pharmacology

authors： Wang Y,Jiang L,Mo X,Lan Y,Yang X,Liu X,Zhang J,Zhu L,Liu J,Wu X

更新日期：2017-09-01 00:00:00

abstract：:Adenosine acting via A2a receptors (A2aR) is a potent cerebral vasodilator that relaxes vascular smooth muscle cells (VSMCs) by a mechanism attributed to activation of cAMP-dependent protein kinase (cAK). We examined effects of adenosine and its mechanism of action on L-type Ca2+ channels in native VSMCs from rat basi...

journal_title：Molecular pharmacology

authors： Murphy K,Gerzanich V,Zhou H,Ivanova S,Dong Y,Hoffman G,West GA,Winn HR,Simard JM

更新日期：2003-09-01 00:00:00

abstract：:In previous studies, we have shown that mouse RAW 264.7 macrophages possess pyrimidinoceptors, coupled to a phosphoinositide-specific phospholipase C, with a higher specificity for UTP than for ATP. In the current study, we explored the mechanism involved in the UTP-induced intracellular acidification seen in this cel...

journal_title：Molecular pharmacology

authors： Lin WW,Chang SH,Wu ML

更新日期：1998-02-01 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：:In standard 3H-opioid binding assays, the benzoylhydrazone derivative of naloxone (6-desoxy-6-benzoylhydrazido-N-allyl-14-hydroxydihydronormorphi none; NalBzoH) inhibited mu, kappa, and delta binding at nanomolar concentrations. At concentrations as low as 1 nM, it also produced a wash-resistant inhibition of opioid b...

journal_title：Molecular pharmacology

authors： Price M,Gistrak MA,Itzhak Y,Hahn EF,Pasternak GW

更新日期：1989-01-01 00:00:00

abstract：:The CB1 cannabinoid receptor has been implicated in the regulation of bone remodeling and bone mass. A high bone mass (HBM) phenotype was reported in CB1-null mice generated on a CD1 background (CD1(CB1-/-) mice). By contrast, our preliminary studies in cb1-/- mice, backcrossed to C57BL/6J mice (C57(CB1-/-) mice), rev...

journal_title：Molecular pharmacology

authors： Tam J,Ofek O,Fride E,Ledent C,Gabet Y,Müller R,Zimmer A,Mackie K,Mechoulam R,Shohami E,Bab I

更新日期：2006-09-01 00:00:00

abstract：:The cannabinoid analog abnormal cannabidiol [abn-cbd; (-)-4-(3-3,4-trans-p-menthadien-[1,8]-yl)-olivetol] does not bind to CB(1) or CB(2) receptors, yet it acts as a full agonist in relaxing rat isolated mesenteric artery segments. Vasorelaxation by abn-cbd is endothelium-dependent, pertussis toxin-sensitive, and is i...

journal_title：Molecular pharmacology

authors： Offertáler L,Mo FM,Bátkai S,Liu J,Begg M,Razdan RK,Martin BR,Bukoski RD,Kunos G

更新日期：2003-03-01 00:00:00