Are alpha9alpha10 nicotinic acetylcholine receptors a pain target for alpha-conotoxins?

abstract：:[3H]P1075 binding to membrane preparations of rabbit skeletal muscle were observed in the presence of nucleotide triphosphates or diphosphates but not AMP, cAMP, adenosine, tripolyphosphate, or pyrophosphate. Nonhydrolyzable or poorly hydrolyzable ATP analogs inhibited MgATP-supported binding. The EC50 value for MgATP...

journal_title：Molecular pharmacology

authors： Dickinson KE,Bryson CC,Cohen RB,Rogers L,Green DW,Atwal KS

更新日期：1997-09-01 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：:G protein-coupled receptor kinases (GRKs) play a key role in the process of receptor homologous desensitization. In the present study, we address the question of whether a variety of receptors coupled to different G protein subtypes and naturally expressed on the same cell are selectively regulated by GRK2. The signal...

journal_title：Molecular pharmacology

authors： Iacovelli L,Franchetti R,Grisolia D,De Blasi A

更新日期：1999-08-01 00:00:00

abstract：:A UDP-glucuronosyltransferase (UDPGT) isoenzyme capable of morphine glucuronidation has been purified to apparent homogeneity and partially characterized from hepatic microsomes of female Wistar rats which have low 3 alpha-hydroxysteroid UDPGT. A rapid and sensitive assay was developed to quantify morphine glucuronide...

journal_title：Molecular pharmacology

authors： Puig JF,Tephly TR

更新日期：1986-12-01 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：:The aim of the current study is to determine whether butein (3,4,2',4'-tetrahydroxychalcone) exhibits antiproliferative effects against tumor cells through suppression of the signal transducer and activator of transcription 3 (STAT3) activation pathway. We investigated the effects of butein on constitutive and inducib...

journal_title：Molecular pharmacology

authors： Pandey MK,Sung B,Ahn KS,Aggarwal BB

更新日期：2009-03-01 00:00:00

abstract：:We have found that stypoldione, a bright red o-quinone isolated from the brown alga Stypopodium zonale, inhibits the division of sea urchin embryos in a concentration-dependent manner (IC50 approximately 2.5 X 10(-6) M). Although previous studies have shown this marine natural product to inhibit beef brain microtubule...

journal_title：Molecular pharmacology

authors： White SJ,Jacobs RS

更新日期：1983-11-01 00:00:00

abstract：:Cholinesterase inhibitors are commonly used to improve cognition and treat psychosis and other behavioral symptoms in Alzheimer's disease, Parkinson's disease, and other neuropsychiatric conditions. However, mechanisms may exist that down-regulate the synaptic response to altered cholinergic transmission, thus limitin...

journal_title：Molecular pharmacology

authors： Volpicelli-Daley LA,Hrabovska A,Duysen EG,Ferguson SM,Blakely RD,Lockridge O,Levey AI

更新日期：2003-12-01 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：: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：:Stimulation of beta2-adrenoceptors with the selective beta2 agonist procaterol caused a biphasic decrease in cell surface M2 muscarinic receptor number in human embryonic lung 299 cells when measured with the hydrophilic antagonist [3H]N-methylscopolamine. In contrast, total muscarinic receptor number, measured with t...

journal_title：Molecular pharmacology

authors： Rousell J,Haddad EB,Mak JC,Webb BL,Giembycz MA,Barnes PJ

更新日期：1996-04-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor δ (PPARδ) has been implicated in vascular pathophysiology. However, its functions in atherogenic changes of the vascular wall have not been fully elucidated. PPARδ activated by GW501516 (2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]ph...

journal_title：Molecular pharmacology

authors： Hwang JS,Ham SA,Yoo T,Lee WJ,Paek KS,Lee CH,Seo HG

更新日期：2016-11-01 00:00:00

abstract：:The level of cellular ceramide, an apoptotic rheostat, is increased by sphingomyelinase or de novo synthesis. The expression of the glutathione S-transferase (GST) gene, whose induction accounts for cell viability, is regulated by activation of CCAAT/enhancer binding protein-beta (C/EBPbeta) and NF-E2-related factor-2...

journal_title：Molecular pharmacology

authors： Park IN,Cho IJ,Kim SG

更新日期：2004-06-01 00:00:00

abstract：:The effect of halothane on synthesis of retained and secreted proteins was investigated using isolated perfused rat livers. Anesthetic exposure rapidly inhibited synthesis of total liver proteins in a dose-dependent manner by a mechanism which appeared to involve reduced rates of both peptide chain initiation and elon...

journal_title：Molecular pharmacology

authors： Flaim KE,Jefferson LS,McGwire JB,Rannels DE

更新日期：1983-09-01 00:00:00

abstract：:The total CYP3A5 mRNA level is significantly greater in carriers of the CYP3A5*1 allele than in CYP3A5*3 homozygotes. Most of the CYP3A5*3 mRNA includes an intronic sequence (exon 3B) containing premature termination codons (PTCs) between exons 3 and 4. Two models were used to investigate the degradation of CYP3A5 mRN...

journal_title：Molecular pharmacology

authors： Busi F,Cresteil T

更新日期：2005-09-01 00:00:00

abstract：:Cadmium is a dangerous metal distributed widely in the environment. Members of our laboratory recently identified the ZIP8 transporter protein, encoded by the mouse Slc39a8 gene, to be responsible for genetic differences in response to cadmium damage of the testis. Stable retroviral infection of the ZIP8 cDNA in mouse...

journal_title：Molecular pharmacology

authors： He L,Girijashanker K,Dalton TP,Reed J,Li H,Soleimani M,Nebert DW

更新日期：2006-07-01 00:00:00

abstract：:The retinoid-related orphan receptors (RORs) and liver X receptors (LXRs) were postulated to have distinct functions. RORs play a role in tissue development and circadian rhythm, whereas LXRs are sterol sensors that affect lipid homeostasis. In this study, we revealed a novel function of RORalpha (NR1F1) in regulating...

journal_title：Molecular pharmacology

authors： Wada T,Kang HS,Angers M,Gong H,Bhatia S,Khadem S,Ren S,Ellis E,Strom SC,Jetten AM,Xie W

更新日期：2008-03-01 00:00:00

abstract：:The incorporation of leucine into protein was studied in Ca2+-depleted and Ca2+-restored preparations of normal liver cells isolated from fed, adult male rats. Ca2+-restored cells incorporated amino acid 5-10-fold more rapidly than did Ca2+-depleted cells for incubation periods up to 1 hr. Readdition of Ca2+ at suprap...

journal_title：Molecular pharmacology

authors： Brostrom CO,Bocckino SB,Brostrom MA,Galuska EM

更新日期：1986-01-01 00:00:00

abstract：:Because cytotoxicity by an alkylating agent such as N-methyl-N'-nitrosoguanidine is markedly increased in adenine methylase-deficient dam-3 Escherichia coli, it was of interest to assess whether mismatch repair was similarly important in the repair of DNA damage induced by cis-diamminedichloroplatinum(II) (CDDP). The ...

journal_title：Molecular pharmacology

authors： Fram RJ,Cusick PS,Wilson JM,Marinus MG

更新日期：1985-07-01 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：:Homopentameric complexes of either the A or As subunit of the 5-hydroxytryptamine3 receptor form Ca(2+)-permeable channels that can be activated by the selective agonist 1-(m-chlorophenyl)-biguanide (mCPBG). In both N1E-115 neuroblastoma cells and human embryonic kidney 293 cells stably expressing the 5-HT3 receptor A...

journal_title：Molecular pharmacology

authors： Hargreaves AC,Gunthorpe MJ,Taylor CW,Lummis SC

更新日期：1996-11-01 00:00:00

abstract：:CC and CXC chemokines coinduced in fibroblasts and leukocytes by cytokines and microbial agents determine the number of phagocytes infiltrating into inflamed tissues. Interleukin-8/CXCL8 and stromal cell-derived factor-1/CXCL12 significantly and dose-dependently increased the migration of monocytes, expressing the cor...

journal_title：Molecular pharmacology

authors： Gouwy M,Struyf S,Noppen S,Schutyser E,Springael JY,Parmentier M,Proost P,Van Damme J

更新日期：2008-08-01 00:00:00

abstract：:Schizophrenia (SZ), schizoaffective (SZA), and bipolar (BP) disorder are neurodevelopmental psychopathological conditions related, in part, to genetic load and, in part, to environmentally induced epigenetic dysregulation of chromatin structure and function in neocortical GABAergic, glutamatergic, and monoaminergic ne...

journal_title：Molecular pharmacology

authors： Dong E,Locci V,Gatta E,Grayson DR,Guidotti A

更新日期：2019-01-01 00:00:00

abstract：:Previous studies have demonstrated that the quinone group may play an important role in modulating the alkylating activity of quinone alkylating agents. Introduction of a quinone moiety markedly increased the alkylating activity and cytotoxic activity of the model quinone alkylating agents benzoquinone mustard and ben...

journal_title：Molecular pharmacology

authors： Begleiter A,Leith MK,Pan SS

更新日期：1991-09-01 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：:mRNA levels for the protooncogene c-fos, measured by Northern blot analysis, were greatly increased in brains of mice undergoing ethanol withdrawal seizures. This increase was transient (levels were increased at the time of the seizure and returned to normal by 24 hr or less after seizure) and was larger in hippocampu...

journal_title：Molecular pharmacology

authors： Dave JR,Tabakoff B,Hoffman PL

更新日期：1990-03-01 00:00:00

abstract：:Stimulation of N-methyl-D-aspartate (NMDA) receptors is believed to underlie long-term memory formation, and excessive NMDA receptor activation has been linked to several neuropathological conditions. Phosphorylation and activation of p42/44 mitogen-activated protein kinase (ERK) is believed to mediate many of these e...

journal_title：Molecular pharmacology

authors： Rakhit S,Clark CJ,O'shaughnessy CT,Morris BJ

更新日期：2005-04-01 00:00:00

abstract：:Although G protein-coupled receptors are often categorized in terms of their primary coupling to a given type of Gα protein subunit, it is now well established that many show promiscuous coupling and activate multiple signaling pathways. Furthermore, some agonists selectively activate signaling pathways by promoting i...

journal_title：Molecular pharmacology

authors： Evans BA,Broxton N,Merlin J,Sato M,Hutchinson DS,Christopoulos A,Summers RJ

更新日期：2011-02-01 00:00:00

abstract：:Voltage-gated sodium channels are inhibited by many local anesthetics, antiarrhythmics, and antiepileptic drugs. The local anesthetic lidocaine appears to be able to access its binding site in the sodium channel only from the membrane phase or from the internal face of the channel. In contrast, the antiepileptic drug ...

journal_title：Molecular pharmacology

authors： Jo S,Bean BP

更新日期：2014-02-01 00:00:00

abstract：:A functional interaction between peroxisome proliferator-activated receptor alpha (PPARalpha) and components of the circadian clock has been suggested, but whether these transcriptional factors interact to regulate the expression of their target genes remains obscure. Here we used a PPARalpha ligand, bezafibrate, to s...

journal_title：Molecular pharmacology

authors： Oishi K,Koyanagi S,Matsunaga N,Kadota K,Ikeda E,Hayashida S,Kuramoto Y,Shimeno H,Soeda S,Ohdo S

更新日期：2010-07-01 00:00:00