Abstract:
:The cis and trans isomers of the photoisomerizable compound, 3,3'-bis-[alpha-(trimethylammonium)methyl]azobenzene (Bis-Q), were purified by high-performance liquid chromatography using the ion-pair partitioning technique on a reverse-phase column. Solutions of cis-Bis-Q are stable at -20 degrees; at 25 degrees, thermal isomerization proceeds at a rate of 0.65%/day. cis-Bis-Q is less than 1% as potent a nicotinic agonist as the trans configuration. At concentrations of 1.5 microM or less, cis-Bis-Q exerts little or no blockade of the conductances induced by agonists. In voltage-clamped Electrophorus electroplaques exposed to cis-Bis-Q, laser flashes induce cis leads to trans photoisomerizations and increase the agonist-induced current by a factor of 20 within a few milliseconds.
journal_name
Mol Pharmacoljournal_title
Molecular pharmacologyauthors
Nerbonne JM,Sheridan RE,Chabala LD,Lester HAsubject
Has Abstractpub_date
1983-03-01 00:00:00pages
344-9issue
2eissn
0026-895Xissn
1521-0111journal_volume
23pub_type
杂志文章abstract::The endogenous bronchodilator, S-nitrosoglutathione (GSNO), increases expression, maturation, and function of both the wild-type and the DeltaF508 mutant of the cystic fibrosis transmembrane conductance regulatory protein (CFTR). Though transcriptional mechanisms of action have been identified, GSNO seems also to have...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.106.023242
更新日期:2006-10-01 00:00:00
abstract::The Notch family consists of four highly conserved transmembrane receptors. The release of the active intracellular domain requires the enzymatic activity of γ-secretase. Notch is involved in embryonic development and in many physiologic processes of normal cells, in which it regulates growth, apoptosis, and different...
journal_title:Molecular pharmacology
pub_type: 杂志文章,评审
doi:10.1124/molpharm.120.000006
更新日期:2020-11-01 00:00:00
abstract::Inhibition of catechol-O-methyltransferase (COMT; EC 2.1.1.6) is a new therapeutic strategy in the treatment of Parkinson's disease. However, nothing is known about the effects of COMT inhibition on levodopa (L-dopa)-induced toxicity in dopamine (DA) neurons. Therefore we evaluated the effects of the selective COMT in...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.57.3.589
更新日期:2000-03-01 00:00:00
abstract::The CYP2C genes are extensively regulated at the transcriptional stage. The present study shows for the first time that CYP2Cs are also regulated post-transcriptionally by microRNAs (miRNAs). By using online search engines, we found potential miRNA response elements (MREs) in the 3'-untranslated region (3'-UTR) of the...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.112.078386
更新日期:2012-09-01 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
pub_type: 杂志文章
doi:10.1124/mol.106.026815
更新日期:2006-10-01 00:00:00
abstract::In rat pancreatic zymogen granules (ZG), an ATP-sensitive K(+) conductance and a Cl(-) conductance have been characterized that are inversely regulated by an approximately 65-kDa multidrug resistance P-glycoprotein (mdr1) gene product. In search of a label for purification of this protein, we found that the dihydropyr...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:2000-02-01 00:00:00
abstract::The metabotropic glutamate 5 receptor and the cannabinoid type 1 receptor are G protein-coupled receptors that are widely expressed in the central nervous system. Metabotropic glutamate 5 receptors, present at the postsynaptic site, are coupled to Gαq/11 proteins and display an excitatory response upon activation, whe...
journal_title:Molecular pharmacology
pub_type: 杂志文章,评审
doi:10.1124/mol.116.104372
更新日期:2016-11-01 00:00:00
abstract::To understand the molecular mechanism by which the angiotensin II (AII) type 1 receptor (AT1 receptor) transduces its biological signal, we examined the role of various signaling molecules involved in AT1 receptor signaling in Chinese hamster ovary cells stably transfected with the AT1 receptor. AT1 receptor-transfect...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1996-09-01 00:00:00
abstract::Receptors for the serine protease thrombin and for lysophospholipids are coupled to G proteins and control a wide range of cellular functions, including mitogenesis. Activators of these receptors are present in blood, and can enter the brain during central nervous system (CNS) injury. Reactive astrogliosis, a prominen...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.64.5.1199
更新日期:2003-11-01 00:00:00
abstract::Valproic acid (VPA) is an effective antiepileptic drug with an additional activity for the treatment of bipolar disorder. It has been assumed that both activities arise from a common target. At the molecular level, VPA targets a number of distinct proteins that are involved in signal transduction. VPA inhibition of in...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.106.030601
更新日期:2007-03-01 00:00:00
abstract::Systematic series of monoamines, diamines, and triamines were used to define the structural requirements for interaction at the polyamine recognition site of the N-methyl-D-aspartate receptor complex. Effects of amines on binding of [3H]MK-801 to washed synaptic plasma membranes were measured in the presence of L-glut...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1992-04-01 00:00:00
abstract::Interleukin-2 (IL-2) is an immunoregulatory cytokine whose biological effects are mediated through interaction with specific receptors on the surface of target cells. Due to its presumed role in generating a normal immune response, IL-2 is being evaluated for the treatment of a variety of tumors, in addition to infect...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1995-01-01 00:00:00
abstract::Hepatocyte nuclear factor 4alpha (HNF4alpha) is a key transcription factor for the constitutive expression of cytochromes P450 (P450s) in the liver. However, human hepatoma HepG2 cells show a high level of HNF4alpha but express only marginal P450 levels. We found that the HNF4alpha-mediated P450 transcription in HepG2...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.106.025403
更新日期:2006-11-01 00:00:00
abstract::We examined the influence of the molecular structure of four novel adamantane derivatives on their ability to block the channels of nicotinic acetylcholine (ACh) and N-methyl-D-aspartate (NMDA) receptors. The structure of the drugs is Ad-CH2-N+H2-(CH2)5-R, where Ad is adamantane and R was varied from ammonium (IEM-175...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1995-03-01 00:00:00
abstract::Cytochrome P450 2C6 (CYP2C6) is a developmentally regulated, constitutively expressed form of rat liver microsomal cytochrome P450 that in the liver of adult male rats is induced to a limited extent by phenobarbital. The gene is not expressed at detectable levels in the lung, kidney, or brain. It is expressed and indu...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1994-07-01 00:00:00
abstract::Antibodies against synthetic peptides of the D2 dopamine receptor were used, in combination with photoaffinity labeling, to localize the region of ligand binding in the receptor. Specific antibodies to peptide sequences 221-234 and 259-272 and to the carboxyl-terminal peptide 402-415, all corresponding to cytoplasmic ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1991-11-01 00:00:00
abstract::The local anesthetic-like Na+ channel-blocking drug [3H]PD85639 [alpha-([4-3H]phenyl)-N-[3-(2,6-dimethyl-1-piperizinyl)-alpha-prop yl] [4-3H]benzeneacetamide] binds specifically to receptor sites on Na+ channels in intact synaptosomes and synaptosomal membranes, purified and reconstituted Na+ channels, and type IIA Na...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1993-06-01 00:00:00
abstract::A family of five cholinergic muscarinic receptor genes (m1, m2, m3, m4, and m5) has recently been identified and cloned. In order to investigate the pharmacological properties of the individual muscarinic receptors, we have transfected each of these genes into Chinese hamster ovary cells (CHO-K1) and have established ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1989-04-01 00:00:00
abstract::Metallothioneins (MTs) are cytoplasmic proteins that sequester certain divalent cations and are considered a primary cellular defense against the toxic transition metal cadmium (Cd(2+)). MT-I/II(-/-) knockout [MT(-/-)] cells are available and serve as an excellent tool to study non-MT-related mechanisms in metal toler...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.105.014241
更新日期:2006-02-01 00:00:00
abstract::High expression of the aflatoxin B1 (AFB1)-8,9-epoxide-conjugating glutathione S-transferase A3 (mGSTA3) subunit in mouse liver confers intrinsic resistance to AFB1 hepatocarcinogenesis. It is not known how the gene encoding this protein is regulated. The murine mGSTA3 gene has been identified using bioinformatics. It...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.64.5.1018
更新日期:2003-11-01 00:00:00
abstract::Cu/Zn-superoxide dismutase (SOD)-accelerated oxidation of the benzene metabolite 1,4-hydroquinone (HQ) results in the enhanced formation of semiquinone anion radicals, electrophilic 1,4-benzoquinone (BQ), and H202. We selected bone marrow stromal cells and phiX-174 double stranded plasmid DNA as model systems to inves...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1996-03-01 00:00:00
abstract::The verapamil-like arylazide (-)-[3H]azidopamil specifically photoaffinity labeled two low molecular mass polypeptides, with apparent molecular masses of 22 and 27 kDa, in the endoplasmic reticulum of guinea pig liver, kidney, adrenal gland, and lung. It was recently shown that the 22-kDa polypeptide binds the anti-is...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1993-11-01 00:00:00
abstract::High-affinity glycine transport in neurons and glial cells is a primary means of inactivating synaptic glycine. We have synthesized a potent selective inhibitor of glycine transporter 1 (GlyT1), and characterized its activity using a quail fibroblast cell line (QT6). The glycine transporters GlyT1A, GlyT1B, GlyT1C, an...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.60.6.1414
更新日期:2001-12-01 00:00:00
abstract::The GABA type A receptor (GABA(A)R) is the major inhibitory receptor in the mammalian central nervous system and the target of numerous pharmaceuticals. The alpha-subunit of these pentameric Cys-loop neurotransmitter-gated ion channels contributes to the binding of both GABA and allosteric modulators such as the benzo...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.109.059832
更新日期:2010-07-01 00:00:00
abstract::GABAA receptors are predominantly composed of alphabetagamma and alphabetadelta isoforms in the brain. It has been proposed that alphabetagamma receptors mediate phasic inhibition, whereas alphabetadelta receptors mediate tonic inhibition. Propofol (2,6-di-isopropylphenol), a widely used anesthetic drug, exerts its ef...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.104.003426
更新日期:2004-12-01 00:00:00
abstract::The biliary excretion of several organic anions is mediated by the canalicular multispecific organic anion transporter (cMOAT), which is hereditarily defective in mutant rats such as Eisai hyperbilirubinemic rats (EHBR). In addition, using a kinetic study with isolated canalicular membrane vesicles, we recently sugges...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1998-06-01 00:00:00
abstract::Dehydroepiandrosterone (DHEA) is a peroxisome proliferating agent when administered in pharmacological dosages, but it has not been shown to function through the peroxisome proliferator-activated receptor in cell-based assays. Because members of the thyroid hormone/vitamins A and D nuclear receptor subfamily, includin...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1996-02-01 00:00:00
abstract::Endothelin (ET) receptors are present in pituitary cells and stimulate hormone release through the phosphoinositide/Ca2+ signaling system. In pituitary cell suspensions, ET caused [Ca2+]i elevations of much higher amplitudes than those induced by other vasoactive hormones, including angiotensin II, vasopressin, and no...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1991-06-01 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
pub_type: 杂志文章
doi:10.1124/mol.104.005447
更新日期:2005-04-01 00:00:00
abstract::Metabolism of the pulmonary toxin, 4-ipomeanol, in microsomal preparations from rabbit liver and lung and in purified cytochrome P-450-dependent monooxygenase systems was investigated. The rate of formation of reactive electrophilic products from 4-ipomeanol was estimated by measuring covalent binding to protein or gl...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1982-11-01 00:00:00