Abstract：
:Angiotensin II (AII) stimulates rapid increases in cytosolic Ca2+ concentrations in Xenopus laevis oocytes after binding to specific receptors located in the surrounding follicular cells. In follicular oocytes, the peptide AII receptor antagonists saralasin (IC50 = 25 nM) and CGP 42112A (IC50 = 400 nM) were orders of magnitude more potent than the non-peptide antagonists DuP 753 and PD-123177 (IC50 greater than 10 microM) as inhibitors of AII-induced Ca2+ mobilization. The relative potencies of the AII antagonists at the Xenopus AII receptor were completely different from their activities at the two known mammalian AII receptor subtypes. These results indicate that the ligand-binding domain of the amphibian AII receptor has a unique conformation that distinguishes with high specificity between peptide and non-peptide AII antagonists. The amphibian AII receptor is pharmacologically distinct from the AT1 receptor subtype, which mediates phosphoinositide hydrolysis and Ca2+ mobilization in mammalian adrenal cells.
journal_name
Mol Pharmacoljournal_title
Molecular pharmacologyauthors
Ji H,Sandberg K,Catt KJsubject
Has Abstractpub_date
1991-02-01 00:00:00pages
120-3issue
2eissn
0026-895Xissn
1521-0111journal_volume
39pub_type
杂志文章abstract：:A polyamine component of Agelenopsis aperta spider venom designated FTX is reported to be a selective antagonist of P-type calcium channels in the mammalian brain. Consequently, this component has frequently been used as a pharmacological tool to determine the presence, distribution, and function of P-type channels in...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1996-10-01 00:00:00
abstract：:Large conductance, Ca(2+)-activated K+ channels are believed to underlie interburst intervals and, thus, contribute to the control of hormone release from neurohypophysial terminals. Because ethanol inhibits the release of vasopressin and oxytocin, we studied its effects on large conductance, Ca(2+)-activated K+ chann...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1996-01-01 00:00:00
abstract：:The glucagon-like peptide-1 receptor (GLP-1R) is a key physiological regulator of insulin secretion and a major therapeutic target for the treatment of type II diabetes. However, regulation of GLP-1R function is complex with multiple endogenous peptides that interact with the receptor, including full-length (1-37) and...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.111.072884
更新日期：2011-09-01 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
pub_type： 杂志文章
doi：10.1124/mol.104.007500
更新日期：2005-03-01 00:00:00
abstract：:Cytosolic liver acetyl-CoA:arylamine N-acetyltransferase (EC 2.3.1.5) from homozygous rapid acetylator rabbits (strain III/J) was purified to homogeneity as judged by gel filtration sodium dodecyl sulfate-polyacrylamide disc gel electrophoresis and isoelectrofocusing. The isoelectric point was estimated to be 5.2. The...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1987-04-01 00:00:00
abstract：:Tetradecyl 2,3-dihydroxybenzoate (ABG-001) is a lead compound derived from neuritogenic gentisides. In the present study, we investigated the mechanism by which ABG-001 induces neurite outgrowth in a rat adrenal pheochromocytoma cell line (PC12). Inhibitors of insulin-like growth factor 1 (IGF-1) receptor, phosphatidy...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.115.097758
更新日期：2015-08-01 00:00:00
abstract：:Bupropion is an atypical antidepressant that also has usefulness as a smoking-cessation aid. Because hydroxybupropion, a major metabolite of bupropion, is believed to contribute to its antidepressant activity, this metabolite may also contribute to the smoking-cessation properties of bupropion. This study investigated...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.104.001313
更新日期：2004-09-01 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：:Guanidine and its alkyl analogs stimulate the neuromuscular junction presynaptically by inhibiting voltage-gated potassium (Kv) channels, leading to enhanced release of acetylcholine in the synaptic cleft. This stimulatory effect of guanidine underlies its use in the therapy for the neuromuscular diseases myasthenic s...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.111.074989
更新日期：2011-12-01 00:00:00
abstract：:Mitochondria contain specific Ca2+ antagonist binding sites that are associated with an inner mitochondrial membrane anion channel. These mitochondrial Ca2+ antagonist receptors can be solubilized with digitonin and partially purified [as assessed by postreversible (+/-)-[3H]nitrendipine binding] using ion exchange ch...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1992-12-01 00:00:00
abstract：:The intermediate-conductance Ca2+-activated K+ channel (KCa3.1) constitutes an attractive pharmacological target for immunosuppression, fibroproliferative disorders, atherosclerosis, and stroke. However, there currently is no available crystal structure of this medically relevant channel that could be used for structu...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.116.108068
更新日期：2017-04-01 00:00:00
abstract：:Iron-loading diseases remain an important problem because of the toxicity of iron-catalyzed redox reactions. Iron loading occurs in the mitochondria of Friedreich's ataxia (FA) patients and may play a role in its pathogenesis. This suggests that iron chelation therapy could be useful. We developed previously the lipop...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.108.046847
更新日期：2008-07-01 00:00:00
abstract：:Recent clinical studies reveal that selective agonists of group II metabotropic glutamate (mGlu) receptors have robust efficacy in treating positive and negative symptoms in patients with schizophrenia. Group II mGlu receptor agonists also modulate the in vivo activity of psychotomimetic drugs and reduce the ability o...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.107.035170
更新日期：2007-08-01 00:00:00
abstract：:Endothelin-1 (ET) and ATP mobilize Ca2+ in rat C6 glioma cells by stimulating phosphoinositide turnover. Both agents also inhibit adenylyl cyclase (AC) activity in C6 glioma cells. The goal of this study was to characterize the molecular mechanisms responsible for the inhibition of AC activity. The administration of e...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1993-07-01 00:00:00
abstract：:A series of aminotriarylmethane dyes were examined for binding to the nicotinic acetylcholine receptor (AChR) from Torpedo californica. Several compounds were found to bind to the noncompetitive antagonist site of the AChR as demonstrated by inhibition of [3H]phencyclidine binding; apparent KD values ranged from 50 nM...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.55.1.159
更新日期：1999-01-01 00:00:00
abstract：:Regulator of G protein signaling (RGS) proteins are negative modulators of G protein signaling that have emerged as promising drug targets to improve specificity and reduce side effects of G protein-coupled receptor-related therapies. Several small molecule RGS protein inhibitors have been identified; however, enhanci...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/molpharm.120.000061
更新日期：2020-12-01 00:00:00
abstract：:Bryostatin 1 and phorbol-12-myristate-13-acetate (PMA) are both potent activators of protein kinase C (PKC), although in primary mouse keratinocytes bryostatin 1 does not induce differentiation and blocks PMA-induced differentiation. We report here that in primary mouse keratinocytes PMA caused translocation of PKC-ep...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1994-11-01 00:00:00
abstract：:Platelet-activating factor (PAF) receptor-coupled activation of phosphoinositide-specific phospholipase C (PLC) was studied in platelets that were made refractory, by short-term pretreatments, to either PAF or thrombin. Generation of [3H]inositol triphosphate ( [3H]IP3) was monitored specifically for this purpose. [3H...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1988-01-01 00:00:00
abstract：:The present study characterizes the methanethiosulfonate (MTS) inhibition profiles of 26 consecutive cysteine-substituted mutants comprising transmembrane (TM) helix 6 of the human apical Na(+)-dependent bile acid transporter (SLC10A2). TM6 is linked exofacially to TM7 via extracellular loop 3. TM7 was identified prev...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.107.041640
更新日期：2008-02-01 00:00:00
abstract：:Acute desensitization of mu opioid receptors is thought to be an initial step in the development of tolerance to opioids. Given the resistance of the respiratory system to develop tolerance, desensitization of neurons in the Kölliker-Fuse (KF), a key area in the respiratory circuit, was examined. The activation of G p...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.117.109603
更新日期：2018-01-01 00:00:00
abstract：:Recent studies from our laboratory have provided evidence that multiple states of the phencyclidine (PCP) receptor exist. In addition, several compounds such as PCP and the novel anticonvulsant MK-801 were found to inhibit binding more potently in the presence of Mg2+ and L-glutamate (L-GLU) than when these agents wer...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1989-07-01 00:00:00
abstract：:Specific toxic and biochemical responses elicited by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in human thymic epithelial (TE) cells in culture are mediated by the TCDD receptor protein. Characterization of the physicochemical properties of the TCDD receptor in cytosol fractions from cultured human TE cells indicates...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1989-05-01 00:00:00
abstract：:Excitotoxin-induced destruction of striatal neurons, proposed as a model of Huntington's disease, involves a process having the biochemical stigmata of apoptosis. Recent studies suggested that transcription factor nuclear factor (NF)-kappa B may be involved in excitotoxicity. To further analyze the contribution of NF ...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.53.1.33
更新日期：1998-01-01 00:00:00
abstract：:Two newly identified, overlapping (1 bp) glucocorticoid response elements (GREs) at -759 and -773 bp in the promoter of the rat phenylethanolamine N-methyltransferase (PNMT; EC 2.1.1.28) gene are primarily responsible for its glucocorticoid sensitivity, rather than the originally identified -533-bp GRE. A dose-depende...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.61.6.1385
更新日期：2002-06-01 00:00:00
abstract：:Eukaryotic cells assemble stress granules (SGs) when translation initiation is inhibited. Different cell signaling pathways regulate SG production. Particularly relevant to this process is 5'-AMP-activated protein kinase (AMPK), which functions as a stress sensor and is transiently activated by adverse physiologic con...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.116.105494
更新日期：2016-10-01 00:00:00
abstract：:S-Adenosylmethionine (SAMe) and its metabolite 5'-methylthioadenosine (MTA) inhibit mitogen-induced proliferative response in liver and colon cancer cells. SAMe and MTA are also proapoptotic in liver cancer cells by selectively inducing Bcl-x(S) expression. The aims of this work were to assess whether these agents are...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.108.054411
更新日期：2009-07-01 00:00:00
abstract：:Adaptive changes in gene expression are thought to contribute to dependence, addiction and other behavioral responses to chronic ethanol abuse. DNA array studies provide a nonbiased detection of networks of gene expression changes, allowing insight into functional consequences and mechanisms of such molecular response...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.58.6.1593
更新日期：2000-12-01 00:00:00
abstract：:Ro 11-2465 is a cyanide derivative of imipramine. In cerebral cortex homogenates, [3H] Ro 11-2465 displays a binding profile similar to that of [3H]imipramine. Agents compete with binding of [3H]Ro 11-2465 in an order of potency similar to their ability to block serotonin uptake, and raphe lesions greatly decrease the...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1983-05-01 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
pub_type： 杂志文章
doi：10.1124/mol.105.014514
更新日期：2005-12-01 00:00:00
abstract：:Inflammation contributes to pain hypersensitivity through multiple mechanisms. Among the most well characterized of these is the sensitization of primary nociceptive neurons by arachidonic acid metabolites such as prostaglandins through G protein-coupled receptors. However, in light of the recent discovery that the no...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.107.040832
更新日期：2008-02-01 00:00:00
