Endothelins and sarafotoxins: physiological regulation, receptor subtypes and transmembrane signaling.


:The endothelins and sarafotoxins are two structurally related families of potent vasoactive peptides. Although the physiological functions of these peptides are not entirely clear, the endothelins are probably involved in pathophysiological conditions such as hypertension and heart failure. This review summarizes the state of the art in some areas of this intensively studied subject, including: (1) structure-function relationships of ET/SRTX, (2) ET concentrations in plasma, (3) ET/SRTX receptor subtypes and (4) signaling events mediated by the activation of ET/SRTX receptors.


Pharmacol Ther


Sokolovsky M




Has Abstract


1992-01-01 00:00:00














  • Clinical benefits and pharmacology of scutellarin: A comprehensive review.

    abstract::Stroke and myocardial infarction are among the most common causes of mortality and disability in the world. The ischemic injury underlying these illnesses is complex, involving intricate interplays among many biological functions including energy metabolism, vascular regulation, hemodynamics, oxidative stress, inflamm...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Wang L,Ma Q

    更新日期:2018-10-01 00:00:00

  • Evidence-based strategies for the characterisation of human drug and chemical glucuronidation in vitro and UDP-glucuronosyltransferase reaction phenotyping.

    abstract::Enzymes of the UDP-glucuronosyltransferase (UGT) superfamily contribute to the elimination of drugs from almost all therapeutic classes. Awareness of the importance of glucuronidation as a drug clearance mechanism along with increased knowledge of the enzymology of drug and chemical metabolism has stimulated interest ...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Miners JO,Rowland A,Novak JJ,Lapham K,Goosen TC

    更新日期:2021-02-01 00:00:00

  • 30 years of dynorphins--new insights on their functions in neuropsychiatric diseases.

    abstract::Since the first description of their opioid properties three decades ago, dynorphins have increasingly been thought to play a regulatory role in numerous functional pathways of the brain. Dynorphins are members of the opioid peptide family and preferentially bind to kappa opioid receptors. In line with their localizat...

    journal_title:Pharmacology & therapeutics

    pub_type: 历史文章,杂志文章,评审


    authors: Schwarzer C

    更新日期:2009-09-01 00:00:00

  • Metabolic polymorphisms.

    abstract::Polymorphisms have been detected in a variety of xenobiotic-metabolizing enzymes at both the phenotypic and genotypic level. In the case of four enzymes, the cytochrome P450 CYP2D6, glutathione S-transferase mu, N-acetyltransferase 2 and serum cholinesterase, the majority of mutations which give rise to a defective ph...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Daly AK,Cholerton S,Gregory W,Idle JR

    更新日期:1993-02-01 00:00:00

  • New hope for cancer treatment: exploring the distinction between normal adult stem cells and cancer stem cells.

    abstract::For decades, intensive studies have attempted to identify the mechanisms underlying malignant tumor growth. Despite significant progress, most therapeutic approaches fail to eliminate all tumor cells. The remaining tumor cells often result in recurrence and metastasis. Recently, the idea of a cancer stem cell was prop...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Zhao RC,Zhu YS,Shi Y

    更新日期:2008-07-01 00:00:00

  • O-GlcNAc and the cardiovascular system.

    abstract::The cardiovascular system is capable of robust changes in response to physiologic and pathologic stimuli through intricate signaling mechanisms. The area of metabolism has witnessed a veritable renaissance in the cardiovascular system. In particular, the post-translational β-O-linkage of N-acetylglucosamine (O-GlcNAc)...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Dassanayaka S,Jones SP

    更新日期:2014-04-01 00:00:00

  • Vascular Disrupting Agents in cancer treatment: Cardiovascular toxicity and implications for co-administration with other cancer chemotherapeutics.

    abstract::Destruction of the established tumour vasculature by a class of compound termed Vascular Disrupting Agents (VDAs) is showing considerable promise as a viable approach for the management of solid tumours. VDAs induce a rapid shutdown and collapse of tumour blood vessels, leading to ischaemia and consequent necrosis of ...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Gill JH,Rockley KL,De Santis C,Mohamed AK

    更新日期:2019-10-01 00:00:00

  • Neuropharmacology of 5-hydroxytryptamine1B/D receptor ligands.

    abstract::In spite of a lack of compounds acting selectively at the 5-hydroxytryptamine (5-HT)1B and 5-HT1D receptor subtypes, by cross-relating the available data, this review attempts to tentatively assign behavioural and other in vivo correlates of these receptor subtypes. In addition, a summary of data from microdialysis st...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Chopin P,Moret C,Briley M

    更新日期:1994-01-01 00:00:00

  • Preventing asthma exacerbations: what are the targets?

    abstract::Exacerbations of asthma are the main cause of asthma morbidity. They induce acute respiratory failure, and sometimes death. Two immunological signals acting in synergy are necessary for inducing asthma exacerbations. The first, triggered by allergens and/or unknown agents leads to the chronic Th2 inflammation characte...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Botturi K,Langelot M,Lair D,Pipet A,Pain M,Chesne J,Hassoun D,Lacoeuille Y,Cavaillès A,Magnan A

    更新日期:2011-07-01 00:00:00

  • Receptor oligomerization: a pivotal mechanism for regulating chemokine function.

    abstract::Since the first reports on chemokine function, much information has been generated on the implications of these molecules in numerous physiological and pathological processes, as well as on the signaling events activated through their binding to receptors. Despite these extensive studies, no chemokine-related drugs ha...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Muñoz LM,Lucas P,Holgado BL,Barroso R,Vega B,Rodríguez-Frade JM,Mellado M

    更新日期:2011-09-01 00:00:00

  • Dietary manipulation of platelet function.

    abstract::Activated platelets contribute to plaque formation within blood vessels in the early and late stages of atherogenesis, and therefore they have been proposed as risk factor for cardiovascular disease. Anti-platelet drugs, such as aspirin, are now the most prescribed pharmacological treatment in Europe. Certain dietary ...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Bachmair EM,Ostertag LM,Zhang X,de Roos B

    更新日期:2014-11-01 00:00:00

  • A critical evaluation of in vitro cell culture models for high-throughput drug screening and toxicity.

    abstract::Drug candidate and toxicity screening processes currently rely on results from early-stage in vitro cell-based assays expected to faithfully represent essential aspects of in vivo pharmacology and toxicology. Several in vitro designs are optimized for high throughput to benefit screening efficiencies, allowing the ent...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Astashkina A,Mann B,Grainger DW

    更新日期:2012-04-01 00:00:00

  • A novel paradigm for therapeutic basis of advanced heart failure--assessment by gene therapy.

    abstract::The precise mechanism(s) of the progression of advanced heart failure (HF) should be determined to establish strategies for its treatment or prevention. Based on pathological, molecular, and physiological findings in 3 animal models and human cases, we propose a novel scheme that a vicious cycle formed by increased sa...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Kawada T,Masui F,Kumagai H,Koshimizu M,Nakazawa M,Toyo-Oka T

    更新日期:2005-07-01 00:00:00

  • Studies on anti-human immunodeficiency virus oligonucleotides that have alternating methylphosphonate/phosphodiester linkages.

    abstract::Preliminary investigations of the physical properties of oligonucleotide analogs that contain alternating methylphosphonate/phosphodiester linkages are described. An alternating oligo-2'-O-methylribonucleoside methylphosphonate, oligomer 1676, whose sequence is complementary to the upper hairpin region of human immuno...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Miller PS,Cassidy RA,Hamma T,Kondo NS

    更新日期:2000-03-01 00:00:00

  • GABAA receptor pharmacology.

    abstract::gamma-Aminobutyric acid (GABA)A receptors for the inhibitory neurotransmitter GABA are likely to be found on most, if not all, neurons in the brain and spinal cord. They appear to be the most complicated of the superfamily of ligand-gated ion channels in terms of the large number of receptor subtypes and also the vari...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Johnston GA

    更新日期:1996-01-01 00:00:00

  • Dopamine D2 autoreceptor interactome: Targeting the receptor complex as a strategy for treatment of substance use disorder.

    abstract::Dopamine D2 autoreceptors (D2ARs), located in somatodendritic and axon terminal compartments of dopamine (DA) neurons, function to provide a negative feedback regulatory control on DA neuron firing, DA synthesis, reuptake and release. Dysregulation of D2AR-mediated DA signaling is implicated in vulnerability to substa...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Chen R,Ferris MJ,Wang S

    更新日期:2020-09-01 00:00:00

  • Regulations of opioid dependence by opioid receptor types.

    abstract::Three major types of opioid receptors, designated mu, delta, and kappa, are widely expressed in the CNS. Development of selective receptor ligands and recent cloning of each receptor have contributed greatly to our increasing knowledge of the neuropharmacological profile of each opioid receptor type. It is of interest...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Narita M,Funada M,Suzuki T

    更新日期:2001-01-01 00:00:00

  • Purinergic P2Y receptors: Molecular diversity and implications for treatment of cardiovascular diseases.

    abstract::Purinergic signaling, mediated mainly by G protein-coupled P2Y receptors (P2YRs), is now attracting attention as a new therapeutic target for preventing or treating cardiovascular diseases. Observations using mice with genetically modified P2YRs and/or treated with a pharmacological P2YR inhibitor have helped us under...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Nishimura A,Sunggip C,Oda S,Numaga-Tomita T,Tsuda M,Nishida M

    更新日期:2017-12-01 00:00:00

  • Enhancement of 5-fluorouracil's anticancer activity by dipyridamole.

    abstract::Although the interaction between FUra and DP in HCT 116 cells is fairly complex, data from other investigators indicate that in cell lines in which inhibition of TS is growth limiting at relatively low concentrations of fluoropyrimidines, DP appears to augment the cytotoxicity of FUra and FdUrd by blocking the salvage...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Grem JL,Fischer PH

    更新日期:1989-01-01 00:00:00

  • A role for 5-HT in the action of antidepressant drugs.

    abstract::Administration of antidepressant drugs to rodents appears to decrease 5-HT2 receptor function while transmission through postsynaptic 5-HT1 receptor synapses may be enhanced. Antidepressant drugs also alter 5-HT mechanisms in humans; some of these changes are congruent with effects noted in animal studies. Thus certai...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Cowen PJ

    更新日期:1990-01-01 00:00:00

  • Transcranial magnetic brain stimulation: therapeutic promises and scientific gaps.

    abstract::Since its commercial advent in 1985, transcranial magnetic stimulation (TMS), a technique for stimulating neurons in the cerebral cortex through the scalp, safely and with minimal discomfort, has captured the imaginations of scientists, clinicians and lay observers. Initially a laboratory tool for neurophysiologists s...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Wassermann EM,Zimmermann T

    更新日期:2012-01-01 00:00:00

  • Estradiol effects on hypothalamic AMPK and BAT thermogenesis: A gateway for obesity treatment?

    abstract::In addition to their prominent roles in the control of reproduction, estrogens are important modulators of energy balance, as evident in conditions of deficiency of estrogens, which are characterized by increased feeding and decreased energy expenditure, leading to obesity. AMP-activated protein kinase (AMPK) is a ubi...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: López M,Tena-Sempere M

    更新日期:2017-10-01 00:00:00

  • Acquisition of inhibitor-sensitive protein kinases through protein design.

    abstract::Protein phosphorylation is the major post-translational modification used by eukaryotic cells to control cellular signaling. Protein kinases have emerged as attractive drug targets because heightened protein kinase activity has been associated with several proliferative diseases, most notably cancer and restenosis. Un...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Bishop AC,Shokat KM

    更新日期:1999-05-01 00:00:00

  • Progranulin: a growth factor, a novel TNFR ligand and a drug target.

    abstract::Progranulin (PGRN) is abundantly expressed in epithelial cells, immune cells, neurons, and chondrocytes, and reportedly contributes to tumorigenesis. PGRN is a crucial mediator of wound healing and tissue repair. PGRN also functions as a neurotrophic factor and mutations in the PGRN gene resulting in partial loss of t...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Liu CJ,Bosch X

    更新日期:2012-01-01 00:00:00

  • The opioid system in neurologic and psychiatric disorders and in their experimental models.

    abstract::Evidence from experimental and clinical studies suggests the involvement of the endogenous opioid system in several neurologic and psychiatric disorders (Alzheimer's, Huntington's and Parkinson's diseases, drug-induced movement disorders, Gilles de la Tourette syndrome, stroke, ischemia, brain and spinal cord injury, ...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Gulya K

    更新日期:1990-01-01 00:00:00

  • Interactions between dyslipidemia and the immune system and their relevance as putative therapeutic targets in atherosclerosis.

    abstract::Cardiovascular disease (CVD) continues to be a leading cause of death worldwide with atherosclerosis being the major underlying pathology. The interplay between lipids and immune cells is believed to be a driving force in the chronic inflammation of the arterial wall during atherogenesis. Atherosclerosis is initiated ...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Lacy M,Atzler D,Liu R,de Winther M,Weber C,Lutgens E

    更新日期:2019-01-01 00:00:00

  • Multi-target strategies for the improved treatment of depressive states: Conceptual foundations and neuronal substrates, drug discovery and therapeutic application.

    abstract::Major depression is a debilitating and recurrent disorder with a substantial lifetime risk and a high social cost. Depressed patients generally display co-morbid symptoms, and depression frequently accompanies other serious disorders. Currently available drugs display limited efficacy and a pronounced delay to onset o...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Millan MJ

    更新日期:2006-05-01 00:00:00

  • Mechanisms of monooxygenase induction and inhibition.

    abstract::The mechanisms of monooxygenase induction and inhibition have been discussed from the standpoint of historic development, from the current concepts about the molecular mechanism of enzyme induction, and from the various possibilities by which inhibitors can interact with the complex cytochrome P-450 monooxygenase syst...

    journal_title:Pharmacology & therapeutics

    pub_type: 历史文章,杂志文章,评审


    authors: Netter KJ

    更新日期:1987-01-01 00:00:00

  • Lorcaserin: A review of its preclinical and clinical pharmacology and therapeutic potential.

    abstract::The selective 5-HT2C receptor agonist lorcaserin, in conjunction with lifestyle modification, was approved by the FDA in 2012 for weight management. It has been marketed in the US as Belviq® since 2013. This article provides a review of the preclinical and clinical pharmacology of lorcaserin, including its pharmacokin...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: Higgins GA,Fletcher PJ,Shanahan WR

    更新日期:2020-01-01 00:00:00

  • Emerging bronchoscopic treatments for chronic obstructive pulmonary disease.

    abstract::Chronic obstructive pulmonary disease (COPD) is a progressive lung disease characterized by pathophysiological factors including airflow limitation, hyperinflation and reduced gas exchange. Treatment consists of lifestyle changes, lung rehabilitation and pharmacological therapies such as long acting beta-2-agonists (L...

    journal_title:Pharmacology & therapeutics

    pub_type: 杂志文章,评审


    authors: van Geffen WH,Kerstjens HAM,Slebos DJ

    更新日期:2017-11-01 00:00:00