Abstract:
:A simple method for solubilization and reconstitution of the A1 adenosine receptor from bovine brain is presented. Solubilization with CHAPS-phosphatidylcholine (CHAPS/PC) mixture did not alter the binding properties of the A1 adenosine receptor antagonist [3H]-DPCPX. The solubilized receptors were chromatographed on hydroxyapatite or DEAE-cellulose to remove native membrane lipids and part of non-receptor proteins. Elution of the receptor fractions was obtained from DEAE-cellulose column with a linear gradient of KCl (0-0.4 M). The fractions corresponding to the peak of [3H]-DPCPX binding activity were then reconstituted in phosphatidylcholine by dialysis. The reconstituted receptor retained all the binding characteristics and the same rank order of competition potency (R-PIA greater than S-PIA greater than NECA) as the native receptor, although its thermal stability was remarkably reduced. The binding of [3H]-DPCPX to A1 adenosine receptors was increased by GTP, probably as result of interactions with coeluted G-proteins.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Ragazzi E,Shryock J,Palczewski Kdoi
10.1016/1043-6618(91)90060-bsubject
Has Abstractpub_date
1991-07-01 00:00:00pages
15-23issue
1eissn
1043-6618issn
1096-1186pii
1043-6618(91)90060-Bjournal_volume
24pub_type
杂志文章abstract::Tachykinins are important in the development of pulmonary inflammation in mice but the tachykinin receptor subtype mediating this response has not been defined. To elucidate the role of tachykinin NK3-receptors on allergen-induced pulmonary inflammation, studies were performed on ovalbumin (OVA) sensitized and challen...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2004.07.002
更新日期:2004-12-01 00:00:00
abstract::Implantable cardioverter-defibrillators (ICDs) have revolutionized the primary and secondary prevention of patients with ventricular arrhythmias. However, the adverse effects of appropriate or inappropriate shocks may require the adjunctive use of anti-arrhythmic drugs (AADs). Beta blockers are the cornerstone of phar...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.03.020
更新日期:2019-05-01 00:00:00
abstract::Postnatal bone marrow contains a subtype of unique progenitor cells that have the capacity to differentiate into functional endothelial cells. Hence, these cells have been termed endothelial progenitor cells (EPCs). In general, circulating EPCs were characterized by the expression of CD133, CD34 and the vascular endot...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2008.07.008
更新日期:2008-08-01 00:00:00
abstract::In 1996, Dr. Costa was invited by Prof. Boris Astrachan, Chairman of the Department of Psychiatry at the University of Illinois at Chicago, to direct the research of the "Psychiatric Institute, Department of Psychiatry, School of Medicine, at the University of Illinois at Chicago." He was asked to develop a seminal re...
journal_title:Pharmacological research
pub_type: 历史文章,杂志文章,评审
doi:10.1016/j.phrs.2011.05.026
更新日期:2011-10-01 00:00:00
abstract::As Traditional Chinese Medicine (TCM) transcends its cultural boundaries and becomes widely used in many countries around the world, one of the major risks to the growing use of TCM internationally is the damage caused to its reputation and to community safety when TCM practitioners are not adequately trained. Ensurin...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105217
更新日期:2020-11-01 00:00:00
abstract::The aminosteroid derivative RM-133 is an effective anticancer molecule for which proof of concept has been achieved in several mouse xenograph models (HL-60, MCF-7, PANC-1 and OVCAR-3). To promote this new family of molecules toward a clinical phase 1 trial, the mechanism of action governing the anticancer properties ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2017.12.024
更新日期:2018-02-01 00:00:00
abstract::Leishmaniases are severe vector-borne diseases affecting humans and animals, caused by Leishmania protozoans. Over one billion people and millions of dogs live in endemic areas for leishmaniases and are at risk of infection. Immune polarization plays a major role in determining the outcome of Leishmania infections: ho...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105288
更新日期:2020-11-01 00:00:00
abstract::TMEM16A plays critical roles in physiological process and may serve as drug targets for diverse diseases. Recently, TMEM16A has started to be regarded as potential primary lung adenocarcinoma targets. Here, we identified that arctigenin, a natural compound, is a novel TMEM16A inhibitor, and it can suppress lung adenoc...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.104721
更新日期:2020-05-01 00:00:00
abstract::We studied here the effect of a wide range of adenosine concentration and time of preincubation, on the histamine release induced in the guinea pig mast cells by different stimulus. Adenosine (10(-5)-10(-3)m) potentiated the histamine release induced by antigen in the guinea pig heart (isolated and dispersed tissue) a...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0589
更新日期:2000-03-01 00:00:00
abstract::The Janus kinase (JAK) family of non-receptor protein-tyrosine kinases consists of JAK1, JAK2, JAK3, and TYK2 (tyrosine kinase-2). Each of these proteins contains a JAK homology pseudokinase (JH2) domain that regulates the adjacent protein kinase domain (JH1). JAK1/2 and TYK2 are ubiquitously expressed whereas JAK3 is...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2016.07.038
更新日期:2016-09-01 00:00:00
abstract::Vaccinations have been used as an essential tool in the fight against infectious diseases, and succeeded in improving public health. However, adverse effects, including autoimmune conditions may occur following vaccinations (autoimmune/inflammatory syndrome induced by adjuvants--ASIA syndrome). It has been postulated ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2014.08.002
更新日期:2015-02-01 00:00:00
abstract::The interaction of mianserin with ethanol in central nervous system (CNS) was investigated. Mianserin was administered at a single dose of 5 or 20 mgkg(-1) i.p. or as daily injections in a dose of 2.5 mgkg(-1) given for 14 days. The influence of mianserin on acute ethanol toxicity (LD(50)), on ED(50) of ethanol in rot...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(02)00031-2
更新日期:2002-07-01 00:00:00
abstract::Extrasynaptically located γ-aminobutyric acid (GABA) receptors type A are often characterized by the presence of a δ subunit in the receptor complex. δ-Containing receptors respond to low ambient concentrations of GABA, or respond to spillover of GABA from the synapse, and give rise to tonic inhibitory currents. In ce...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.05.014
更新日期:2016-09-01 00:00:00
abstract::In the present study, hyperglycaemia was induced by intraperitoneal injection of streptozotocin (65 mg/kg). Treatment with glibenclamide (GB) in a dose of 0.45 or 0.9 mg/kg significantly decreased plasma glucose level in a dose-related manner. Administration of nadolol (ND) in a dose of 5 or 10 mg/kg did not affect pl...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1996.0057
更新日期:1996-07-01 00:00:00
abstract::Some macrolide antibiotics have been shown to produce significant drug-drug interactions through the inhibition of cytochrome P450 (CYP) enzymes. In renal transplant patients these interactions pose potentially serious problems for the safe administration of cyclosporine A (CSA), a substrate of CYP3A4. The effects of ...
journal_title:Pharmacological research
pub_type: 临床试验,杂志文章
doi:10.1016/s1043-6618(03)00018-5
更新日期:2003-06-01 00:00:00
abstract::Several studies on disease and treatment effects on neurohormones have been conducted with small numbers of patients, using one blood sample as representative of their states. The aim of this study was to assess the within-patient variability of plasma concentrations of several hormones and cytokines of recent interes...
journal_title:Pharmacological research
pub_type: 临床试验,杂志文章
doi:10.1006/phrs.1998.0288
更新日期:1998-03-01 00:00:00
abstract::We previously demonstrated that the typical mitochondrial uncoupler carbonyl cyanide m-chlorophenylhydrazone (CCCP) inhibited artery constriction, but CCCP was used only as a pharmacological tool. Niclosamide is an anthelmintic drug approved by FDA. Niclosamide ethanolamine (NEN) is a salt form of niclosamide and has ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.11.008
更新日期:2017-01-01 00:00:00
abstract::Because many Ca2+ channel blocking agents are known to cause adverse systemic effects, in this study we tested the haemodynamic side effects of nimodipine with and without a mild hypoxic-ischaemic (HI) insult in a newborn piglet model. Fifteen min after completing a brief period of asphyxia we gave i.v. nimodipine as ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1996.0002
更新日期:1996-01-01 00:00:00
abstract::Hypercalcemia and hypercalciuria observed both in humans and in animals who were on long-term theophylline therapy, prompted us to investigate whether oral theophylline treatment at optimal doses causes any adverse side effects on bone metabolism in mild asthmatics. Therefore, serum osteocalcin (BGP) and total alkalin...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0486
更新日期:1999-08-01 00:00:00
abstract::Osteoporosis caused by aging and menopause had become an emerging threat to human health. The reduction of osteoblast differentiation has been considered to be an essential cause of osteoporosis. Osteoblast differentiation could be regulated by LncRNAs, and increasing evidences have proved that LncRNAs may be adopted ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105230
更新日期:2021-01-01 00:00:00
abstract::Derivatization of phenothiazine (PTZ, 1) has been a commonly used method to develop drugs with various pharmacological properties. In the present study, a series of PTZ derivatives 1-11 were investigated on the inhibition of the cloned α7 subunit of the human nicotinic acetylcholine receptor (α7-nAChR) expressed in Xe...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2012.05.008
更新日期:2012-09-01 00:00:00
abstract::A major focus of contemporary drug screening strategies is the identification of novel anticancer compounds, which often results in underutilization of resources. Current drug evaluation involves in vivo tumor (xenograft) regression as proof-of-principle for cytotoxicity (POC). However, this end-point lacks any assess...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.07.018
更新日期:2016-09-01 00:00:00
abstract::Beta-endorphin/beta-lipotropin immunoreactivity (BE/BLPH-IR) content was evaluated in the CSF of patients suffering by deafferentation pain syndromes. BE/BLPH-IR CSF concentrations of these patients were compared with those obtained in a group of patients affected by low back pain and in a control group without pain p...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(05)80120-3
更新日期:1991-02-01 00:00:00
abstract::ABT-737, ABT-263 (Navitoclax) and ABT-199 (Venetoclax) are under intensive preclinical and clinical investigation as treatments for hematologic and other malignancies. These small molecules mimic pro-death B-cell lymphoma-2 (Bcl-2) Homology 3 (BH3) domain-only proteins. They also bear a structural resemblance to certa...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.01.040
更新日期:2019-04-01 00:00:00
abstract::Receptor tyrosine kinase-like orphan receptor 1 (ROR1) is an onco-embryonic antigen presented on chronic lymphocytic leukemia (CLL), but not on normal adult tissues, which promotes CLL-cell survival. Here, ROR1 was identified as a new client of Heat Shock Protein 90 (HSP90) via a mass spectrometry-based screen for ROR...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.104512
更新日期:2020-01-01 00:00:00
abstract::Pharmacokinetics is a relatively young branch of the life sciences, which has developed rapidly in the last 15-20 years, thanks to a series of analytical achievements that have allowed drug concentrations to be measured in biological matrices with highly selective and sensitive methods. Most old drugs and all new drug...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1006/phrs.1997.0254
更新日期:1997-12-01 00:00:00
abstract::N-acetyl penicillamine (NAP), a derivative of penicillamine and copper chelator has been employed as a potential protector of host stress organ injury during Plasmodium berghei infection in mice. Intramuscular injection of NAP (60 mg kg-1 body wt for 10 days) to P. berghei mice was able to restrict the hepato- and spl...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1997.0233
更新日期:1997-10-01 00:00:00
abstract::Baroreflex plays a crucial role in regulation of arterial blood pressure (BP). Recently, Piezo1 and Piezo2, the mechanically-activated (MA) ion channels, have been identified as baroreceptors. However, the underlying molecular mechanism for regulating these baroreceptors in hypertension remains unknown. In this study,...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105391
更新日期:2020-12-19 00:00:00
abstract::Since the regenerative capacity of the adult mammalian heart is limited, cardiac injury leads to the formation of scar tissue and thereby increases the risk of developing compensatory heart failure. Stem cell therapy is a promising therapeutic approach but is facing problems with engraftment and clinical feasibility. ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2017.07.020
更新日期:2018-01-01 00:00:00
abstract::Prader-Willi syndrome (PWS), the leading genetic cause of obesity, is characterized by a striking hyperphagic behavior that can lead to obesity, type-2 diabetes, cardiovascular disease and death. The molecular mechanism underlying impaired satiety in PWS is unknown. Oleoylethanolamide (OEA) is a lipid mediator involve...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.12.024
更新日期:2017-03-01 00:00:00