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Yveline Henchoz et al.
Journal of medicinal chemistry, 51(3), 396-399 (2008-01-15)
Accurate determinations of lipophilicity indices benefit from recent advances in chromatographic sciences such as the launch of ultraperformance liquid chromatography (UPLC). The fast strategy presented here emerges as a powerful method suitable for high-throughput log P measurements of therapeutic compounds
Jillian G Baker et al.
Journal of medicinal chemistry, 54(19), 6874-6887 (2011-08-30)
The growing practice of exploiting noninvasive fluorescence-based techniques to study G protein-coupled receptor pharmacology at the single cell and single molecule level demands the availability of high-quality fluorescent ligands. To this end, this study evaluated a new series of red-emitting
M J Millan et al.
Neuropharmacology, 38(6), 909-912 (1999-08-28)
(-)-Pindolol (2.5-20.0 mg/kg, s.c.) markedly increased extracellular levels of dopamine (DA) and noradrenaline (NA) in single dialysate samples of the frontal cortex (FCX) of freely-moving rats. This action was specific inasmuch as serotonin (5-HT) levels were not significantly modified. In
J S Olver et al.
The Australian and New Zealand journal of psychiatry, 34(1), 71-79 (2001-02-24)
To critically review the literature on clinical trials in which pindolol, a 5HT1A receptor antagonist, has been used to augment the effects of antidepressants in patients with depression and to examine the pharmacodynamics and pharmacokinetics that may underlie such augmentations.
Antihypertensive effects of pindolol.
L M Gonasun
American heart journal, 104(2 Pt 2), 374-387 (1982-08-01)
Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(12), 2302-2308 (2010-09-17)
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predictive in vivo, in vitro, and in silico models to identify compounds
Sónia A Silva et al.
Pharmacology, 89(1-2), 29-36 (2012-02-04)
The in vitro contractile response of the human uterine artery to sumatriptan was compared to that of human cerebral blood vessels. Artery rings were prepared for isometric contraction. Tachyphylaxis to the triptan-induced vascular contraction was observed in the uterine artery
Pär Matsson et al.
Journal of medicinal chemistry, 48(2), 604-613 (2005-01-22)
The influence of different drug transport routes in intestinal drug permeability screening assays was studied. Three experimental models were compared: the small-intestine-like 2/4/A1 cell model, which has a leaky paracellular pathway, the Caco-2 cell model, which has a tighter paracellular
The Medical journal of Australia, 150(11), 646-646 (1989-06-05)
In an open study that was conducted in general practice, 22 patients with previously-untreated mild hypertension received an average daily dose of 11.7 mg of pindolol over a 50-week study period. The total cholesterol, high-density lipoprotein fraction and plasma triglyceride
M T Ubeda-Torres et al.
Journal of chromatography. A, 1380, 96-103 (2015-01-17)
In reversed-phase liquid chromatography in the absence of additives, cationic basic compounds give rise to broad and asymmetrical peaks as a result of ionic interactions with residual free silanols on silica-based stationary phases. Ionic liquids (ILs), added to the mobile
Andrew A Udy et al.
Critical care (London, England), 18(6), 657-657 (2014-11-30)
The aim of this study was to explore changes in glomerular filtration (GFR) and renal tubular function in critically ill patients at risk of augmented renal clearance (ARC), using exogenous marker compounds. This prospective, observational pharmacokinetic (PK) study was performed
Klaus Martiny et al.
Nordic journal of psychiatry, 66(3), 147-154 (2012-03-31)
Pindolol has been widely investigated as an augmenter of antidepressant drug response. Results have been inconsistent. In this study, we used pindolol together with venlafaxine because of its ability to achieve a rapid onset of serotonin transporter blockade. The object
T Puzantian et al.
Pharmacotherapy, 19(2), 205-212 (1999-02-25)
Although in the last few years new antidepressants have become available in the United States, responses in many patients differ, from none, to partial, to delayed therapeutic response to the agents. If the antidepressant properties of these drugs could be
Takeaki Saijo et al.
PloS one, 7(8), e42589-e42589 (2012-08-11)
A novel investigational antidepressant with high affinity for the serotonin transporter and the serotonin 1A (5-HT(1A)) receptor, called Wf-516 (structural formula: (2S)-1-[4-(3,4-dichlorophenyl)piperidin-1-yl]-3-[2-(5-methyl-1,3,4-oxadiazol-2-yl)benzo[b]furan-4-yloxy]propan-2-ol monohydrochloride), has been found to exert a rapid therapeutic effect, although the mechanistic basis for this potential advantage
P Blier et al.
The Journal of clinical psychiatry, 59 Suppl 5, 16-23 (1998-06-27)
Serotonin (5-HT) selective reuptake inhibitors (SSRIs) and monoamine oxidase inhibitors are thought to have a delayed onset of antidepressant action attributable in part to the decrease in firing activity of 5-HT neurons they produce upon treatment initiation. As cell body
Haruka Okamoto et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 1051, 33-40 (2017-03-13)
Cationic amphiphilic drugs (CADs) can induce the hyperaccumulation of phospholipids in cells and tissues. This side effect, which is known as drug-induced phospholipidosis, is sometimes problematic in the development and clinical use of CADs. It is known that CADs generally
Alfredo Del Giaccio et al.
Investigacion clinica, 51(1), 77-86 (2010-09-08)
Calcium channel blockers, beta adrenergic receptor blockers and Na/K ATPase inhibitors are widely used drugs, mainly for cardiovascular diseases. Their pharmacological targets are not restricted to the cardivascular tissue, nociceptive system structures also express similar targets, which strongly suggests a
Ivan Skelin et al.
Neurochemistry international, 61(8), 1417-1423 (2012-10-23)
Antidepressant treatments, including those that increase serotonin (5-HT) neurotransmission, require several weeks or months until the onset of the therapeutic effect in depressed patients. The negative feedback on 5-HT transmission exhibited by the 5-HT(1A) and 5-HT(1B) autoreceptors has been postulated
Mohammed Amine Abdelkrim et al.
Canadian journal of physiology and pharmacology, 90(4), 407-414 (2012-03-28)
Circulating autoantibodies directed against the 2nd extracellular loop (EL-2) of β(1)-adrenoceptors (β(1)-AABs) have been detected in the serum of patients with various cardiovascular pathologies. β(1)-AABs induce agonistic, positive inotropic effects via β(1)-adrenoceptors (β(1)ARs). In the mammalian heart, β(1)-AR can exist
Haiyan Li et al.
European journal of medicinal chemistry, 44(4), 1600-1606 (2008-09-05)
The first-principle, quantitative structure-hepatic clearance relationship for 50 drugs was constructed based on selected molecular descriptors calculated by TSAR software. The R(2) of the predicted and observed hepatic clearance for the training set (n=36) and test set (n=13) were 0.85
A M Agius et al.
Rhinology, 51(2), 143-153 (2013-05-15)
Patients often present to otolaryngologists with chronic facial pain, presumed to be of sinus origin despite normal nasal endoscopy and sinus CT. This pain has increasingly been recognized as being of neurological origin with one of the commonest underlying causes
Weifeng Liu et al.
Chirality, 32(3), 370-377 (2020-01-14)
We present a new concept of synthesis for preparation of molecularly imprinted polymers using a functionalized initiator to replace the traditional functional monomer. Using propranolol as a model template, a carboxyl-functionalized radical initiator was demonstrated to lead to high-selectivity polymer
Naomi L Kruhlak et al.
Toxicology mechanisms and methods, 18(2-3), 217-227 (2008-01-01)
ABSTRACT Drug-induced phospholipidosis (PL) is a condition characterized by the accumulation of phospholipids and drug in lysosomes, and is found in a variety of tissue types. PL is frequently manifested in preclinical studies and may delay or prevent the development
A Guerra et al.
European journal of medicinal chemistry, 45(3), 930-940 (2009-12-22)
A neural model based on a numerical molecular representation using CODES program to predict oral absorption of any structure is described. This model predicts both high and low-absorbed compounds with a global accuracy level of 74%. CODES/ANN methodology shows promising
Maja Mandić et al.
PloS one, 9(11), e112664-e112664 (2014-11-18)
Glucose metabolism is under the cooperative regulation of both insulin receptor (IR) and β(2)-adrenergic receptor (β(2)AR), which represent the receptor tyrosine kinases (RTKs) and seven transmembrane receptors (7TMRs), respectively. Studies demonstrating cross-talk between these two receptors and their endogenous coexpression
Jennifer L Miller et al.
Journal of molecular biology, 413(3), 628-638 (2011-09-13)
Conformational thermostabilisation of G-protein-coupled receptors is a successful strategy for their structure determination. The thermostable mutants tolerate short-chain detergents, such as octylglucoside and nonylglucoside, which are ideal for crystallography, and in addition, the receptors are preferentially in a single conformational
David Buttar et al.
Bioorganic & medicinal chemistry, 18(21), 7486-7496 (2010-09-28)
The displacement of probes that bind selectively to subdomains IIA or IIIA on human serum albumin (HSA) by competing compounds has been followed using fluorescence spectroscopy, and has therefore been used to assign a primary binding site for these compounds
Andiara E Freitas et al.
Molecular neurobiology, 51(3), 1504-1519 (2014-08-03)
Hyperactivation of the hypothalamic-pituitary-adrenal axis is a common finding in major depression; this may lead to increased levels of cortisol, which are known to cause oxidative stress imbalance and apoptotic neuronal cell death, particularly in the hippocampus, a key region
Elisenda Fornells et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 117, 227-235 (2018-02-27)
The development of methods to increase the bioavailability of drugs is of great interest, especially for those which are poorly soluble or permeable. One of the strategies to enhance the solubility (which in turn has the potential of increase bioavailability)
C A Fornal et al.
The Journal of pharmacology and experimental therapeutics, 291(1), 229-238 (1999-09-22)
Clinical studies have shown that pindolol can enhance the effects of antidepressant drugs, presumably by acting as an antagonist at somatodendritic 5-hydroxytryptamine (5-HT)(1A) autoreceptors, which regulate the firing rate of central serotonergic neurons. The current study characterized the action of
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