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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
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
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
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
Silvia Rocchi et al.
Journal of chromatography. A, 1381, 149-159 (2015-01-24)
A novel sub-2 μm chiral stationary phase (CSP) was prepared immobilizing vancomycin onto 1.8 μm diol hydride-based silica particles. The CSP was packed into fused silica capillaries of 75 μm i.d. with a length of 11 cm and evaluated by
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.
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
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
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
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
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
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
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
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
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
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
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
Andreia Teixeira-Castro et al.
Brain : a journal of neurology, 138(Pt 11), 3221-3237 (2015-09-17)
Polyglutamine diseases are a class of dominantly inherited neurodegenerative disorders for which there is no effective treatment. Here we provide evidence that activation of serotonergic signalling is beneficial in animal models of Machado-Joseph disease. We identified citalopram, a selective serotonin
R McAskill et al.
The British journal of psychiatry : the journal of mental science, 173, 203-208 (1999-02-02)
Antidepressant therapy is not always effective and is slow to take effect. In theory, these shortfalls may be caused by induction of neuronal negative feedback via pre-synaptic 5-HTIA receptors. Pindolol, an antagonist at somatodentritic pre-synaptic 5-HTIA receptors has been investigated
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
Drug therapy. Pindolol: a new beta-adrenoceptor antagonist with partial agonist activity.
W H Frishman
The New England journal of medicine, 308(16), 940-944 (1983-04-21)
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
D Herpin et al.
Annales de medecine interne, 139(7), 484-487 (1988-01-01)
Twenty-one patients with mild or moderate hypertension were randomised to receive either Atenolol 100 mg (N = 10) or Pindolol 15 mg (N = 11) in a once daily dosage over a two month period. The effects of these two
Maria J Portella et al.
The Journal of clinical psychiatry, 72(7), 962-969 (2010-11-03)
Since depression entails not only dramatic personal disruption but also a huge amount of medical and socioeconomic burden, slowness of antidepressant action and difficulties to attain remission are entangled issues to be solved. Given the controversial previous findings with enhancing
Monika Agnieszka Zielińska-Pisklak et al.
Magnetic resonance in chemistry : MRC, 49(5), 284-290 (2011-04-15)
The β-blockers are important drugs and decades of clinical experience proved their high medical status. However, to the best of our knowledge, there is no complete assignment of (1)H and (13)C NMR resonances of popular representatives: acebutolol, alpenolol, pindolol, timolol
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
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