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Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.
Donald M N Sikazwe et al.
Bioorganic & medicinal chemistry, 17(4), 1716-1723 (2009-01-22)
Arylcycloalkylamines, such as phenyl piperidines and piperazines and their arylalkyl substituents, constitute pharmacophoric groups exemplified in several antipsychotic agents. A review of previous reports indicates that arylalkyl substituents can improve the potency and selectivity of the binding affinity at D(2)-like
Peter Kranke et al.
European journal of clinical pharmacology, 68(11), 1465-1472 (2012-05-02)
Buspirone, a partial 5HT(1A) agonist and D₂ and D₃ antagonist, has shown promising antiemetic efficacy when given parenterally in animal models, but its efficacy for the prevention of postoperative nausea and vomiting (PONV) is unknown. To study the efficacy and
A Gobert et al.
Neuroscience, 93(4), 1251-1262 (1999-09-29)
The serotonin1A receptor partial agonist, buspirone, also displays antagonist properties at D2 receptors and is metabolized to the alpha2-adrenergic receptor antagonist, 1-(2-pyrimidinyl-piperazine). Herein, we examined mechanisms underlying the influence of buspirone alone, and in association with the serotonin reuptake inhibitor
D Manahan-Vaughan et al.
European journal of pharmacology, 294(2-3), 617-624 (1995-12-29)
The effects of acute and repeated treatment with 1-(2-pyrimidinyl)piperazine (1-PP), a metabolite of the 5-HT1A receptor ligand azapirones, were investigated on hippocampal excitatory synaptic transmission. Recordings of the electrically evoked field population excitatory post-synaptic potentials (e.p.s.p.s.) were carried out in
P H Marathe et al.
The Journal of pharmacy and pharmacology, 51(5), 601-607 (1999-07-20)
Pharmacokinetics of buspirone and its active metabolite, 1-pyrimidinyl piperazine (1-PP) following oral administration were assessed in rhesus monkeys at doses used in chronic toxicology studies. The study was conducted over four periods in three male and three female rhesus monkeys.
Yumi Sugimoto et al.
Biological & pharmaceutical bulletin, 28(4), 733-735 (2005-04-02)
Effects of serotonergic anxiolytic buspirone on immobilization-induced hyperglycemia were studied in mice. Stress elicited hyperglycemia in mice. Pretreatment with buspirone significantly reduced immobilization-induced hyperglycemia. Buspirone increased serum insulin levels in both non- and stressed mice. The major metabolite of buspirone
B J Cao et al.
Neuropharmacology, 36(8), 1089-1097 (1997-08-01)
It has been suggested that in vivo formation of the metabolite 1-(2-pyrimidinyl)-piperazine (1-PP) may be a major drawback in the use of buspirone as an anti-anxiety agent. To test this hypothesis, the effects of buspirone, alone or with proadifen (an
Lijuan Zhang et al.
Proteomics, 9(16), 4093-4097 (2009-08-07)
A novel strategy based on carboxy group derivatization is presented for specific characterization of phosphopeptides. By tagging the carboxy group with 1-(2-pyrimidyl) piperazine (PP), the ion charge states of phosphopeptides can be largely enhanced, showing great advantages for sequencing phosphorylated
Klaas P Zuideveld et al.
The Journal of pharmacology and experimental therapeutics, 303(3), 1130-1137 (2002-11-20)
The objective of this investigation was to compare the in vivo potency and intrinsic activity of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine (1-PP) in rats by pharmacokinetic-pharmacodynamic modeling. Following intravenous administration of buspirone (5 or 15 mg/kg in 15 min) or
I Berlin et al.
British journal of clinical pharmacology, 39(3), 243-249 (1995-03-01)
1. Because the 5-HT1A agonist anxiolytic azapirones have a common alpha 2-adrenoceptor antagonist metabolite, 1-(2-pyrimidinyl)-piperazine (1PP), we measured central and peripheral alpha 2-adrenoceptor dependent responses before and after intravenous administration of 0.15 mg clonidine when healthy subjects were taking buspirone
Lenka Munoz et al.
Journal of neuroinflammation, 4, 21-21 (2007-09-06)
An accumulating body of evidence is consistent with the hypothesis that excessive or prolonged increases in proinflammatory cytokine production by activated glia is a contributor to the progression of pathophysiology that is causally linked to synaptic dysfunction and hippocampal behavior
L L von Moltke et al.
Psychopharmacology, 140(3), 293-299 (1999-01-07)
Biotransformation of gepirone to its principal metabolite, 1-(2-pyrimidinyl)-piperazine (1-PP), was studied in human liver microsomes and in microsomes from cDNA-transfected human lymphoblastoid cells. Formation of 1-PP from gepirone in liver microsomes proceeded with a mean apparent Km ranging from 335
O Van Reeth et al.
Behavioural pharmacology, 10(2), 119-130 (2000-04-26)
Abnormal timing in the circadian system is reported in endogenous depression. Gepirone, a 5HT1A receptor partial agonist, has anxiolytic and antidepressant properties. We determined whether gepirone was able to modify the functioning of the circadian system. Single i.p. injections of
M Hascoët et al.
Pharmacology, biochemistry, and behavior, 67(1), 45-53 (2000-12-13)
Although numerous animal procedures have been employed in the study of antidepressants (ADs) in anxiety, the results following acute administration remain highly variable. The present study investigated the effect of the SSRI paroxetine (4, 8, and 16 mg/kg, IP) in
David J Greenblatt et al.
Biopharmaceutics & drug disposition, 24(2), 87-94 (2003-03-06)
Biotransformation of gepirone to 1-(2-pyrimidinyl)-piperazine (1-PP) and 3'-OH-gepirone, as well as two other hydroxylated metabolites, was studied in vitro using a human liver microsomal preparation and heterologously expressed human CYP3A4 and CYP2D6. The focus was on a low range of
Yumi Sugimoto et al.
Journal of pharmacological sciences, 93(4), 446-450 (2004-01-23)
Effects of the serotonergic anxiolytic buspirone on plasma glucose and glucose-induced hyperglycemia were studied in mice. Buspirone did not affect plasma glucose levels of non-fasted mice, while it increased serum insulin levels. In fasted mice, buspirone significantly reduced glucose-induced hyperglycemia
Juneha Bak et al.
Analytical sciences : the international journal of the Japan Society for Analytical Chemistry, 36(10), 1269-1274 (2020-06-23)
Sulfated saccharides exhibit diverse physiological activities, but a lack of any convenient assay hinders their evaluation. Herein, an assay for the analysis of sulfated saccharides is described using 1H nuclear magnetic resonance (NMR) spectroscopy by employing ligands that can form
A H Vaidya et al.
Methods and findings in experimental and clinical pharmacology, 27(4), 245-255 (2005-08-06)
Most studies concerning the effects of oral buspirone in the rat elevated plus-maze (EPM) test, spontaneous motor activity (SMA) test, and Vogel conflict (VC) test have used Sprague-Dawley or Wistar rats. Although it has been documented that the behavior of
J Odontiadis et al.
Journal of pharmaceutical and biomedical analysis, 14(3), 347-351 (1996-01-01)
Buspirone is a member of the azapirone group of anxiolytic drugs and has one major metabolite, 1-(2-pyrimidinyl)piperazine (1-PP). The analyte, its metabolite and the internal standard were extracted from plasma utilizing solid-phase extraction columns. Chromatography was performed using isocratic reversed-phase
I Mahmood et al.
Clinical pharmacokinetics, 36(4), 277-287 (1999-05-13)
Buspirone is an anxiolytic drug given at a dosage of 15 mg/day. The mechanism of action of the drug is not well characterised, but it may exert its effect by acting on the dopaminergic system in the central nervous system
Jinjun Wu et al.
Journal of ethnopharmacology, 170, 251-254 (2015-05-24)
Wutou (WT, Radix Aconiti), the mother root of Aconitum carmichaelii Debx., is a famous Chinese herb against rheumatoid arthritis. In Chinese clinics, PWT is often prepared as a decoction in combination with other herbs, such as Wutou decoction (WTD). The
K T Kivistö et al.
Pharmacology & toxicology, 84(2), 94-97 (1999-03-06)
The effects of inhibition and induction of the metabolism of buspirone on the plasma concentrations of 1-(2-pyrimidinyl)-piperazine (a piperazine metabolite), the principal active metabolite of buspirone, were investigated. Two separate randomized, placebo-controlled cross-over studies with two phases were carried out
Lijun Zhu et al.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 51, 396-403 (2012-10-23)
Aconitum species are widely used to treat rheumatism, cardiovascular diseases, and tumors in China and other Asian countries. The herbs are always used with drugs such as paclitaxel. Aconitine (AC) is one of the main bioactive/high-toxic alkaloids of Aconitum roots.
V Jagannathan et al.
Methods and findings in experimental and clinical pharmacology, 19(5), 351-362 (1997-06-01)
This study was designed to evaluate the relationship between the pharmacokinetic(s) (PK) and CNS pharmacodynamic(s) (PD) of buspirone, an antidepressant/anxiolytic, in 6 healthy male volunteers placed on an acute L-tryptophan deficient (ATD) diet. The study was a randomized, double-blind, placebo-controlled
Robert A Myers et al.
Neurourology and urodynamics, 23(7), 709-715 (2004-09-24)
To examine the effects of 1-(2-pyrimidinyl)-piperazine (1-PP), a buspirone metabolite, on bladder function in vivo. Micturition reflexes in the rat were evaluated in two models of bladder function; a constant infusion model employing 0.5% acetic acid and an isovolumic model.
A J Gower et al.
European journal of pharmacology, 155(1-2), 129-137 (1988-10-11)
The anxiolytic effects of buspirone, its metabolite, 1-(2-pyrimidyl)piperazine (1-PP) and several alpha 2-adrenoceptor antagonists have been compared in an anticonflict (shock-induced suppression of drinking) paradigm in rats. Idazoxan, WY 26392 and yohimbine had anticonflict effects comparable to those of buspirone
Kari Laine et al.
European journal of clinical pharmacology, 59(10), 761-766 (2003-10-21)
Preliminary in vitro findings indicated that the novel anxiolytic drug, deramciclane is a substrate for the cytochrome P(450) (CYP) 3A4 isoenzyme. Moreover, its co-administration with buspirone, another anxiolytic drug, is likely in clinical practice. The primary objective of the present
Xiaoqiang Qiao et al.
Rapid communications in mass spectrometry : RCM, 25(5), 639-646 (2011-02-04)
Piperazine-based derivatives, including 1-(2-pyridyl)piperazine (2-PP), 1-(2-pyrimidyl)piperazine (2-PMP), 1-(4-pyridyl)piperazine (4-PP), and 1-(1-methyl-4-piperidinyl)piperazine (M-PP), were used for the derivatization of carboxyl groups on peptides with 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) and 1-hydroxy-7-azabenzotriazole (HOAt) as coupling reagents, and trifluoroacetic acid (TFA) as activator. Taking synthetic
K T Kivistö et al.
Therapeutic drug monitoring, 21(3), 317-321 (1999-06-12)
Two separate gas chromatographic methods for the determination of buspirone and its active metabolite, 1-(2-pyrimidinyl)-piperazine (1-PP) in human plasma are described. Both procedures involve solid-phase extraction (the packing material of the cartridges used was C8 for buspirone and a mixed-mode
David J Edwards et al.
Journal of clinical pharmacology, 46(5), 508-514 (2006-04-28)
Buspirone is used to treat generalized anxiety disorder in children and may be useful in developmental disorders in which brain serotonin synthesis is altered. Autistic children (13 boys, 7 girls) were given a single oral dose of 2.5 mg (2-3
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