Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.4.16.2 (PCP)
3,761 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Permeable spheroplasts were prepared from two strains of Saccharomyces cerevisiae by incubating with zymolyase without a permeabilizing agent. The loss of the plasma membrane barrier was confirmed by the nucleotide release, the activity of glucose 6-phosphate dehydrogenase with external substrates and by the effects on respiration of mitochondrial substrates and ADP. Mitochondrial integrity was maintained, as shown by respiration with lactate, pyruvate, glucose and ethanol, and its acceleration by ADP showed a coupled respiration. Potassium uptake into the vacuole was measured with a selective electrode and found to be taken up effectively by spheroplasts only in the presence of Mg-ATP; it was reverted by CCCP and PCP and inhibited by bafilomycin A1, but not by sodium vanadate or sodium azide. Potassium ions did not alter DeltaPsi of the vacuole, followed with oxonol V, but caused vacuolar alkalinization, as followed with pyranine. The increase of vacuolar pH was non-selective and observed at 50-200 mM of several monovalent cations. Isolated vacuoles with pyranine inside showed similar changes of the internal pH in the presence of KCl. Results indicate that some strains do not require a permeabilizing agent to directly access the vacuole in spheroplasts prepared with zymolyase. The hypothesis about the existence of a K+/H+ antiporter in the vacuolar membrane of S. cerevisiae is discussed.
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PMID:In situ study of K+ transport into the vacuole of Saccharomyces cerevisiae. 1603 2

Phencyclidine (1-(1-phenylcyclohexyl)piperidine, CAS 956-90-1, PCP) has shown analgesic effects. Some of its derivatives were synthesized and their biological properties were studied. To date, only saturated ketones have been used as starting materials for synthesizing the phencyclidine family. In order to show desirable biological activity, the aromatic and piperidine rings are necessary for these compounds. Using alpha-tetralone as a starting material, 2-hydroxy-1-(-phenyltetralyl)piperidine, an analogue of the phencyclidine family, and some of its intermediates were synthesized. This ketone was reacted with phenyl magnesium bromide and the resultant alcohol was reacted with acetic anhydride to give alkene that was treated with potassium permanganate to give diol. This compound was treated with a suspension of sodium azide and trichloroacetic acid to give the azide compound that was reduced with LiAlH4 to give the primary amine. Cyclization of this compound with 1,5-dibromopentane finally gave a tertiary amine. It is predicted that the title compound 2-hydroxy-1-(1-phenyltetralyl)piperidine exerts a potent analgesic effect on acute and phasic pain.
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PMID:Synthesis and biological properties of 2-hydroxy-1-(1-phenyltetralyl)piperidine and some of its intermediates as derivatives of phencyclidine. 1622 17

The current concentrations of polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs) were determined in soils contaminated with Chinese technical product sodium pentachlorophenate (Na-PCP). The estimated half-life of octachlorodioxin (OCDD) was about 14 years in contaminated soils based on the local historical record and mass balance calculation during the past 43 years (1960-2003). The isomer profiles remained the same regardless of paddy field soil or riverbank soil. The results indicated that the congener-specific information was efficient in estimating the PCDD/Fs fate in contaminated soils.
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PMID:Estimation of OCDD degradation rate in soil. 1646 91

Lacosamide (LCM) is anticonvulsant in animal models and is in phase 3 assessment for epilepsy and neuropathic pain. Here we seek to identify cellular actions for the new drug and effects on recognised target sites for anticonvulsant drugs. Radioligand binding and electrophysiology were used to study the effects of LCM at well-established mammalian targets for clinical anticonvulsants. 10 microM LCM did not bind with high affinity to a plethora of rodent, guinea pig or human receptor sites including: AMPA; Kainate; NMDA (glycine/PCP/MK801); GABA(A) (muscimol/benzodiazepine); GABA(B); adenosine A1,2,3; alpha1, alpha2; beta1, beta2; M1,2,3,4,5; H1,2,3; CB1,2; D1,2,3,4,5; 5HT1A,1B,2A,2C,3,5A,6,7 and KATP. Weak displacement (25%) was evident at batrachotoxin site 2 on voltage gated Na+ channels. LCM did not inhibit neurotransmitter transport mechanisms for norepinephrine, dopamine, 5-HT or GABA, nor did it inhibit GABA transaminase. LCM at 100 microM produced a significant reduction in the incidence of excitatory postsynaptic currents (EPSC's) and inhibitory postsynaptic currents (IPSC's) in cultured cortical cells and blocked spontaneous action potentials (EC50 61 microM). LCM did not alter resting membrane potential or passive membrane properties following application of voltage ramps between -70 to +20 mV. The voltage-gated sodium channel (VGSC) blocker phenytoin potently blocked sustained repetitive firing (SRF) but, in contrast, 100 microM LCM failed to block SRF. No effect was observed on voltage-clamped Ca2+ channels (T-, L-, N- or P-type). Delayed-rectifier or A-type potassium currents were not modulated by LCM (100 microM). LCM did not mimic the effects of diazepam as an allosteric modulator of GABA(A) receptor currents, nor did it significantly modulate evoked excitatory neurotransmission mediated by NMDA or AMPA receptors (n > or = 5). Evidently LCM perturbs excitability in primary cortical cultures but does not appear to do so via a high-affinity interaction with an acknowledged recognition site on a target for existing antiepileptic drugs.
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PMID:Seeking a mechanism of action for the novel anticonvulsant lacosamide. 1662 Aug 82

Cystine-knot microproteins exhibit several properties that make them highly interesting as scaffolds for oral peptide drug delivery. It was therefore the aim of the study to evaluate the novel clinically relevant cystine-knot microprotein McoEeTI regarding its potential for oral delivery. Additionally, based on the gained results, important features of McoEeTI were improved. Enzymatic degradation was caused by chymotrypsin, trypsin and porcine small intestinal juice whereas McoEeTI was stable towards elastase, membrane bound proteases, pepsin and porcine gastric juice. Only minor McoEeTI degradation was observed during a 24h incubation period in rat plasma. In the presence of various physiological ions about 50% of McoEeTI formed di- and/or trimers. P(app) value of McoEeTI was determined to be (7.4+/-0.4)x10(-6)cm/s. Sodium caprate and polycarbophil-cysteine (PCP-Cys) had no beneficial effect on McoEeTI permeation, whereas the utilization of a chitosan-thiobutylamidine (Chito-TBA) system improved McoEeTI permeation 3-fold. Enzymatic stability could be strongly improved by the utilization of Bowman-Birk-Inhibitor (BBI) as well as PCP-Cys. In conclusion, this study indicates that McoEeTI represents a promising candidate as a novel scaffold for oral peptide drug delivery.
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PMID:Evaluation and improvement of the properties of the novel cystine-knot microprotein McoEeTI for oral administration. 1707 Jun 61

Hydrothermal decomposition of pentachlorophenol (PCP, C6HCl5O), as the probable human carcinogen, was investigated in a tubular reactor under subcritical and supercritical water with sodium hydroxide (NaOH) addition. The experiments were conducted at a temperature range of 300-420 degrees C and a fixed pressure of 25 MPa, with a residence time that ranged from 10 s to 70 s. Under the reaction conditions, the initial PCP concentrations were varied from 0.25 to 1.39 mmol/L and the NaOH concentrations were varied from 2.5 to 25 times of the concentrations of PCP. The result of this study showed that PCP conversion in supercritical water was highly dependent on the reaction temperature, residence time, and NaOH concentration. PCP conversion in subcritical water is, however, only dependent on reaction temperature. NaOH concentration and residence times were found to have little effect on PCP conversion in subcritical condition. It was found that NaOH concentration affected the dechlorinations of PCP in the supercritical water. The intermediates detected were proposed to be tetrachlorophenol and trichlorophenol, respectively.
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PMID:Hydrothermal decomposition of pentachlorophenol in subcritical and supercritical water with sodium hydroxide addition. 1796 37

The concentration of polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs) were determined in soils and different species of vegetation collected from the Dongting Lake region, China. Use of sodium pentachlorophenate (Na-PCP) was the main contamination source of PCDD/Fs for soil/sediment and vegetation in the Dongting Lake region. Reed (Phragmitas communis Trin), Polygonum orientale L., and Artemisia selengensis Turcz ex Bess were selected as model plants to explore the pathway of PCDD/Fs transfer from contaminated soil to vegetation. In the vegetation tissue samples, the total international toxic equivalency values ranged from 0.14 to 1.64 pg international toxic equivalency/g dry weight with a mean value of 0.67 pg international toxic equivalency/g dry weight. Polychlorinated dibenzo-p-dioxins and dibenzofurans congener distribution and bioaccumulation varied among vegetation species. Polychlorinated dibenzo-p-dioxins and dibenzofuran levels in the leaves were found to be higher than those in the root and stem, which were affected considerably by volatilization from contaminated soil. Volatilization from polluted soil and subsequent sorption to leaves may be a significant pathway for contamination of vegetation in Dongting Lake region.
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PMID:Tissue-dependent distribution and bioaccumulation of polychlorinated dibenzo-p-dioxins and dibenzofurans in vegetation samples collected from Dongting Lake, China. 1809 69

Dongting Lake is the second largest freshwater lake in China. Technical sodium pentachlorophenate (Na-PCP) had been sprayed since 1960s to control the spread of snailborne schistosomiasis up to the middle of 1990s. As one of the by-products of Na-PCP, polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs) may enter the environment. It has been reported that the concentrations of PCDD/Fs in sediments in Dongting Lake were 130-891 pg I-TEQ g(-1) in 1995. High toxicity of sediment to exposed microorganisms and fish may be risk on environment. In order to determine the present levels of the contamination, eight sediment samples from Dongting Lake were analyzed for PCDD/Fs using HRGC-HRMS. Total I-TEQ values for these samples were at a ranged of 0.7-11 pg g(-1), with a mean value of 4.5 pg g(-1). The results show that PCDD/Fs concentrations of contemporary sediment have declined since 1995. Certain PCDD/F congeners as well as OCDD, typical for Na-PCP, predominated in lake sediment indicating that the using of PCP-Na is the main source of PCDD/Fs in the lake. These variations in levels can reflect changes in PCDD/F sources to the environment over time.
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PMID:Declining polychlorinated dibenzo-p-dioxins and dibenzofurans levels in the sediments from Dongting Lake in China. 1845 58

Using western blottings, microdialysis, and functional assays we tested the hypothesis that phencyclidine (PCP) modifies the expression and function of glutamate (Glu) transporters in the rat frontal cortex. Western blotting studies revealed that administration of PCP (10 mg/kg/day; 7 days) increased significantly the expression of the astrocytic Glu transporter GLT-1/EAAT2. Functional studies showed that PCP increased significantly Na+-dependent Glu uptake in slices and in neuron/astrocyte co-cultures, and microdialysis studies evidenced that PCP treatment reduced basal Glu output. In our experimental conditions, PCP did not induce toxicity. These studies show that PCP increases the expression of GLT-1 in the cerebral cortex, thereby increasing Glu uptake and reducing extracellular [Glu].
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PMID:GLT-1 expression and Glu uptake in rat cerebral cortex are increased by phencyclidine. 1861 69

Early effects of 0.0001-10 mM sodium pentachlorophenate (PCP-Na) on the green alga Chlorella pyrenoidosa Chick. S-39 involves a rapid (within 1-2 min) decrease in the light-induced oxygen evolution by algal cells. The suppressed relative yield of variable chlorophyll fluorescence in C. pyrenoidosa in the presence of high PCP-Na concentrations and its dynamics provide evidence for rapid inactivation of photosystem 2, which is not observed at low concentrations of the toxicant. An analysis of the induction curve of delayed chlorophyll fluorescence in algal cells suggests that PCP-Na at low concentrations disturbs the coupling of electron transport and phosphorylation, whereas at high concentrations it inhibits electron transport and decreases the energy potential of photosynthetic membranes. The early toxic effect of PCP-Na is responsible for subsequent impairment of C. pyrenoidosa productivity.
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PMID:[Early effect of sodium pentachlorophenate on photosynthetic activity of the alga Chlorella pyrenoidosa Chick S-39]. 1866 67


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