Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.4.16.2 (PCP)
 3,761 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Rats were given fixed-time, 1-min food-pellet delivery sessions, for 3 h every day, which resulted in over drinking (schedule-induced polydipsia). In previous research, groups of animals came to prefer solutions of cocaine or lidocaine to concurrently presented water, if the drugs were first offered in a glucose/saccharin vehicle, which was then gradually eliminated, so that the choice became a drug solution in water vehicle versus water. In the present experiment, the same procedure produced a preference for 0.025 mg/ml quinine solution to water, indicating that a bitter solution that was not a topical anesthetic agent could come to be preferred. After establishing preference for quinine solution, it was possible to gradually remove quinine while increasing phencyclidine (PCP) concentration to produce preference for 0.075 mg/ml PCP solution, and similarly to produce subsequent preference for 0.1 mg/ml caffeine solution, although not for all animals. For additional groups, drinking either 0.15 mg/ml PCP or 0.1 mg/ml caffeine, while gradually reducing the glucose/saccharin vehicle to water vehicle was a less successful procedure for establishing the respective drug preferences. The latter result suggests that first instituting a preference for quinine solution to water facilitated the later establishment of preferences for PCP and caffeine solutions.
 ...
PMID:Establishing oral preference for quinine, phencyclidine and caffeine solutions in rats. 1078 Mar

The delayed effects of phencyclidine (PCP) have been shown to disrupt latent inhibition (LI) in a conditioned taste-aversion paradigm. In an attempt to understand the mechanism of this disruption, the delayed effects of the selective sigma receptor agonist 1,3-Di(2-tolyl)guanidine (DTG) and the selective NMDA receptor antagonist MK-801 on latent inhibition were assessed in the same paradigm. Water-deprived male rats were allowed access to either water (nonpreexposed; NPE) or 5% sucrose (preexposed; PE) for 30 min on 2 consecutive days. On the third day, animals were allowed access to sucrose and subsequently injected with lithium chloride. On the forth day, animals were allowed access to both sucrose and water. LI was assessed by comparing the percent sucrose consumed in PE and NPE groups on the fourth day. DTG (1.0, 5.0, or 10.0 mg/kg), MK-801 (0.5, 1.0, or 2.0 mg/kg), or vehicle was administered IP 20 h before preexposure (days 1 and 2) and conditioning (day 3). In vehicle-treated groups, PE animals consumed a significantly higher percent sucrose on the test day than NPE animals, indicating the presence of LI. DTG (10.0 mg/kg) and MK-801 (2.0 mg/kg) decreased the percent sucrose consumed by animals in the PE group to the level observed in the NPE group, indicating disrupted LI. However, this dose of MK-801 was found to produce a decrease in percent sucrose consumed in PE animals not treated with lithium chloride, indicating that the decrease observed in the LI paradigm could be due to MK-801-induced decrease in taste preference for sucrose rather than a disruption of LI. Lower doses of MK-801 that did not produce a decrease in taste preference for sucrose did not significantly disrupt LI. None of the doses of DTG tested altered taste preference for sucrose. These data suggest a role for sigma receptors in the previously observed PCP-induced disruption of LI. Published by Elsevier Science Inc., 2000
 ...
PMID:The delayed effects of DTG and MK-801 on latent inhibition in a conditioned taste-aversion paradigm. 1089 66

The German Environmental Survey (GerES) is a large-scale, representative population study that has been carried out three times up to now with a time interval of about 7 years. GerES I was performed in 1985/1986, GerES IIa in 1990/1991 in West Germany, and GerES IIb in 1991/1992 in East Germany, the former German Democratic Republic (GDR). In GerES II, blood, urine, and scalp hair samples of 4021 adults aged 25-69 years and of 736 children aged 6-14 years were analysed as well as environmental samples (house dust, drinking water, indoor and personal air, diet). Characteristics of the frequency distributions of the substances analysed in the different media were calculated. The geometric mean (GM) for lead, cadmium, and mercury in the blood of adults amounted to 45.3, 0.36, and 0.51 microg/l, respectively. The corresponding values of arsenic, cadmium, and mercury in urine were 6.3, 0.29, and 0.54 microg/l, respectively. The concentrations of lead in blood, cadmium in blood and urine, and mercury in blood are lower in children than in adults. The GM ofpentachlorophenol (PCP) in urine of adults was 2.67 microg/l and in urine of children, 4.15 microg/l. These results of GerES II were compared with the so-called HBM values which represent health-based exposure guidelines and have been defined by the Human Biomonitoring Commission (HBC) of the Federal Environmental Agency, interalia for lead in blood, cadmium in urine, mercury in blood and urine, and PCP in urine. They also provided asound basis for the setting of reference values to describe the status of the German population. A total of 1.8% and 0.6% of the German females in child-bearing age had a level of lead in blood higher than HBM-I (100 microg/l) and HBM-II ( 150 microg/l), respectively. One percent of the children had a blood lead level above HBM-I. House dust and drinking water were analysed to characterise exposure in the domestic environment. Arsenic, cadmium, and lead deposition in homes amounted to 5.4 ng/(m2 day), 11.7 ng/(m2 day), and 0.29 microg/(m2 day), respectively. In the content of vacuum cleaner bags, concentrations were 2.1,0.9, and 5.9 microg/g. PCP, lindane and permethrin could be detected in the house dust of most German households. The pollutant load of the drinking water is significantly influenced by the corrosion of pipe materials and fittings. The new EC limit value of 10 microg/l for lead was exceeded in 7.7% of the first draw samples. The relatively high percentage (14%) of samples from East Germany that exceeded the current German guideline value for formaldehyde of 0.1 ppm in indoor air may be explained by the widespread use of contaminated particleboard in the former GDR.
 ...
PMID:The German Environmental Survey 1990/1992 (GerES II): reference concentrations of selected environmental pollutants in blood, urine, hair, house dust, drinking water and indoor air. 1114 Apr 39

The effect of phencyclidine (PCP) on latent learning was investigated using a one-trial water-finding task in mice. Mice without water deprivation were given PCP or saline before a training trial, which consisted of exposure to a novel open-field environment with an alcove containing a water tube. Twenty to twenty-four hours after water deprivation, animals were placed in the same apparatus and the time required to find the water tube measured (test trial). Saline-treated trained mice showed a significantly shorter time to find the water tube during the test trial (finding latency) than naive mice that had not been trained. When PCP (1mg/kg i.p.) was administered before the training trial, the finding latency was significantly prolonged in comparison with that in the saline-treated mice, indicating that PCP induced impairment of latent learning. 1-(3,4-Dimethoxy-phenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride (SA4503: 0.3 mg/kg s.c.) and (+)-pentazocine (1 mg/kg s.c.), selective sigma(1) receptor agonists, or D-cycloserine (10 and 30mg/kg, s.c.), a glycine binding site agonist, significantly counteracted the PCP-induced impairment of latent learning, whereas (+)-SKF-10,047 (0.1-3 mg/kg s.c.), a putative sigma(1) receptor agonist, did not. The ameliorating effects of SA4503 and (+)-pentazocine were antagonized by N,N-dipropyl-2-(4-methoxy-3-(2-phenylethoxy) phenyl) ethylamine (NE-100: 1 mg/kg i.p.), a selective sigma(1) receptor antagonist. SA4503 also ameliorated the impairment of latent learning induced by dizocilpine, a non-competitive N-methyl-D-aspartate receptor antagonist, the effect being antagonized by NE-100. These results suggest that PCP induces an impairment of latent learning, this effect being mediated via glutamatergic systems, and that activation of sigma(1) receptors ameliorates impairment of latent learning induced by PCP.
 ...
PMID:Phencyclidine impairs latent learning in mice: interaction between glutamatergic systems and sigma(1) receptors. 1118 40

The excitatory amino acid (EAA) agonists, N-methyl-D-aspartate (NMDA) and kainate, elicit a copious drinking response in pigeons. NMDA-induced drinking, as compared with kainate- and water deprivation-induced drinking, is selectively antagonized by the competitive, NMDA receptor antagonist CGS 19755, and appears to be mediated by NMDA receptors located in brain. There have been several studies which have reported differences between competitive and non-competitive (PCP-like) NMDA antagonists in blocking various behavioral effects of NMDA, such as discriminative stimulus effects. The present studies examined the effects of the non-competitive antagonists, phencyclidine (PCP) and dizocilpine, on drinking elicited by NMDA, kainate, and water deprivation. PCP and dizocilpine were effective antagonists of NMDA-induced drinking, resulting in surmountable shifts to the right in agonist dose-response functions. These compounds had little effect on drinking evoked by either kainate or water deprivation. These results support the notion that the dipsogenic effects of NMDA are mediated by NMDA-type receptors, and also provide important information as to the characteristics of non-competitive NMDA antagonists. EAA-induced drinking provides a useful tool for the examination of the behavioral pharmacology of EAA agonists and antagonists.
 ...
PMID:Effects of phencyclidine and dizocilpine on NMDA-, kainate-, and water deprivation-induced drinking in pigeons. 1122 93

Previous drug discrimination studies have elucidated the importance of the NMDA, GABA(A) and 5-HT(1) receptor systems in mediating the discriminative stimulus effects of ethanol. The present study used a three-choice drug discrimination paradigm in an attempt to determine whether the salient NMDA antagonistic effects were separable from other stimulus effects of ethanol. Adult Long-Evans rats (n = 7) were trained to discriminate ethanol (1.5g/kg, intragastric (i.g.)), the uncompetitive NMDA antagonist dizocilpine (0.17mg/kg, i.g.) or water (3.5ml, i.g.) under a food-reinforced fixed-ratio 15 (FR15) schedule of reinforcement. Following training, substitution tests were conducted with the GABA(A)/benzodiazepine (GABA(A)/BDZ) positive modulator pentobarbital (PB, 5.6-17mg/kg, i.g.), the uncompetitive NMDA antagonist phenycldine (PCP, 0.1-5.6mg/kg, i.p.) and the 5-HT(1) agonist RU 24969 (0.1-3.0mg/kg, i.p.). Complete substitution of PCP (ED(50), 0.9mg/kg) for dizocilpine was found in all animals. Conversely, PB (ED(50), 10mg/kg) substituted fully for ethanol in five of seven animals, whereas RU 24969 (ED(50), 1.4mg/kg) completely substituted for ethanol in only three of seven animals tested. The result demonstrate that a three-choice discrimination using dizocilpine, ethanol and water as training conditions can be established in rats. By contrasting the discriminative stimulus effects of an uncompetitive NMDA antagonist to ethanol, the ethanol-like effects of pentobarbital and RU 24969 are attenuated compared to previous studies of two-choice ethanol water discrimination.
 ...
PMID:Assessment of the mixed discriminative stimulus effects of ethanol in a three-choice ethanol-dizocilpine-water discrimination in rats. 1122 67

Neuroprotective and biobehavioral properties of a series of novel open chain MK-801 analogs, as well as their structure-activity relationships have been investigated. Three groups of compounds were synthesized: monobenzylamino, benzhydrylamino, and dibenzylamino (DBA) analogs of MK-801. It was revealed that DBA analogs exhibit pronounced glutamate-induced calcium uptake blocking properties and anti-NMDA activity. The hit compound of DBA series, NT-1505, was investigated for its ability to improve cognition functions in animal model of Alzheimer's disease type dementia, simulated by treating animals with cholinotoxin AF64A. The results from an active avoidance test and a Morris water maze test showed that experimental animals, treated additionally with NT-1505, exhibited much better learning ability and memory than the control group (AF64A treated) and close to that of the vehicle group of animals (treated with physiological solution). Study of NT-1505 influence on locomotor activity revealed that it is characterized by a spectrum of behavioral activity radically different from that of MK-801, and in contrast to the latter one does not produce any psychotomimetic side effects in the therapeutically significant dose interval. The computed docking of MK-801 and its flexible analogs on the NMDA receptor elucidated the crucial role of the hydrogen bond formed between these compounds and the asparagine residue for magnesium binding in the NMDA receptor. It was suggested that strong hydrophobic interaction between MK-801 and the hydrophobic pocket in the NMDA receptor-channel complex determines much higher irreversibility of this adduct compared to the intermediates formed between this site and Mg ions or flexible DBA derivatives, which might explain the absence of PCP-like side effects of the latter compounds.
 ...
PMID:Neuroprotective and cognition-enhancing properties of MK-801 flexible analogs. Structure-activity relationships. 1146 74

The Dreissena-Monitor is a biological early warning system for the continuous monitoring of river water quality, based on the valve movements of two groups of 42 zebra mussels (Dreissena polymorpha). Laboratory experiments with Cd, PCP, and 2-chloro-4-nitro-aniline were conducted in combination with suspended particles (a mixture of stinging nettle powder, bentonite, and quartz powder). An increase of suspended particles up to a nominal concentration of 540 mg/L within 5 min did not evoke any reactions by the mussels significantly different from normal. The distribution between water and solids was analyzed for Cd and 2-chloro-4-nitroaniline, with the result that the former quickly adsorbed to the particles, whereas the latter did not bind to the particles at all. The behavior of the zebra mussels revealed that the detection of 2-chloro-4-nitro-aniline was not affected by the presence of suspended matter. In the cases of Cd and PCP, D. polymorpha was able to detect these substances when they were particle-associated at least as well or better as when they were dissolved in the water. The results are discussed with respect to the physiology of the organisms and the bioavailability of toxicants, as well as to the consequences these results may have under field conditions.
 ...
PMID:The influence of suspended particles on the acute toxicity of 2-chloro-4-nitro-aniline, cadmium, and pentachlorophenol on the valve movement response of the zebra mussel (Dreissena polymorpha). 1152 92

Lake Baikal, a unique habitat for a great number of endemic species, is the largest freshwater reservoir in the world which is still largely unaffected by anthropogenic pollution, except for some shore regions with industrial activity. The expressions of a biomarker of exposure (heat shock protein Hsp70) and a biomarker of effect (DNA single-strand breaks) were measured for the first time in endemic Baikalian sponge species (Baikalospongia intermedia, Lubomirskia fusifera, and Lubomirskia abietina). Tissue cubes of B. intermedia and dissociated cells of L. fusifera and L. abietina reacted to temperature stress (10-16 degrees C above ambient temperature) with a time-dependent increase in expression of Hsp70. In B. intermedia, the effects of model pollutants (lead, copper, and zinc, and the organochlorines tetrachloroguaiacol, TCG, and pentachlorophenol, PCP) and of the wastewater from the final refinement and aeration reservoirs of the Baikalsk Pulp and Paper Plant (BPPP), located at the shore of the southern basin of Lake Baikal, on the expression of Hsp70 and the extent of DNA damage were investigated. It was found that lead and zinc but not copper cause a strong induction of Hsp70 in this sponge, while the frequency of DNA single-strand breaks increased after exposure to all these heavy metals tested. Induction of DNA single-strand breaks was also observed after exposure to TCG and PCP, but these compounds did not (consistently) enhance Hsp70 expression. Wastewater taken from the final water aeration pond of BPPP caused a concentration-dependent increase in Hsp70 expression in B. intermedia. However, there was no difference in the basal levels of Hsp70 between sponges collected in the shallow water at an unpolluted site near Baikalsk City and at a polluted site where the wastewaters of BPPP are discharged into the lake. There was also no clear difference in the wastewater concentration-dependent induction of Hsp70 expression between sponges collected at these sites, indicating no adaptation to continuous stress exposure.
 ...
PMID:Heat shock protein Hsp70 expression and DNA damage in Baikalian sponges exposed to model pollutants and wastewater from Baikalsk Pulp and Paper Plant. 1193 6

Photocatalysts Pt/TiO2 coated on hollow glass beads were prepared by tetrabutyl titanate hydrolysis with Sodium silicate on hollow glass beads at various condition and loaded with platinum varying from 0.2% to 2.4% by weight. Sodium pentachlorophenolate (PCP-Na) solution were used to examined for their photoactivity and characterized by X-ray and BET. The results indicated that the optimization condition to prepare photocatalysts: Water to titanium alkoxides was 100, Sintering temperature was 650 degrees C, Diameter of hollow glass beads was 0.5 mm, TiO2: sodium silicate: hollow glass beads was 10:2.5:20, Platinum content of photocatalysts was about 1.4%-1.6%. When the experiments were carried out in such conditions, the initial concentration of PCP-Na was 100 mg/L, initial pH was 6.5, oxygen flux was 1.6 mL/s, illumination intensity was 30 kW.m-2, catalysts was 2 g/L, illumination time was 2 hours, respectively. Then the rates removals of PCP-Na could reach 92.0%.
 ...
PMID:[Tetrabutyl titanate hydrolysis prepared TiO2 photocatalysis loaded with platinum technology]. 1198 10


<< Previous 1 2 3 4 5 6 7 8 9 10 Next >>