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)

Using Sokoloff's 2-deoxyglucose (2-DG) autoradiographic technique, the psychotomimetic drug, phencyclidine (PCP, "angel dust") dramatically increased metabolism in diencephalic and telencephalic brain regions known to be rich in high affinity PCP receptors. These effects were greatest in the limbic circuit described in 1937 by the neurologist James Papez (mammillary bodies, anterior thalamus, cingulate gyrus, entorhinal cortex, hippocampus, fornix) and the terminal zones of dopaminergic projections. Caudal to the prefrontal cortex, the cerebral cortex developed an anterior-posterior metabolic gradient somewhat similar to that reported in schizophrenia. Brainstem areas were generally unaffected. These data 1) provide functional data to support Papez' assertion that his central limbic circuit may be important in emotional expression, 2) reaffirm the potential importance of dopaminergic function in psychotic-like behaviors, 3) provide an animal model for schizophrenia, and 4) establish that PCP uses high affinity PCP receptor binding sites to express its psychobiological effects.
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PMID:Dramatic limbic and cortical effects mediated by high affinity PCP receptors. 284 May 40

The effects of phencyclidine (PCP) on regional cerebral glucose utilization was determined by using quantitative autoradiography with [14C]-2-deoxyglucose. PCP increased brain metabolism in selected areas of cortex, particularly limbic, and in the basal ganglia and thalamus, whereas the drug decreased metabolism in areas related to audition. These results are consistent with the known physiology of central PCP neurons and may help to suggest brain areas involved in PCP-mediated actions. Moreover, based on the behavioral similarities between PCP psychosis and an acute schizophrenic episode, these data may be relevant to the understanding of schizophrenia. The PCP-receptor-acylating agent, metaphit, blocked most of these PCP actions. In addition, metaphit by itself was found to diminish glucose utilization rather uniformly throughout brain. These results indicate an antagonist effect of metaphit on the PCP system and suggest a widespread action of metaphit, putatively at a PCP-related site, possibly in connection with the N-methyl-D-aspartate (NMDA) receptor.
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PMID:PCP-induced alterations in cerebral glucose utilization in rat brain: blockade by metaphit, a PCP-receptor-acylating agent. 285 Jun 26

Phencyclidine (PCP) is a widely abused drug of the arylcyclohexylamine class which is capable of producing symptoms of acute psychosis in man. PCP interacts with a specific CNS receptor, for which a putative endogenous peptide ligand has been identified. We have investigated whether PCP receptor binding parameters are modulated by activity in central opiate pathways. We have found that chronic administration of both an opiate agonist (etonitazene) and an opiate antagonist (naloxone) are able to decrease the affinity of the PCP receptor for TCP, a thienyl derivative of PCP. Furthermore, naloxone, but not etonitazene, resulted in a significant increase in the Bmax of TCP binding to the PCP receptor. These results suggest that neural activity mediated by CNS opioids systems is capable of affecting the binding parameters of the PCP receptor.
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PMID:Rat brain PCP receptors: alterations in binding parameters following chronic administration of opiate agonists and antagonists. 289 Oct 74

PCP or "angel dust" is a dissociative anesthetic agent with notoriety as an abuse substance. Numerous members of many subcultures are frequent users of this drug. It is well known in California's psychedelia, along the East Coast, and in the middle- and working-class suburbs of the Midwest. It is important that practitioners become acquainted with the drug and its effects. Persons intoxicated with PCP have murdered their own children and have even jumped out of high-rise apartment buildings. States of florid psychosis lasting for days can follow a brief encounter with PCP. Inadvertent administration of narcotics and barbiturates to patients with acute PCP intoxication can lead to a crisis that could prove to be fatal.
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PMID:Phencyclidine (PCP) abuse. A close-up look at a growing problem. 293 52

PCP is again becoming a popular drug of abuse in the United States, particularly among the young. A variety of medical, psychiatric and pathologic effects make PCP both appealing and profoundly dangerous to naive and chronic drug users. Pharmacologic intervention is helpful in PCP-induced acute intoxication and psychosis. Effective long-term treatment is available in addiction programs.
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PMID:PCP: a dangerous drug. 304 73

We performed a retrospective chart analysis of 33 patients with an Emergency Department discharge diagnosis of phencyclidine (PCP) intoxication. All 33 cases presented to the Emergency Department between November 1986 and April 1987. Thirty of the 33 patients (91%) were classified as mildly intoxicated (per clinical syndrome as described by Aronow and Done) while the remaining 3 patients (9%) were moderately intoxicated. Two of the patients (6%) required benzodiazepine therapy for agitation while an additional 3 patients (9%) required haloperidol for psychotic symptoms. Twenty-three patients (70%) did not require any medication. Of particular interest was our finding that 11 of the 27 males (41%) required leather restraints for agitation or violent behavior while none of the 6 female patients required leather restraints (Fisher's exact test, p = 0.00078). While nursing perception of physical strength may be a confounder, level of agitation and violent behavior is our primary indication for use of restraints. We believe that there is a sexual disparity in level of agitation and violent behavior induced by PCP. We hypothesize that this may be due to pharmacokinetic factors (such as difference in body fat distribution between the sexes) or biological differences in the central nervous system.
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PMID:Analysis of sexual disparity of violent behavior in PCP intoxication. 335 86

The effect of trifluoperazine (TFP) and phencyclidine (PCP) on acetylcholine receptor (AChR) function was studied in rat muscles differentiated in cell culture. While both drugs exerted an inhibitory effect on carbamylcholine (CCh)-induced Na+ or Ca2+ influx (I50 = 5-7 microM), alpha-bungarotoxin binding was not affected. The inhibitory effect of both drugs was independent of CCh concentration, which deems it unlikely that these drugs enhanced desensitization. The mutual inhibitory effect of TFP and PCP on Ca2+ influx was analyzed using three alternative models of interaction between the two drugs: competitive, additive and synergistic inhibition models. Our results are in accordance with a synergistic interaction between the drugs. This synergistic interaction between the drugs provides a biochemical rationale to the phenothiazine contraindication in the treatment of PCP psychosis.
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PMID:Trifluoperazine and phencyclidine inhibit synergistically carbamylcholine-induced cation influx in muscle cultures. 343 92

In a public hospital emergency room, 580 urines were screened for phencyclidine (PCP) with the routine EMIT-DAU PCP screen, the extended EMIT-DAU PCP screen, and a gas chromatograph/mass spectrometer/computer (GC/MS/COMP) in selected ion mode, which was chosen as the reference method. The extended method produced a 38.5% increase in positives detected over the routine EMIT-DAU PCP screen and allowed 66.4% of the specimens to be signed out as negative without confirmation by GC/MS/COMP. This ability to provide a rapid, relatively inexpensive screen for PCP in urine and, in particular, to eliminate those patients whose specimens are negative, is important in a psychiatric population that contains many acutely psychotic individuals with grossly abnormal behavior.
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PMID:Extended EMIT-DAU phencyclidine screen. 351 84

An individual suspected of being under the influence of phencyclidine (PCP) exhibited acute psychotic and violent behavior which was followed by cardiac arrest, coma, and renal failure. Sections of the damaged muscle showed rhabdomyolysis, and sections of the kidneys showed myoglonin casts positive for immunoperoxidase stain. Extensive toxicology studies for narcotics, PCP, and cocaine were negative. Therefore, a correlation between PCP and rhabdomyolysis associated with acute psychotic and violent behavior could not be made with certainty. The etiology and pathogenesis of rhabdomyolysis are discussed in depth.
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PMID:Rhabdomyolysis following violent behavior and coma. 357 46

The effect of trifluoperazine (TFP) and phencyclidine (PCP) on acetylcholine receptor (AChR) function was studied in rat myotubes differentiated in vitro. While both drugs exerted an inhibitory effect on carbamylcholine (CCh)-induced Na+ or Ca2+ flux (I50 = 5-9 microM), alpha-bungarotoxin (alpha-Bgt) binding was not affected. The inhibitory effect of both drugs was independent of CCh concentration. The mutual inhibitory effect of TFP and PCP on Ca2+ influx was analyzed using three alternative models of interaction between the two drugs: competitive, additive and synergistic inhibition models. Our results are in accord with a synergistic interaction between the drugs probably not through desensitization. This synergistic interaction between the drugs provides a biochemical rationale to the phenothiazine contraindication in the treatment of PCP psychosis.
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PMID:Synergistic inhibition by trifluoperazine and phencyclidine of carbamylcholine-induced cation influx in muscle cultures. 360 41


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