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)

The effects of phencyclidine on aggressive behavior in mice and the possible mechanism of action for these effects were examined. PCP at a dose of 10.0 mg/kg significantly decreased the number of attacks by resident mice toward intruders. Significant increases in the number of attacks by non-drugged residents toward the intruders who were given high doses of PCP (6.0 and 10.0 mg/kg) were observed. Only the higher doses of PCP (6.0 and 10.0 mg/kg) significantly increased the duration of locomotion. The increase in locomotion was dependent upon the time after administration of the drug. Hyperactivity was present at 30 minutes for both doses and hypoactivity was present at three hours after administration of 3.0 mg/kg. PCP did not significantly alter the frequency of attacks in an unfamiliar test locale. Pretreatment with haloperidol (1 mg/kg) partially blocked the PCP-induced hyperactivity but pretreatment with methysergide (3 mg/kg) did not. Neither haloperidol nor methysergide blocked the suppressive effects of PCP on aggressive behavior. It is concluded that PCP does not increase aggressive behavior in mice but high doses will decrease aggression. PCP-treated intruder animals provoke more aggression by non-drugged animals. PCP-induced hyperactivity appears to be mediated by dopaminergic systems.
Pharmacol Biochem Behav 1982 Sep
PMID:Effects of phencyclidine on aggressive behavior in mice. 689 Jun 86

To test the sensitivity and specificity of hemodynamic criteria for acute right ventricular infarction (RVI), two groups of patients with anatomically proved acute myocardial infarction and hemodynamic monitoring were studied. Group A included 22 patients acute RVI and group B, 38 with infarction confined to the left ventricle. In both groups, the closest relation between right atrial and pulmonary capillary pressures (RAP and PCP), as well as the presence of a severe noncompliant pattern (SNCP), were studied. A SNCP was defined as a y descent deeper than the x descent in RAP. RAP was equal to or higher than PCP in 10 patients from group A and in none from group B. In group B, a significant relation was found between RAP and PCP (r = 0.777, y = 0.43x + 0.18) (p less than 0.05), and the 95% confidence limits could be calculated. Above these limits, a closer relation between RAP and PCP was only found in patients with RVI. However, six patients with RVI showed an RAP/PCP relation within 95% confidence limits of group B (sensitivity 72.7%, specificity 100%). A SNCP was present in 12 patients with RVI and only in one without RVI (p less than 0.01) (sensitivity 54.5% and specificity 97.4%). When either criterion is present (close relation between RAP and PCP or SNCP), a high sensitivity (81.8%) and specificity (97.4%) can be achieved in the diagnosis of acute RVI.
Circulation 1981 Sep
PMID:Sensitivity and specificity of hemodynamic criteria in the diagnosis of acute right ventricular infarction. 726 Dec 84

By utilizing a glass capillary gas chromatographic nitrogen detector (GC2-N) method specific for phencyclidine (PCP) and sensitive to pg/mL in blood or urine samples, we have demonstrated occupational intoxication of law enforcement personnel charged with handling confiscated illegal PCP preparations. Further, we have demonstrated persistence of PCP in blood and urine for at least 6 months after the last known occupational exposure in one officer. Some aspects of the PCP problem are outlined, and possible mechanisms of the occupational intoxication are discussed.
Clin Toxicol 1981 Sep
PMID:Occupational intoxication and long-term persistence of phencyclidine (PCP) in law enforcement personnel. 731 86

Seventeen different compounds having structural similarities o PCP (phencyclidine) were analyzed by radioimmunoassay (RIA) using 125I-phencyclidine reagents (Roche). Affinities were compared with molecular structures and several observations were made. It was found that the three-ring structure (1-phenylcyclo-hexylpiperidine) is essential for reactivity. Changes in and to the cyclohexyl ring and/or the piperidine ring reduced reactivity, while changes in the phenyl ring increased reactivity.
Clin Toxicol 1981 Sep
PMID:Phencyclidine (PCP)-structure versus reactivity. 731 89

ATP and ADP stimulated the release of specific prostaglandin products from the perfused rabbit kidney heart. The two nucleotides produced the same qualitative profile of prostaglandin products. In kidney, prostaglandin E2 was the major product, whereas in heart 6-keto prostaglandin F1 alpha and prostaglandin E2 predominated. ATP was a slightly more potent than ADP. ATP administered into the perfused heart to kidney was rapidly hydrolyzed to ADP and AMP. The prostaglandin E2 generating activity of ATP was increased 6-10 fold when ATP was given together with AMP-PCP or AMP-PNP which competitively inhibit the activity of vascular ATPase. Thus, the rapid hydrolysis of ATP reduces its agonistic activity for prostaglandin release. ATP and ADP administered together at maximal stimulating doses produced an additive response for prostaglandin E2 release. These results and the results of tachyphylaxis experiments indicate that ATP and ADP interact independently with different types of purinergic receptors.
Eur J Pharmacol 1981 Sep 11
PMID:Evidence for different purinergic receptors for ATP and ADP in rabbit kidney and heart. 732 99

Because AIDS patients frequently present with minimal symptomatology, radionuclide imaging with its ability to survey the entire body, is especially valuable. Gallium-67 citrate, the most commonly performed radionuclide study for localizing infection in these patients, is most useful for detecting opportunistic infections, especially in the thorax. A negative gallium scan, particularly when the chest X-ray is unremarkable, rules strongly against pulmonary disease. A negative gallium scan in a patient with an abnormal chest X-ray and Kaposi's sarcoma, suggests that the patient's respiratory distress is related to the neoplasm. Diffuse pulmonary parenchymal uptake of gallium in the HIV (+) patient is most often associated with PCP. While there are other causes of diffuse pulmonary uptake, the more intense or heterogeneous the uptake, the more likely the patient is to have PCP. Focal pulmonary uptake is usually associated with bacterial pneumonia although PCP may occasionally present in this fashion. Lymph node uptake of gallium is usually associated with Mycobacterium avium complex, tuberculosis, or lymphoma. When corresponding abnormalities are present on thallium scintigraphy lymphoma is likely. Gallium positive, thallium negative, studies suggest mycobacterial disease. Labeled leukocyte imaging is not useful for detecting opportunistic infections probably because of the inflammatory response incited by these organisms. Leukocyte imaging is, however, more sensitive for detecting bacterial pneumonia. In the abdomen, gallium imaging is most useful for identifying lymphadenopathy, while labeled leukocyte imaging is superior for detecting AIDS-associated colitides. In summary, radionuclide studies are valuable diagnostic modalities in AIDS. Their success can be maximized by tailoring the study to the individual's needs.
Q J Nucl Med 1995 Sep
PMID:The role of gallium and labeled leukocyte scintigraphy in the AIDS patient. 755 45

The anticonvulsant effects of 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(f)quinoxaline (NBQX), phencyclidine (PCP) and diazepam against audiogenic seizures in DBA/2 mice and against seizures induced by methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM) in NMRI mice were compared. Motor impairment was assessed in a rotarod apparatus in DBA/2 as well as NMRI mice. At 30 min after i.p. administration, NBQX was as effective as PCP and diazepam in protecting against audiogenic seizures and had a therapeutic ratio slightly higher than diazepam's and 7-fold higher than PCP's. Whereas diazepam was fully effective, NBQX and PCP were both ineffective against seizures induced by DMCM 30 min after i.p. administration. The anticonvulsant potential and motor-impairing effects of NBQX were evaluated further by the i.p. and the i.v. routes at different time points after administration. At all pretreatment intervals, NBQX protected against audiogenic seizures more potently than it produced motor impairment. NBQX administered i.p. protected against DMCM-induced seizures when given 15 min but not 5 min before testing, whereas after i.v. administration NBQX produced anticonvulsant and motor-impairing effects in the same dose range. NBQX only slightly and non-dose-dependently attenuated the discriminative effects of pentylenetetrazole in rats, showing a limited anxiolytic potential. NBQX produced no PCP-like or morphine-like discriminative effects in rats, suggesting lack of PCP or opiate-like subjective effects. These data demonstrate that NBQX has anticonvulsant effects, has limited anxiolytic effects, and does not produce subjective effects of PCP or opiate type.
J Pharmacol Exp Ther 1995 Sep
PMID:Anticonvulsant, anxiolytic and discriminative effects of the AMPA antagonist 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(f)quinoxaline (NBQX). 756 77

A series of permanently charged benzo[b]quinolizinium cations having lower lipophilicity than MK-801 or phencyclidine (PCP) were synthesized. Data relating agonist independent block of N-methyl-D-aspartic acid (NMDA) ion channels to log D are described. Closed channel access is predicted to result in a more noncompetitive profile of antagonism compared to selective open channel blockers, which are uncompetitive inhibitors. Reduced closed channel block may underlie the absence of PCP or MK-801-like behavioral side effects observed for benzo[b]-quinolizinium cations.
J Med Chem 1995 Sep 01
PMID:Novel benzo[b]quinolizinium cations as uncompetitive N-methyl-D-aspartic acid (NMDA) antagonists: the relationship between log D and agonist independent (closed) NMDA channel block. 765 45

Capsaicin in the adult animal causes antinociception due to the massive release of neurotransmitters, including substance P (SP), from primary afferent C-fibers. The results of the present study indicate that capsaicin-induced antinociception in the adult is sensitive to inhibition by dizocilpine (MK-801). The failure of a high dose (10 nmoles) of (+-)-3-(2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid (CPP) to mimic the effect of MK-801 (1 nmole) on antinociception induced by 0.8 micrograms of capsaicin suggests that the inhibition by MK-801 is mediated by a phencyclidine (PCP) site but is not associated with NMDA activity. The inability of haloperidol (1 nmole) to affect the actions of capsaicin argues against an interaction with sigma sites. Behavioral sensitization to intrathecally administered kainic acid (KA) has been proposed to reflect similar neuronal activity to that underlying pain transmission. KA sensitization is inhibited by pretreatment with capsaicin (0.8 microgram) or SP(1-7) (10 nmoles) and the influence of MK-801, CPP and haloperidol on these inhibitory effects of capsaicin and SP(1-7) were identical to those on capsaicin-induced antinociception. These data are consistent with the hypothesis that the antinociceptive effect of capsaicin in the adult is similar to that of the N-terminus of SP, both of which involve a pathway sensitive to MK-801 but not mediated by NMDA-type activity.
Neuroreport 1993 Sep 03
PMID:MK-801 inhibits the effects of capsaicin in the adult mouse by an action involving phencyclidine (PCP) sites not linked to NMDA activity. 769 10

Behavioral responses to kainic acid (KA) injected intrathecally in mice are enhanced by N-but not C-terminal fragments of substance P (SP). Repeated injections of KA result in sensitization to KA-induced activity, an effect that appears to be mediated by SP N-terminal activity and inhibited by PCP ligands. The present study was initiated to determine whether the ability of SP N-terminal fragments to enhance KA activity is also sensitive to PCP ligands. We compared the effect of a PCP ligand, dizocilpine (MK-801), to that of haloperidol, a sigma ligand and dopamine antagonist. MK-801 (1 nmol) failed to alter the enhancement of behavioral responses to KA (25 pmol) produced by SP(1-7) (22.5 pmol, 30 min). However, pretreatment with 1 nmol of either haloperidol or the N-terminal SP antagonist, [D-Pro2-D-Phe7]SP(1-7) [D-SP(1-7)], prevented potentiation of KA by SP(1-7). Like SP(1-7), 5 nmol of the sigma ligand 1,3-di(2-tolyl)guanidine (DTG) also enhanced behaviors elicited by KA, and this effect was also blocked by haloperidol or D-SP(1-7), but not spiperone (2.5 nmol), a dopamine antagonist. Together these data suggest that sigma receptors are involved in the potentiation of KA. A large dose of SP(1-7) (10 nmol) or DTG (20 nmol) did not alter the response to KA 24 hr later, yet further potentiated responses to KA 30 min after SP(1-7) (22.5 pmol) or DTG (5 nmol), suggesting sensitization to the effects of these compounds.(ABSTRACT TRUNCATED AT 250 WORDS)
Neuropharmacology 1993 Sep
PMID:Regulation of sigma activity by the amino-terminus of substance P in the mouse spinal cord: involvement of phencyclidine (PCP) sites not linked to N-methyl-D-aspartate (NMDA) activity. 769 72


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