keyword
MENU ▼
Read by QxMD icon Read
search

phencyclidine

keyword
https://www.readbyqxmd.com/read/29324345/synthesis-and-biological-evaluation-of-a-series-of-multi-target-n-substituted-cyclic-imide-derivatives-with-potential-antipsychotic-effect
#1
Mingshuo Xu, Yu Wang, Feipu Yang, Chunhui Wu, Zhen Wang, Bin Ye, Xiangrui Jiang, Qingjie Zhao, Jianfeng Li, Yongjian Liu, Junchi Zhang, Guanghui Tian, Yang He, Jingshan Shen, Hualiang Jiang
In the present study, a series of multi-target N-substituted cyclic imide derivatives which possessed potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties were synthesized and evaluated as potential antipsychotics. Among these compounds, (3aR,4R,7S,7aS)-2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione hydrochloride (3d) held a promising pharmacological profile. 3d not only showed potent and balanced in vitro activities on D2/5-HT1A/5-HT2A receptors, but also endowed with low to moderate activities on 5-HT2C, H1, α1A, M3 receptors and hERG channel, suggesting a low liability to induce side effects such as weight gain, orthostatic hypotension and QT prolongation...
January 4, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29309433/association-studies-of-wd-repeat-domain-3-and-chitobiosyldiphosphodolichol-beta-mannosyltransferase-genes-with-schizophrenia-in-a-japanese-population
#2
Momoko Kobayashi, Daisuke Jitoku, Yoshimi Iwayama, Naoki Yamamoto, Tomoko Toyota, Katsuaki Suzuki, Mitsuru Kikuchi, Tasuku Hashimoto, Nobuhisa Kanahara, Akeo Kurumaji, Takeo Yoshikawa, Toru Nishikawa
Schizophrenia and schizophrenia-like symptoms induced by the dopamine agonists and N-methyl-D aspartate type glutamate receptor antagonists occur only after the adolescent period. Similarly, animal models of schizophrenia by these drugs are also induced after the critical period around postnatal week three. Based upon the development-dependent onsets of these psychotomimetic effects, by using a DNA microarray technique, we identified the WD repeat domain 3 (WDR3) and chitobiosyldiphosphodolichol beta-mannosyltransferase (ALG1) genes as novel candidates for schizophrenia-related molecules, whose mRNAs were up-regulated in the adult (postnatal week seven), but not in the infant (postnatal week one) rats by an indirect dopamine agonist, and phencyclidine, an antagonist of the NMDA receptor...
2018: PloS One
https://www.readbyqxmd.com/read/29296031/dextromethorphan-in-cough-syrup-the-poor-man-s-psychosis
#3
Bridgette Martinak, Ramy A Bolis, Jeffrey Ryne Black, Rachel E Fargason, Badari Birur
Dextromethorphan (3-methoxy-N-methylmorphinan), also known as "DXM" and "the poor man's PCP," is a synthetically produced drug that is available in more than 140 over-the-counter cough and cold preparations. Dextromethorphan (DXM) has overtaken codeine as the most widely used cough suppressant due to its availability, efficacy, and safety profile at directed doses. However, DXM is subject to abuse. When consumed at inappropriately high doses (over 1500 mg/day), DXM can induce a state of psychosis characterized by Phencyclidine (PCP)-like psychological symptoms, including delusions, hallucinations, and paranoia...
September 15, 2017: Psychopharmacology Bulletin
https://www.readbyqxmd.com/read/29291439/novel-non-sulfonamide-5-ht6-receptor-partial-inverse-agonist-in-a-group-of-imidazo-4-5-b-pyridines-with-cognition-enhancing-properties
#4
David Vanda, Miroslav Soural, Vittorio Canale, Séverine Chaumont-Dubel, Grzegorz Satała, Tomasz Kos, Petr Funk, Veronika Fülöpová, Barbora Lemrová, Paulina Koczurkiewicz, Elżbieta Pękala, Andrzej J Bojarski, Piotr Popik, Philippe Marin, Paweł Zajdel
A small library of novel 3H-imidazo[4,5-b]pyridine and 1H-imidazo[4,5-c]pyridine derivatives was designed and synthesized as non-sulfonamide 5-HT6 receptor ligands. In vitro evaluation allowed to identify compound 17 (2-ethyl-3-(3-fluorobenzyl)-7-(piperazin-1-yl)-3H-imidazo[4,5-b]pyridine) as potent 5-HT6 receptor partial inverse agonist in Gs signaling (Ki = 6 nM, IC50 = 17.6 nM). Compound 17 displayed high metabolic stability, favorable cytochrome P450 isoenzyme (2D6, 3A4) profile, did not affect PgP-protein binding, without evoking mutagenic effects...
December 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29289597/hippocampal-gabaa-antagonism-reverses-the-novel-object-recognition-deficit-in-sub-chronic-phencyclidine-treated-rats
#5
Nichole M Neugebauer, Masanori Miyauchi, Tatsuya Sato, Jun Tadano, Hanife Akal, Hossein Ardehali, Herbert Y Meltzer
BACKGROUND: Abnormalities in prefrontal cortical and hippocampal GABAergic function are postulated to be major causes of the cognitive impairment associated with schizophrenia (CIAS). There are conflicting views on whether diminished or enhanced GABAergic activity contributes to the deficit in short-term novel object recognition (NOR) in the sub-chronic phencyclidine (scPCP) rodent model of CIAS. This study assessed the role of GABAA signaling in the medial prefrontal cortex (mPFC) and ventral hippocampus (vHPC) in NOR in saline (scSAL)- and scPCP-treated rats...
December 28, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29278697/downregulation-of-5-hydroxytryptamine7-receptor-in-the-medial-prefrontal-cortex-ameliorates-impulsive-actions-in-animal-models-of-schizophrenia
#6
Junhui Liu, Wei Zhang, Jinteng Feng, Min Jia, Guangjian Zhang, Xiaopeng Wen
5-hydroxytryptamine7 (5-HT7) receptors in the medial prefrontal cortex (mPFC) play a critical role in complex cognitive impairment in schizophrenia. The mouse model of schizophrenia was established through the neonatal administration of phencyclidine (nPCP). Recombinant adeno-associated virus-mediated gene knockdown was used to investigate the role of mPFC 5-HT7 receptor in the schizophrenia-like symptoms in mice. Under baseline conditions in the 5-choice serial reaction time task (5-CSRTT), nPCP produced a significant attentional impairment that was exacerbated when mice were tested under LITI...
December 23, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29244082/quantitation-of-cocaine-and-metabolites-phencyclidine-butalbital-and-phenobarbital-in-meconium-by-liquid-chromatography-tandem-mass-spectrometry
#7
Triniti L Scroggin, Gwendolyn A McMillin
In this study, a quantitative polarity switching liquid chromatography coupled with a tandem mass spectrometer (LC-MS/MS) method was developed to detect and quantify cocaine and metabolites (cocaethylene, benzoylecgonine and meta-hydroxybenzoylecgonine), phencyclidine (PCP) and barbiturates (phenobarbital and butalbital) in meconium. Accuracy and precision samples at 0.0125% and 75% of the upper limit of quantitation (ULOQ) were analyzed in triplicate over 5 days with accuracy above 84% and average %CV values below 11%...
December 13, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29225006/mechanistic-studies-on-ketamine-induced-mitochondrial-toxicity-in-zebrafish-embryos
#8
Bonnie L Robinson, Melanie Dumas, Syed F Ali, Merle G Paule, Qiang Gu, Jyotshna Kanungo
Ketamine, a phencyclidine derivative, is an antagonist of the Ca2+-permeable N-methyl-d-aspartate (NMDA)-type glutamate receptors. It is a pediatric anesthetic and has been implicated in developmental neurotoxicity. Ketamine has also been shown to deplete ATP in mammalian cells. Our previous studies showed that acetyl l-carnitine (ALCAR) prevented ketamine-induced cardiotoxicity and neurotoxicity in zebrafish embryos. Based on our finding that ALCAR's protective effect was blunted by oligomycin A, an inhibitor of ATP synthase, we further investigated the effects of ketamine and ALCAR on ATP levels, mitochondria and ATP synthase in zebrafish embryos...
December 7, 2017: Neurotoxicology and Teratology
https://www.readbyqxmd.com/read/29205946/surveillance-of-drug-abuse-in-hong-kong-by-hair-analysis-using-lc-ms-ms
#9
K Wing Leung, Zack C F Wong, Janet Y M Ho, Ada W S Yip, Jerry K H Cheung, Karen K L Ho, Ran Duan, Karl W K Tsim
The aim of this study is to reveal the habits of drug abusers in hair samples from drug rehabilitation units in Hong Kong. With the application of LC-MS/MS technology, a total of 1,771 hair samples were analyzed during the period (Jan 2012 to Mar 2016) of hair testing service provided to fourteen drug rehabilitation units including non-governmental organizations (NGOs), rehabilitation centers and medical clinics. Hair samples were analyzed for abused drugs and their metabolites simultaneously, including ketamine, norketamine, cocaine, benzoylecgonine, cocaethylene, norcocaine, codeine, MDMA, MDA, MDEA, amphetamine, methamphetamine, morphine, 6-acetylmorphine, phencyclidine and methadone...
December 4, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29196183/nmda-receptor-antagonist-rodent-models-for-cognition-in-schizophrenia-and-identification-of-novel-drug-treatments-an-update
#10
REVIEW
Daniela Cadinu, Ben Grayson, Giovanni Podda, Michael K Harte, Nazanin Doostdar, Joanna C Neill
Negative and cognitive deficit symptoms in schizophrenia remain an unmet clinical need. Improved understanding of the neuro- and psychopathology of cognitive dysfunction in the illness is urgently required to enhance the development of new improved therapeutic strategies. Careful validation of animal models that mimic the behaviour and pathology of complex psychiatric disorders is an essential step towards this goal. Non-competitive NMDAR (N-Methyl-d-aspartate receptor) antagonists e.g. phencyclidine (PCP), ketamine and dizocilpine (MK-801) can effectively replicate certain aspects of negative and cognitive deficits associated with schizophrenia in animals...
November 28, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29187755/a-mouse-model-of-the-schizophrenia-associated-1q21-1-microdeletion-syndrome-exhibits-altered-mesolimbic-dopamine-transmission
#11
Jacob Nielsen, Kim Fejgin, Florence Sotty, Vibeke Nielsen, Arne Mørk, Claus T Christoffersen, Leonid Yavich, Jes B Lauridsen, Dorte Clausen, Peter H Larsen, Jan Egebjerg, Thomas M Werge, Pekka Kallunki, Kenneth V Christensen, Michael Didriksen
1q21.1 hemizygous microdeletion is a copy number variant leading to eightfold increased risk of schizophrenia. In order to investigate biological alterations induced by this microdeletion, we generated a novel mouse model (Df(h1q21)/+) and characterized it in a broad test battery focusing on schizophrenia-related assays. Df(h1q21)/+ mice displayed increased hyperactivity in response to amphetamine challenge and increased sensitivity to the disruptive effects of amphetamine and phencyclidine hydrochloride (PCP) on prepulse inhibition...
November 30, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/29186585/fatality-following-ingestion-of-tetrahydrofuranylfentanyl-u-49900-and-methoxy-phencyclidine
#12
Alex J Krotulski, Donna M Papsun, Melissa Friscia, Jennifer L Swartz, Brian D Holsey, Barry K Logan
Novel psychoactive substances (NPS), and specifically novel opioids, continue to cause adverse events, including death, within drug-using populations. As the number of opioid-related overdoses continues to increase, laboratories have identified the emergence of new fentanyl analogues and other synthetic opioid-related drugs. Tetrahydrofuranylfentanyl (THFF) has been identified in Europe and the United States as an emerging novel opioid, causing death in at least 15 drug-using individuals to date. THFF is structurally similar to furanylfentanyl, a previously characterized novel opioid responsible for numerous adverse events, including death...
November 24, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29186455/recommendations-for-toxicological-investigation-of-drug-impaired-driving-and-motor-vehicle-fatalities-2017-update
#13
Barry K Logan, Amanda L D'Orazio, Amanda L A Mohr, Jennifer F Limoges, Amy K Miles, Colleen E Scarneo, Sarah Kerrigan, Laura J Liddicoat, Karen S Scott, Marilyn A Huestis
This report describes the outcomes of a process undertaken to review and update the National Safety Council's Alcohol, Drugs and Impairment Division's recommendations for the toxicological investigation of suspected alcohol and drug-impaired driving cases and motor vehicle fatalities. The updates to the recommendations are made based on a survey of practices in laboratories in the USA and Canada performing testing in these cases, consideration of existing epidemiological crash and arrest data, current drug use patterns, and practical considerations of widely available technology platforms in laboratories performing this work...
November 23, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29175446/phencyclidine-increased-while-isolation-rearing-did-not-affect-progressive-ratio-responding-in-rats-investigating-potential-models-of-amotivation-in-schizophrenia
#14
Nurith Amitai, Susan B Powell, Jared W Young
BACKGROUND: Schizophrenia is a debilitating neurodevelopmental disorder affecting 1% of the global population with heterogeneous symptoms including positive, negative, and cognitive. While treatment for positive symptoms exists, none have been developed to treat negative symptoms. Animal models of schizophrenia are required to test targeted treatments and since patients exhibit reduced effort (breakpoints) for reward in a progressive ratio (PR) task, we examined the PR breakpoints of rats treated with the NMDA receptor antagonist phencyclidine or those reared in isolation - two common manipulations used to induce schizophrenia-relevant behaviors in rodents...
November 22, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29170178/false-positive-phencyclidine-pcp-on-urine-drug-screen-attributed-to-desvenlafaxine-pristiq-use
#15
T Michael Farley, Emily N Anderson, Jade N Feller
We report a likely false-positive phencyclidine (PCP) result detected with a urine drug screen (UDS) (Medtox, St Paul, Minnesota, USA) in the setting of therapeutic desvenlafaxine (Pristiq) use. Desvenlafaxine (O-desmethylvenlafaxine) is the active metabolite of venlafaxine (Effexor). Prior reports have confirmed venlafaxine use resulting in a false-positive for PCP on a UDS. However, there has been a paucity of reporting of commercially available desvenlafaxine formulations (Pristiq, Khedezla) resulting in false-positives for PCP on a UDS...
November 23, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/29128144/the-antipsychotic-drug-brexpiprazole-reverses-phencyclidine-induced-disruptions-of-thalamocortical-networks
#16
Hanna E van den Munkhof, Jørn Arnt, Pau Celada, Francesc Artigas
Brexpiprazole (BREX), a recently approved antipsychotic drug in the US and Canada, improves cognitive dysfunction in animal models, by still largely unknown mechanisms. BREX is a partial agonist at 5-HT1A and D2 receptors and antagonist at α1B- and α2C-adrenergic and 5-HT2A receptors all with a similar potency. The NMDA receptor antagonist phencyclidine (PCP), used as pharmacological model of schizophrenia, activates thalamocortical networks and decreases low frequency oscillations (LFO; <4 Hz). These effects are reversed by antipsychotics...
November 8, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29122692/blockade-of-platelet-activating-factor-receptor-attenuates-abnormal-behaviors-induced-by-phencyclidine-in-mice-through-down-regulation-of-nf-%C3%AE%C2%BAb
#17
The-Vinh Tran, Se Jin Park, Eun-Joo Shin, Hai-Quyen Tran, Ji Hoon Jeong, Choon-Gon Jang, Yu Jeung Lee, Seung-Yeol Nah, Toshitaka Nabeshima, Hyoung-Chun Kim
Accumulating evidence suggests that neuroinflammation is one of the important etiologic factors of abusive and neuropsychiatric disorders. Platelet-activating factor (PAF) is potent proinflammatory lipid mediat1or and plays a pivotal role in neuroinflammatory disorders through the specific PAF receptor (PAF-R). Phencyclidine (PCP) induces a psychotomimetic state that closely resembles schizophrenia. Here, we investigated the role of PAF-R in the abnormal behaviors induced by PCP in mice. Repeated treatment with PCP resulted in a significant increase in PAF-R gene expression in the prefrontal cortex (PFC) and in the hippocampus...
November 7, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/29118102/phencyclidine-discoordinates-hippocampal-network-activity-but-not-place-fields
#18
Hsin-Yi Kao, Dino Dvořák, EunHye Park, Jana Kenney, Eduard Kelemen, André A Fenton
We used the psychotomimetic phencyclidine (PCP) to investigate the relationships between cognitive behavior, coordinated neural network function and information processing within the hippocampus place cell system. We report in rats that PCP (5mg/kg i.p.) impairs a well-learned hippocampus-dependent place avoidance behavior in rats that requires cognitive control, even when PCP is injected directly into dorsal hippocampus. PCP increases 60-100 Hz medium gamma oscillations in hippocampus CA1 and these increases correlate with the cognitive impairment caused by systemic PCP administration...
November 8, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29082316/the-use-of-cannabis-by-patients-with-sickle-cell-disease-increased-the-frequency-of-hospitalization-due-to-vaso-occlusive-crises
#19
Samir K Ballas
Introduction: The objective of this study was to determine if patients with sickle cell disease using cannabis had decreased frequency of acute vaso-occlusive crises (VOCs) that required hospitalization. Method: This was a retrospective study in which 270 urine drug screen tests were done on 72 patients: 40 males and 32 females. Results: Cannabinoids were found in 144 urine tests from 37 patients and were negative in 126 tests from 35 patients. Males who used cannabis were significantly younger (p<0.001) than males who did not...
2017: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/29076977/multiple-actions-of-phencyclidine-and-mk-801-on-isolated-bovine-cerebral-arteries
#20
Woodrow W Wendling, Dong Chen, Karen S Wendling, Ihab R Kamel
This study examines the direct effects of 3 noncompetitive N-methyl-D-aspartate receptor antagonists, phencyclidine (PCP), (+)MK-801, and (-)MK-801, on bovine middle cerebral arteries (BMCA). Rings of BMCA were mounted in isolated tissue chambers equipped with isometric tension transducers to obtain pharmacologic dose-response curves. In the absence of endogenous vasoconstrictors, the 3 N-methyl-D-aspartate antagonists each produced direct constriction of BMCA. The thromboxane A2 receptor antagonist SQ-29,548, the TxA2 synthase inhibitor furegrelate, the calcium antagonist nimodipine, and calcium-deficient media all inhibited maximal phencyclidine or (+)MK-801-induced constriction...
October 25, 2017: Journal of Neurosurgical Anesthesiology
keyword
keyword
9459
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"