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Article ; Online: Oral r-(-)-11-o-valeryl-n-n-propylnoraporphine reverses motor deficits in mptp-treated marmosets.

Lincoln, Louise / Fisher, Ria / Jackson, Michael J / Jenner, Peter / Neumeyer, John / Sromek, Anna W / Lees, Andrew J / Rose, Sarah

Movement disorders : official journal of the Movement Disorder Society

2016 Volume 31, Issue 9, Page(s) 1381–1388

Abstract: ... the need for parenteral administration. We now describe the effects of the orally active compound R-(-)-11 ... O-valeryl-N-n-propylnoraporphine (11-OH-NPa valerate) on reversal of motor disability and expression ...

Abstract	Background: The D1/D2 dopamine agonist apomorphine has poor oral bioavailability, necessitating subcutaneous administration in the treatment of Parkinson's disease (PD). Acute subcutaneous injection is used as rescue therapy from "off" periods, whereas continuous subcutaneous infusion is used to increase "on" periods and to reduce dyskinesia when oral treatment fails. An orally active derivative of apomorphine would avoid the need for parenteral administration. We now describe the effects of the orally active compound R-(-)-11-O-valeryl-N-n-propylnoraporphine (11-OH-NPa valerate) on reversal of motor disability and expression of dyskinesia in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated, l-dopa-primed dyskinetic common marmosets. Methods: Locomotor activity, motor disability, and dyskinesia were assessed in MPTP-treated marmosets following the administration of apomorphine (0.075 mg/kg, subcutaneous and 0.28 to 1.12 mg/kg, oral) and 11-OH-NPa valerate (0.19, 0.38, and 0.75mg/kg, oral). Results: Subcutaneous administration of apomorphine (0.075 mg/kg) produced a short-lasting reversal of motor disability and the expression of established dyskinesia, but when administered orally (0.28-1.12 mg/kg) it had no effect. In contrast, oral treatment with 11-OH-NPa valerate (0.19 and 0.75 mg/kg) induced a dose-related reversal of motor disability and increased locomotor activity with only mild to moderate dyskinesia. Only at the highest dose (0.75 mg/kg) was marked dyskinesia seen accompanying an extended period of motor disability reversal and increased locomotor activity. Conclusion: Oral administration of 11-OH-NPa valerate produced a rapid reversal of motor disability and, at effective dose levels, had a limited propensity to induce dyskinesia. 11-OH-NPa valerate is the first orally active derivative of apomorphine with potential for use in PD. © 2016 International Parkinson and Movement Disorder Society.
Language	English
Publishing date	2016-09
Publishing country	United States
Document type	Journal Article ; Review
ZDB-ID	607633-6
ISSN	1531-8257 ; 0885-3185
ISSN (online)	1531-8257
ISSN	0885-3185
DOI	10.1002/mds.26626
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Article ; Online: Evaluating the invariance of the factor structure of the EPQ-R-N among adolescents.

Mor, Nilly / Zinbarg, Richard E / Craske, Michelle G / Mineka, Susan / Uliaszek, Amanda / Rose, Raphael / Griffith, James W / Waters, Allison M

Journal of personality assessment

2008 Volume 90, Issue 1, Page(s) 66–75

Abstract: ... EPQ-R-N; S. B. G. Eysenck, Eysenck & Barrett, 1985) and its factor invariance across sex and racial ... model to previous models of the EPQ-R-N and to single-factor and 3-factor structures. The hierarchical ... of the variance in EPQ-R-N total scores and was invariant across sex and ethnicity. The 3 group factors varied ...

Abstract	We examined the factor structure of the Neuroticism scale of the Eysenck Personality Questionnaire (EPQ-R-N; S. B. G. Eysenck, Eysenck & Barrett, 1985) and its factor invariance across sex and racial/ethnic groups in a sample of 1,979 adolescents. Using confirmatory factor analyses, we compared a hierarchical model to previous models of the EPQ-R-N and to single-factor and 3-factor structures. The hierarchical factor structure in which a general factor coexists with 3 group factors (depression, social concerns, and worry) was superior to alternative models. The general factor accounted for more than 60% of the variance in EPQ-R-N total scores and was invariant across sex and ethnicity. The 3 group factors varied across ethnicity and sex. We discuss the implications of these findings for conceptualization and assessment of neuroticism using the EPQ-R-N.
MeSH term(s)	Adolescent ; Adolescent Behavior/psychology ; Ethnic Groups/statistics & numerical data ; Factor Analysis, Statistical ; Humans ; Neurotic Disorders/diagnosis ; Neurotic Disorders/ethnology ; Personality Inventory/statistics & numerical data ; Psychometrics ; Reproducibility of Results ; Self Concept ; Surveys and Questionnaires
Language	English
Publishing date	2008-01
Publishing country	England
Document type	Comparative Study ; Evaluation Studies ; Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	121962-5
ISSN	1532-7752 ; 0022-3891
ISSN (online)	1532-7752
ISSN	0022-3891
DOI	10.1080/00223890701693777
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Article: High-dose and combination antipsychotic prescribing in acute adult wards in the UK: the challenges posed by p.r.n. prescribing.

Paton, Carol / Barnes, Thomas R E / Cavanagh, Mary-Rose / Taylor, David / Lelliott, Paul

The British journal of psychiatry : the journal of mental science

2008 Volume 192, Issue 6, Page(s) 435–439

Abstract: ... baseline 43%; re-audit 39%). As required ('p.r.n.') prescriptions were the principal cause of both high ... of p.r.n. prescribing. ...

Abstract	Background: Clinical guidelines recommend the routine use of a single antipsychotic drug in a standard dose, but prescriptions for high-dose and combined antipsychotics are common in clinical practice. Aims: To evaluate the effectiveness of a quality improvement programme in reducing the prevalence of high-dose and combined antipsychotic prescribing in acute adult in-patient wards in the UK. Method: Baseline audit was followed by feedback of benchmarked data and delivery of a range of bespoke change interventions, and then by a further audit 1 year later. Results: Thirty-two services participated, submitting data for 3,942 patients at baseline and 3,271 patients at the 1-year audit. There was little change in the prevalence of high-dose (baseline 36%; re-audit 34%) or combined antipsychotic prescribing (baseline 43%; re-audit 39%). As required ('p.r.n.') prescriptions were the principal cause of both high-dose and combined antipsychotic prescribing on both occasions. Conclusions: The quality improvement programme did not have a demonstrable impact on prescribing practice in the majority of services. Future efforts to align practice with clinical guidelines need to specifically target the culture and practice of p.r.n. prescribing.
MeSH term(s)	Adolescent ; Adult ; Aged ; Antipsychotic Agents/administration & dosage ; Drug Therapy, Combination ; Drug Utilization Review ; Female ; Guideline Adherence/standards ; Hospitals, Psychiatric/standards ; Humans ; Male ; Medical Audit ; Mental Disorders/drug therapy ; Middle Aged ; Practice Guidelines as Topic ; Regression Analysis ; State Medicine/standards ; United Kingdom
Chemical Substances	Antipsychotic Agents
Language	English
Publishing date	2008-06
Publishing country	England
Document type	Journal Article ; Multicenter Study ; Research Support, Non-U.S. Gov't
ZDB-ID	218103-4
ISSN	1472-1465 ; 0007-1250
ISSN (online)	1472-1465
ISSN	0007-1250
DOI	10.1192/bjp.bp.107.042895
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Article: Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.

Trivedi, B K / Padia, J K / Holmes, A / Rose, S / Wright, D S / Hinton, J P / Pritchard, M C / Eden, J M / Kneen, C / Webdale, L / Suman-Chauhan, N / Boden, P / Singh, L / Field, M J / Hill, D

Journal of medicinal chemistry

1998 Volume 41, Issue 1, Page(s) 38–45

Abstract: We have previously described the design and development of CI-988, a peptoid analogue of CCK-4 with excellent binding affinity and selectivity for the CCK-B receptor. Due to its anxiolytic profile in animal models of anxiety, this compound was developed ... ...

Abstract	We have previously described the design and development of CI-988, a peptoid analogue of CCK-4 with excellent binding affinity and selectivity for the CCK-B receptor. Due to its anxiolytic profile in animal models of anxiety, this compound was developed as a clinical candidate. However, during its development, it was determined that CI-988 had low bioavailability in both rodent and nonrodent species. In the clinic, it was further established that CI-988 had poor bioavailability. Thus, there was a need to identify an analogue with an improved pharmacokinetic (PK) profile. The poor bioavailability was attributed to poor absorption and efficient hepatic extraction. We envisaged that reducing the molecular weight of the parent compound (5, MW = 614) would lead to better absorption. Thus, we synthesized a series of analogues in which the key alpha-methyltryptophan and adamantyloxycarbonyl moieties, required for receptor binding, were kept intact and the C-terminus was extensively modified. This SAR study led to the identification of tricyclo[3.3.1.1(3,7)]dec-2-yl [1S-[1 alpha(S*)2 beta]-[2-[(2-hydroxycyclohexyl)amino]-1-(1H-indol-3- ylmethyl)-1-methyl-2-oxoethyl]carbamate (CI-1015, 31) with binding affinities of 3.0 and 2900 nM for the CCK-B and CCK-A receptors, respectively. The compound showed CCK-B antagonist profile in the rat ventromedial hypothalamus assay with a Ke of 34 nM. It also showed an anxiolytic like profile orally in a standard anxiety paradigm (X-maze) with a minimum effective dose (MED) of 0.1 microgram/kg. Although the compound is less water soluble than CI-988, oral bioavailability in rat was improved nearly 10 times relative to CI-988 when dosed in HP beta CD. The blood-brain permeability of CI-1015 (31) was also enhanced relative to CI-988 (5). On the basis of the overall improved pharmacokinetic profile as well as enhanced brain penetration, CI-1015 (31) was chosen as a development candidate.
MeSH term(s)	Adamantane/analogs & derivatives ; Adamantane/chemical synthesis ; Adamantane/chemistry ; Adamantane/pharmacokinetics ; Animals ; Anti-Anxiety Agents/chemical synthesis ; Anti-Anxiety Agents/chemistry ; Anti-Anxiety Agents/pharmacokinetics ; Anti-Anxiety Agents/pharmacology ; Biological Availability ; Blood-Brain Barrier ; Maze Learning/drug effects ; Mice ; Models, Molecular ; Molecular Structure ; Peptoids ; Rats ; Rats, Wistar ; Receptor, Cholecystokinin A ; Receptor, Cholecystokinin B ; Receptors, Cholecystokinin/antagonists & inhibitors ; Receptors, Cholecystokinin/metabolism ; Tetragastrin/analogs & derivatives ; Tryptophan/analogs & derivatives ; Tryptophan/chemical synthesis ; Tryptophan/chemistry ; Tryptophan/pharmacokinetics
Chemical Substances	Anti-Anxiety Agents ; Peptoids ; Receptor, Cholecystokinin A ; Receptor, Cholecystokinin B ; Receptors, Cholecystokinin ; Tetragastrin (0OL293AV80) ; CI 1015 (6RYQ64Z587) ; Tryptophan (8DUH1N11BX) ; Adamantane (PJY633525U)
Language	English
Publishing date	1998-01-01
Publishing country	United States
Document type	Comparative Study ; Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/jm970065l
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Zs.B 151: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular ab Jg. 2022: Lesesaal (EG)
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Article ; Online: First recorded presence of anthropogenic fly-ash particles in coral skeletons.

Roberts, L R / Kersting, D K / Zinke, J / Rose, N L

The Science of the total environment

2024 Volume 921, Page(s) 170665

Abstract: Fly-ash particles formed during industrial fossil-fuel combustion show a globally observed rapid increase in concentration within natural archives post-1950 and have been proposed as a marker for the Anthropocene Epoch. Here, we present the first record ... ...

Abstract	Fly-ash particles formed during industrial fossil-fuel combustion show a globally observed rapid increase in concentration within natural archives post-1950 and have been proposed as a marker for the Anthropocene Epoch. Here, we present the first record of fly-ash particles incorporated into coral skeletons. Particles are present in Mediterranean corals between CE 1957 and 1992 at concentrations of 8-30 g
MeSH term(s)	Animals ; Anthozoa/metabolism ; Coal Ash ; Plastics/metabolism ; Fossil Fuels ; Coal ; Coral Reefs
Chemical Substances	Coal Ash ; Plastics ; Fossil Fuels ; Coal
Language	English
Publishing date	2024-02-02
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	121506-1
ISSN	1879-1026 ; 0048-9697
ISSN (online)	1879-1026
ISSN	0048-9697
DOI	10.1016/j.scitotenv.2024.170665
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Article ; Online: Activation of TRPV4 channels promotes the loss of cellular ATP in organotypic slices of the mouse neocortex exposed to chemical ischemia.

Pape, Nils / Rose, Christine R

The Journal of physiology

2023 Volume 601, Issue 14, Page(s) 2975–2990

Abstract: The vertebrate brain has an exceptionally high energy need. During ischemia, intracellular ATP concentrations decline rapidly, resulting in the breakdown of ion gradients and cellular damage. Here, we employed the nanosensor ATeam1 ... ...

Abstract	The vertebrate brain has an exceptionally high energy need. During ischemia, intracellular ATP concentrations decline rapidly, resulting in the breakdown of ion gradients and cellular damage. Here, we employed the nanosensor ATeam1.03
MeSH term(s)	Mice ; Animals ; TRPV Cation Channels/metabolism ; Neocortex/metabolism ; Transient Receptor Potential Channels/metabolism ; Astrocytes/physiology ; Ischemia/metabolism ; Adenosine Triphosphate/metabolism
Chemical Substances	TRPV Cation Channels ; Transient Receptor Potential Channels ; Adenosine Triphosphate (8L70Q75FXE)
Language	English
Publishing date	2023-06-06
Publishing country	England
Document type	Journal Article
ZDB-ID	3115-x
ISSN	1469-7793 ; 0022-3751
ISSN (online)	1469-7793
ISSN	0022-3751
DOI	10.1113/JP284430
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Article: Fundamentals of blood banking in anesthesiology: A problem-based learning simulation session as an addition to a novel curriculum of transfusion medicine education for anesthesiology residents.

Kenfield, Meaghan R / Tannenbaum, Alex P / Hess, Aaron S / Rose, William N

Academic pathology

2023 Volume 10, Issue 3, Page(s) 100089

Abstract: We have previously published a novel transfusion medicine curriculum for first-year anesthesiology residents, making available open access learning materials. We now present a curriculum iteration, by incorporating resident feedback and developing an ... ...

Abstract	We have previously published a novel transfusion medicine curriculum for first-year anesthesiology residents, making available open access learning materials. We now present a curriculum iteration, by incorporating resident feedback and developing an additional "capstone" session for use at the end of the rotation that integrates several learning points into a practical problem-based simulation. This iteration of the curriculum was piloted with the 2019-2020 PGY-1 anesthesiology residents of the University of Wisconsin Hospitals and Clinics. Pre-course and post-course surveys, which assessed trainee understanding of course topics, were used to subjectively evaluate the usefulness of the curriculum. Results of the surveys demonstrated post-test mean scores were significantly increased when compared with the equivalent pre-course questions. This suggests the piloted curriculum iteration serves as a useful tool for resident learning. As an adjunct to our previous existing materials, in the spirit of open-access education, we share this additional curriculum material, consisting of four patient cases with 16 questions that can be used immediately for teaching purposes.
Language	English
Publishing date	2023-07-26
Publishing country	United States
Document type	Journal Article
ZDB-ID	2819382-9
ISSN	2374-2895
ISSN	2374-2895
DOI	10.1016/j.acpath.2023.100089
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Article ; Online: First evidence of industrial fly-ash in an Antarctic ice core.

Thomas, E R / Tetzner, D R / Roberts, S L / Turner, S D / Rose, N L

Scientific reports

2023 Volume 13, Issue 1, Page(s) 6529

Abstract: Spheroidal carbonaceous particles (SCPs) are a component of fly-ash, the particulate by-product of industrial high temperature combustion of fuel-oil and coal-series fuels. We provide the first evidence that these indelible markers of industrialisation ... ...

Abstract	Spheroidal carbonaceous particles (SCPs) are a component of fly-ash, the particulate by-product of industrial high temperature combustion of fuel-oil and coal-series fuels. We provide the first evidence that these indelible markers of industrialisation have been deposited in Antarctic ice, thousands of kilometres from any potential source. The earliest observed particle was deposited in an ice layer from 1936 CE. While depositional fluxes are low, chemical analysis of individual SCPs indicates a coal combustion origin.
Language	English
Publishing date	2023-04-21
Publishing country	England
Document type	Journal Article
ZDB-ID	2615211-3
ISSN	2045-2322 ; 2045-2322
ISSN (online)	2045-2322
ISSN	2045-2322
DOI	10.1038/s41598-023-33849-x
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Article: Intravascular squamous cell carcinoma treated with cemiplimab.

Rose, Alexander N / Yilmaz, Emrullah / Durkin, John R

JAAD case reports

2021 Volume 14, Page(s) 82–84

Language	English
Publishing date	2021-06-19
Publishing country	United States
Document type	Case Reports
ZDB-ID	2834220-3
ISSN	2352-5126
ISSN	2352-5126
DOI	10.1016/j.jdcr.2021.06.017
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Article ; Online: Growth with Commensal Streptococci Alters

Rose, M / Wilson, N / Williams, E / Letner, H / Bettinger, R / Bouchendouka, A / Batagower, J / Kaspar, J R

Journal of dental research

2023 Volume 102, Issue 4, Page(s) 450–458

Abstract: As oral bacteria grow and persist within biofilms attached to the tooth's surface, they interact with other species to form synergistic or antagonistic exchanges that govern homeostasis for the overall population. One example are the interactions between ...

Abstract	As oral bacteria grow and persist within biofilms attached to the tooth's surface, they interact with other species to form synergistic or antagonistic exchanges that govern homeostasis for the overall population. One example are the interactions between the cariogenic species
MeSH term(s)	Streptococcus mutans/genetics ; Streptococcus sanguis/physiology ; Streptococcus gordonii/metabolism ; Symbiosis ; Microbiota ; Biofilms
Language	English
Publishing date	2023-01-23
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural
ZDB-ID	80207-4
ISSN	1544-0591 ; 0022-0345
ISSN (online)	1544-0591
ISSN	0022-0345
DOI	10.1177/00220345221145906
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