Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction
…, DJ Begley, T Obradovic, IJ Hidalgo, S Coggon… - … of Pharmacology and …, 2007 - ASPET
… In this study, brain perfusions were performed over a 30-s period to ensure that the K in
values were determined on the linear region of the brain uptake curve. This also facilitated the …
values were determined on the linear region of the brain uptake curve. This also facilitated the …
New quinoline NK3 receptor antagonists with CNS activity
…, S Flynn, DM Bradley, R Porter, S Coggon… - Bioorganic & medicinal …, 2009 - Elsevier
… The (S)-cyclopropanated amines utilised in this work were prepared as shown in
Scheme 1. Reaction of the appropriate benzaldehyde with d-valinol generated chiral imine …
Scheme 1. Reaction of the appropriate benzaldehyde with d-valinol generated chiral imine …
SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino) ethyl]-N-[(4′-{[(2-phenylethyl) amino] methyl}-4-biphenylyl) methyl] propanamide dihydrochloride), a novel 5-ht5A …
…, LA Dawson, VA Fry, SA Coggon, S Faedo… - …, 2006 - Elsevier
… In the present study [ 35 S]GTPγS binding to guinea pig 5-ht 5A /HEK293 membranes
was characterised further using a number of 5-ht 5A receptor agonists and antagonists. The …
was characterised further using a number of 5-ht 5A receptor agonists and antagonists. The …
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry
…, SF Moss, SM Bromidge, SA Coggon… - Bioorganic & medicinal …, 2005 - Elsevier
… Compound 11b was further evaluated in a human 5-ht 5A receptor functional assay
utilising 5-carboxamidotryptamine (5-CT)-stimulated [ 35 S]GTPγS binding to cell membranes …
utilising 5-carboxamidotryptamine (5-CT)-stimulated [ 35 S]GTPγS binding to cell membranes …
[HTML][HTML] Data-driven Bayesian inference of turbulence model closure coefficients incorporating epistemic uncertainty
…, P Bekemeyer, S Görtz, S Coggon, S Sharma - Acta Mechanica …, 2021 - Springer
… For example, in this paper a turbulence model here is the negative S–A. This is the first
hypothesis in the statistical inference method. As this first hypothesis for example, other …
hypothesis in the statistical inference method. As this first hypothesis for example, other …
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder. Synthesis and activity of functionalized glutaramides
…, C Kohl, K Beaumont, S Coggon… - Journal of medicinal …, 2006 - ACS Publications
Female sexual arousal disorder (FSAD) is a highly prevalent sexual disorder affecting up to
40% of women. We describe herein our efforts to identify a selective neutral endopeptidase (…
40% of women. We describe herein our efforts to identify a selective neutral endopeptidase (…
An extended harmonic balance method based on incremental nonlinear control parameters
A new formulation for calculating the steady-state responses of multiple-degree-of-freedom (MDOF)
non-linear dynamic systems due to harmonic excitation is developed. This is aimed …
non-linear dynamic systems due to harmonic excitation is developed. This is aimed …
Efficient prediction and uncertainty propagation of correlated loads
I Tartaruga, P Sartor, JE Cooper, S Coggon… - 56th AIAA/ASCE/AHS …, 2015 - arc.aiaa.org
… ) (M) and the number of stations of interest (S). Thus, the dimensions of each matrix are (D)
x (… 𝑇 , whose dimensions are (K) x (N x M x S), where K is the number of singular values that …
x (… 𝑇 , whose dimensions are (K) x (N x M x S), where K is the number of singular values that …
Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist, NBI‐74330, using a murine CXCR3 internalization assay
…, GF Watt, S Fisher, H Birch, S Coggon… - British journal of …, 2007 - Wiley Online Library
Background and purpose: Pharmacokinetic/pharmacodynamic (PK/PD) models are necessary
to relate the degree of drug exposure in vivo to target blockade and pharmacological …
to relate the degree of drug exposure in vivo to target blockade and pharmacological …
Locomotor reactivity to a novel environment and sensitivity to MK-801 in five strains of mice
M Kalinichev, ST Bate, SA Coggon… - Behavioural …, 2008 - journals.lww.com
The ability of a noncompetitive antagonist of the N-methyl-D-aspartate receptor, MK-801, to
stimulate locomotor activity (LMA) in mice was compared across CD-1, MF1, NIH Swiss (NIHS…
stimulate locomotor activity (LMA) in mice was compared across CD-1, MF1, NIH Swiss (NIHS…