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22 hits

Bibliografisk träff 2023-07-19

A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs.

Sutherland JJ, Yonchev D, Fekete A, Urban L.

Nat Commun · research support, non-u.s. gov't; research-article; journal article · DOI 10.1038/s41467-023-40064-9

Bibliografisk träff 2014-06-17

Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors.

Storer RI, Brennan PE, Brown AD, Bungay PJ, Conlon KM, Corbett MS, DePianta RP, Fish PV, Heifetz A, Ho DK, Jessiman AS, McMurray G, de Oliveira CA, Roberts LR, Root JA, Shanmugasundaram V, Shapiro MJ, Skerten M, Westbrook D, Wheeler S, Whitlock GA, Wright J.

J Med Chem · journal article · DOI 10.1021/jm5003292

Bibliografisk träff 2013-11-19

Flexible and biomimetic analogs of triple uptake inhibitor 4-((((3S,6S)-6-benzhydryltetrahydro-2H-pyran-3-yl)amino)methyl)phenol: Synthesis, biological characterization, and development of a pharmacophore model.

Sharma H, Santra S, Debnath J, Antonio T, Reith M, Dutta A.

Bioorg Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2013.11.017

Bibliografisk träff 2011-04-07

Species independence in brain tissue binding using brain homogenates.

Di L, Umland JP, Chang G, Huang Y, Lin Z, Scott DO, Troutman MD, Liston TE.

Drug Metab Dispos · journal article · DOI 10.1124/dmd.111.038778

Bibliografisk träff 2011-03-29

Further structure-activity relationship studies on 4-((((3S,6S)-6-benzhydryltetrahydro-2H-pyran-3-yl)amino)methyl)phenol: identification of compounds with triple uptake inhibitory activity as potential antidepressant agents.

Gopishetty B, Hazeldine S, Santra S, Johnson M, Modi G, Ali S, Zhen J, Reith M, Dutta A.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm200020a

Bibliografisk träff 2010-10-21

Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.

Alelyunas YW, Empfield JR, McCarthy D, Spreen RC, Bui K, Pelosi-Kilby L, Shen C.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2010.10.068

Bibliografisk träff 2010-03-01

1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as potent and selective norepinephrine reuptake inhibitors.

Vu AT, Cohn ST, Zhang P, Kim CY, Mahaney PE, Bray JA, Johnston GH, Koury EJ, Cosmi SA, Deecher DC, Smith VA, Harrison JE, Leventhal L, Whiteside GT, Kennedy JD, Trybulski EJ.

J Med Chem · journal article · DOI 10.1021/jm901559e

Bibliografisk träff 2010-02-01

Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.

Varma MV, Obach RS, Rotter C, Miller HR, Chang G, Steyn SJ, El-Kattan A, Troutman MD.

J Med Chem · journal article · DOI 10.1021/jm901371v

Bibliografisk träff 2009-09-01

1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.

Zhang P, Terefenko EA, Bray J, Deecher D, Fensome A, Harrison J, Kim C, Koury E, Mark L, McComas CC, Mugford CA, Trybulski EJ, Vu AT, Whiteside GT, Mahaney PE.

J Med Chem · journal article · DOI 10.1021/jm900888c

Bibliografisk träff 2009-08-01

Physicochemical determinants of human renal clearance.

Varma MV, Feng B, Obach RS, Troutman MD, Chupka J, Miller HR, El-Kattan A.

J Med Chem · journal article · DOI 10.1021/jm900403j

Bibliografisk träff 2009-03-18

3-(Arylamino)-3-phenylpropan-2-olamines as a new series of dual norepinephrine and serotonin reuptake inhibitors.

Vu AT, Cohn ST, Terefenko EA, Moore WJ, Zhang P, Mahaney PE, Trybulski EJ, Goljer I, Dooley R, Bray JA, Johnston GH, Leiter J, Deecher DC.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2009.03.054

Bibliografisk träff 2008-10-11

Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.

Zhang P, Terefenko EA, McComas CC, Mahaney PE, Vu A, Trybulski E, Koury E, Johnston G, Bray J, Deecher D.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2008.10.026

Bibliografisk träff 2008-08-22

Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.

McComas CC, Vu AT, Mahaney PE, Cohn ST, Fensome A, Marella MA, Nogle L, Trybulski EJ, Ye F, Zhang P, Alfinito P, Bray J, Johnston G, Koury E, Deecher DC.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2008.08.060

Bibliografisk träff 2008-04-21

Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.

Obach RS, Lombardo F, Waters NJ.

Drug Metab Dispos · journal article · DOI 10.1124/dmd.108.020479

Bibliografisk träff 2008-03-20

Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition.

Fish PV, Deur C, Gan X, Greene K, Hoople D, Mackenny M, Para KS, Reeves K, Ryckmans T, Stiff C, Stobie A, Wakenhut F, Whitlock GA.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2008.03.050

Bibliografisk träff 2008-02-16

[4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors.

Fish PV, Ryckmans T, Stobie A, Wakenhut F.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2008.02.036

Bibliografisk träff 2006-06-05

N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.

Jonathan Fray M, Bish G, Brown AD, Fish PV, Stobie A, Wakenhut F, Whitlock GA.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2006.05.051

Bibliografisk träff 2006-06-05

Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.

Fray MJ, Bish G, Fish PV, Stobie A, Wakenhut F, Whitlock GA.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2006.05.049

Bibliografisk träff 2004-02-01

Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.

Plisson C, McConathy J, Martarello L, Malveaux EJ, Camp VM, Williams L, Votaw JR, Goodman MM.

J Med Chem · research support, u.s. gov't, p.h.s.; research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1021/jm030384e

Bibliografisk träff 2003-12-01

Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.

Orjales A, Mosquera R, Toledo A, Pumar MC, García N, Cortizo L, Labeaga L, Innerárity A.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm0309349

Bibliografisk träff 2003-04-01

Inhibition of P-glycoprotein by newer antidepressants.

Weiss J, Dormann SM, Martin-Facklam M, Kerpen CJ, Ketabi-Kiyanvash N, Haefeli WE.

J Pharmacol Exp Ther · research support, non-u.s. gov't; journal article · DOI 10.1124/jpet.102.046532

Bibliografisk träff 2003-03-01

Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography.

Goodman MM, Chen P, Plisson C, Martarello L, Galt J, Votaw JR, Kilts CD, Malveaux G, Camp VM, Shi B, Ely TD, Howell L, McConathy J, Nemeroff CB.

J Med Chem · research support, non-u.s. gov't; research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1021/jm0100180