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Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors

Autor: Kelly Krause, Andrew P. Degnan, George O. Tora, Yu-Wen Li, Daniel G. Morgan, Ramkumar Rajamani, Joanna Hu, Ying Han, Rudolph G. Krause, Joanne J. Bronson, Robert L. Bertekap, Sarah J. Taylor, Kevin W. Gillman, Nicholas J. Lodge, Matthew T. Taber, John E. Macor, Gail K. Mattson, Melissa A. Cunningham, Carl D. Davis

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:3039-3043

Depression is a serious illness that affects millions of patients. Current treatments are associated with a number of undesirable side effects. Neurokinin 1 receptor (NK1R) antagonists have recently been shown to potentiate the antidepressant effects

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b85bad869a118e4a255bfbb6b6ebb60f
https://doi.org/10.1016/j.bmcl.2015.04.098

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The Effects of Moral Licensing and Moral Cleansing in Contingent Valuation and Laboratory Experiments on the Demand to Reduce Externalities

Autor: Antonio M. Bento, Benjamin Ho, Gregory L. Poe, John T. Taber

Publikováno v: Environmental and Resource Economics. 64:317-340

Recent field experiments show that peer information can induce people to reduce their production of negative externalities. Related work in psychology demonstrates that inducing feelings of relative culpability in one domain can induce spillover pro-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c2b9d9e5772b52c0684be746e0d0a046
https://doi.org/10.1007/s10640-014-9872-y

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NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the Gerbil forced swim test

Autor: Kimberly Newberry, Kevin W. Gillman, Matthew T. Taber, Snjezana Lelas, Tanya L. Wallace-Boone, Yu-Wen Li, Carl D. Davis, Rick L. Pieschl, Nicholas J. Lodge, John E. Macor, Thaddeus F. Molski, Michael F. Parker, Joanne J. Bronson, Amy Newton

Publikováno v: Neuropharmacology. 73:232-240

The known interactions between the serotonergic and neurokinin systems suggest that serotonin reuptake inhibitor (SSRIs) efficacy may be improved by neurokinin-1 receptor (NK1R) antagonism. In the current studies combination of a subeffective dose of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d2478511e61245db99427a73ea617f5
https://doi.org/10.1016/j.neuropharm.2013.05.038

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Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression

Autor: Yu-Wen Li, George O. Tora, Snjezana Lelas, Kim A. Johnson, Matthew T. Taber, Joanne J. Bronson, Michael F. Parker, Rudolf G. Krause, Amy Newton, Robert L. Bertekap, Kelly D. Lengyel, Kevin W. Gillman, Nicholas J. Lodge, Rick L. Pieschl, John E. Macor, Andrew P. Degnan, Silva Mark, Sarah J. Taylor

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:407-411

A series of substituted pyridines, ether linked to a phenylpiperidine core were optimized for dual NK(1)/SERT affinity. Optimization based on NK(1)/SERT binding affinities, and minimization of off-target ion channel activity lead to the discovery of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::357bdb8f1a8f0c5d53b0870959d77c3f
https://doi.org/10.1016/j.bmcl.2012.11.094

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Consumer Valuation of Environmentally Friendly Production Practices in Wines, considering Asymmetric Information and Sensory Effects

Autor: Todd M. Schmit, John T. Taber, Bradley J. Rickard

Publikováno v: Journal of Agricultural Economics. 64:483-504

Agricultural producers and food marketers are increasingly responding to environmentally friendly cues from consumers, even though privately appropriated values associated with a range of food products commonly rank above their public-good counterpar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::44690c11ca2a25120c8c8a6ca9d724fe
https://doi.org/10.1111/1477-9552.12001

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Conformationally Restricted Homotryptamines. Part 7: 3-cis-(3-Aminocyclopentyl)indoles As Potent Selective Serotonin Reuptake Inhibitors

Autor: Qi Gao, Brett R. Beno, Zhaoxing Meng, Jeffrey A. Deskus, Charles P. Sloan, Nicholas J. Lodge, John E. Macor, Matthew T. Taber, Melissa A. Lapaglia, Dalton King, Thaddeus F. Molski, Ronald J. Mattson, Edward S. Kozlowski, Gail K. Mattson

Publikováno v: Journal of Medicinal Chemistry. 53:7564-7572

A series of conformationally restricted homotryptamines has been synthesized and shown to be potent inhibitors of hSERT. Conformational restriction of the homotryptamine side chain was attained by the insertion of a cyclopentyl ring, with the indole

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2330471c299d61a2a41989281465e08c
https://doi.org/10.1021/jm100515z

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Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF1R)

Autor: Gene M. Dubowchik, Kaitlin E. Browman, Lynn A. Balanda, Kevin D. Burris, John E. Macor, Bireshwar Dasgupta, Sokhom S. Pin, Vivekananda M. Vrudhula, Lawrence K. Fung, Matthew T. Taber, Tracey Fiedler, Jie Zhang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:1905-1909

Several tetrahydroimidazopyrimidines were prepared using silver assisted cyclization as the key step. The binding affinities of compounds thus prepared were evaluated in vitro toward hCRF(1)R. Initial lead compound 16 (K(i)=32 nM) demonstrated modest

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c7fd258ce27ad91ced45f6db8058fc7
https://doi.org/10.1016/j.bmcl.2010.01.127

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Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors

Autor: Rudolph G. Krause, Charles P. Sloan, Jingfang Qian-Cutrone, Thaddeus F. Molski, Joseph A. Cipollina, Gail K. Mattson, Matthew T. Taber, Qi Gao, Ronald J. Mattson, Jeffrey A. Deskus, James R. Epperson, Brett R. Beno, Baoqing Ma, Nicholas J. Lodge, Pierre Dextraze

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:3099-3104

A series of indole tetrahydropyridine and indole cyclohexenylamines was prepared, and their binding affinities at the human serotonin transporter (SERT) were determined. In particular, a nitrile substituent at the C5 position of the indole ring gave

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d533201a7aa23d4da087350d780e6d89
https://doi.org/10.1016/j.bmcl.2007.03.040

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An orally active corticotropin releasing factor 1 receptor antagonist from 8-aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes

Autor: Tracey Fiedler, Matthew T. Taber, Jie Zhang, Shelly X. Ren, Robert Macci, Sokhom S. Pin, Gene M. Dubowchik, Kaitlin E. Browman, Lynn A. Balanda, Jay O. Knipe, Kevin D. Burris, Rita L. Civiello, Xiaojun Han

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:2026-2030

8-Aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes represent a novel series of high-affinity corticotropin-releasing factor-1 receptor (CRF1R) antagonists. Herein we report the synthesis and SAR around the tricyclic core and the anxiolytic activity of an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af1143383cd229586f3c2af1512e57b5
https://doi.org/10.1016/j.bmcl.2007.01.008

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