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Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins

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Standard

Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. / Bridges, Thomas M; Marlo, Joy E; Niswender, Colleen M; Jones, Carrie K; Jadhav, Satyawan B; Gentry, Patrick R; Plumley, Hyekyung C; Weaver, C David; Conn, P Jeffrey; Lindsley, Craig W.

I: Journal of Medicinal Chemistry, Bind 52, Nr. 11, 11.06.2009, s. 3445-8.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

Harvard

Bridges, TM, Marlo, JE, Niswender, CM, Jones, CK, Jadhav, SB, Gentry, PR, Plumley, HC, Weaver, CD, Conn, PJ & Lindsley, CW 2009, 'Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins', Journal of Medicinal Chemistry, bind 52, nr. 11, s. 3445-8. https://doi.org/10.1021/jm900286j

APA

Bridges, T. M., Marlo, J. E., Niswender, C. M., Jones, C. K., Jadhav, S. B., Gentry, P. R., Plumley, H. C., Weaver, C. D., Conn, P. J., & Lindsley, C. W. (2009). Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. Journal of Medicinal Chemistry, 52(11), 3445-8. https://doi.org/10.1021/jm900286j

Vancouver

Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR o.a. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. Journal of Medicinal Chemistry. 2009 jun 11;52(11):3445-8. https://doi.org/10.1021/jm900286j

Author

Bridges, Thomas M ; Marlo, Joy E ; Niswender, Colleen M ; Jones, Carrie K ; Jadhav, Satyawan B ; Gentry, Patrick R ; Plumley, Hyekyung C ; Weaver, C David ; Conn, P Jeffrey ; Lindsley, Craig W. / Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. I: Journal of Medicinal Chemistry. 2009 ; Bind 52, Nr. 11. s. 3445-8.

Bibtex

@article{fbc862ee1ece4777b620d2be21a1f695,
title = "Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins",
abstract = "This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5). Functional HTS, identified VU0119498, which displayed micromolar potencies for potentiation of acetylcholine at M1, M3, and M5 receptors in cell-based Ca(2+) mobilization assays. Subsequent optimization led to the discovery of VU0238429, which possessed an EC(50) of approximately 1.16 microM at M5 with >30-fold selectivity versus M1 and M3, with no M2 or M4 potentiator activity.",
keywords = "Allosteric Regulation/physiology, Animals, CHO Cells, Cricetinae, Cricetulus, Isatin/analogs & derivatives, Mice, Receptor, Muscarinic M5/drug effects",
author = "Bridges, {Thomas M} and Marlo, {Joy E} and Niswender, {Colleen M} and Jones, {Carrie K} and Jadhav, {Satyawan B} and Gentry, {Patrick R} and Plumley, {Hyekyung C} and Weaver, {C David} and Conn, {P Jeffrey} and Lindsley, {Craig W}",
year = "2009",
month = jun,
day = "11",
doi = "10.1021/jm900286j",
language = "English",
volume = "52",
pages = "3445--8",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "11",

}

RIS

TY - JOUR

T1 - Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins

AU - Bridges, Thomas M

AU - Marlo, Joy E

AU - Niswender, Colleen M

AU - Jones, Carrie K

AU - Jadhav, Satyawan B

AU - Gentry, Patrick R

AU - Plumley, Hyekyung C

AU - Weaver, C David

AU - Conn, P Jeffrey

AU - Lindsley, Craig W

PY - 2009/6/11

Y1 - 2009/6/11

N2 - This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5). Functional HTS, identified VU0119498, which displayed micromolar potencies for potentiation of acetylcholine at M1, M3, and M5 receptors in cell-based Ca(2+) mobilization assays. Subsequent optimization led to the discovery of VU0238429, which possessed an EC(50) of approximately 1.16 microM at M5 with >30-fold selectivity versus M1 and M3, with no M2 or M4 potentiator activity.

AB - This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5). Functional HTS, identified VU0119498, which displayed micromolar potencies for potentiation of acetylcholine at M1, M3, and M5 receptors in cell-based Ca(2+) mobilization assays. Subsequent optimization led to the discovery of VU0238429, which possessed an EC(50) of approximately 1.16 microM at M5 with >30-fold selectivity versus M1 and M3, with no M2 or M4 potentiator activity.

KW - Allosteric Regulation/physiology

KW - Animals

KW - CHO Cells

KW - Cricetinae

KW - Cricetulus

KW - Isatin/analogs & derivatives

KW - Mice

KW - Receptor, Muscarinic M5/drug effects

U2 - 10.1021/jm900286j

DO - 10.1021/jm900286j

M3 - Journal article

C2 - 19438238

VL - 52

SP - 3445

EP - 3448

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 11

ER -

ID: 213627227