High-affinity fluorescent ligands for the 5-HT 3 receptor

Jonathan Simonin; Sanjeev Kumar V. Vernekar; Andrew J. Thompson; J. Daniel Hothersall; Christopher N. Connolly; Sarah C.R. Lummis; Martin Lochner

doi:10.1016/j.bmcl.2011.11.097

High-affinity fluorescent ligands for the 5-HT ₃ receptor

Jonathan Simonin
, Sanjeev Kumar V. Vernekar
, Andrew J. Thompson
, J. Daniel Hothersall
, Christopher N. Connolly
, Sarah C.R. Lummis
, Martin Lochner

Research output: Contribution to journal › Article › peer-review

20 Scopus citations

Abstract

The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT ₃ receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT ₃AR.

Original language	English (US)
Pages (from-to)	1151-1155
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	22
Issue number	2
DOIs	https://doi.org/10.1016/j.bmcl.2011.11.097
State	Published - Jan 15 2012
Externally published	Yes

Bibliographical note

Funding Information:
This research was supported by the Swiss National Science Foundation (SNSF-professorship PP00P2_123536 to ML), the EPSRC (EP/E042139/1) and the Wellcome Trust (085141 (CNC and JDH) and 081925/Z/07/Z (SCRL and AJT)). SCRL is a Wellcome Trust Senior Research Fellow in Basic Biomedical Science.

Keywords

5-HT receptor
Cys-loop ligand-gated ion channels
Fluorescent ligands
In vivo imaging
Radioligand binding

Publisher link

10.1016/j.bmcl.2011.11.097

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Cite this

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title = "High-affinity fluorescent ligands for the 5-HT 3 receptor",

abstract = "The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT 3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT 3AR.",

keywords = "5-HT receptor, Cys-loop ligand-gated ion channels, Fluorescent ligands, In vivo imaging, Radioligand binding",

author = "Jonathan Simonin and Vernekar, \{Sanjeev Kumar V.\} and Thompson, \{Andrew J.\} and Hothersall, \{J. Daniel\} and Connolly, \{Christopher N.\} and Lummis, \{Sarah C.R.\} and Martin Lochner",

note = "Funding Information: This research was supported by the Swiss National Science Foundation (SNSF-professorship PP00P2\_123536 to ML), the EPSRC (EP/E042139/1) and the Wellcome Trust (085141 (CNC and JDH) and 081925/Z/07/Z (SCRL and AJT)). SCRL is a Wellcome Trust Senior Research Fellow in Basic Biomedical Science. ",

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AU - Simonin, Jonathan

AU - Vernekar, Sanjeev Kumar V.

AU - Thompson, Andrew J.

AU - Hothersall, J. Daniel

AU - Connolly, Christopher N.

AU - Lummis, Sarah C.R.

AU - Lochner, Martin

N1 - Funding Information: This research was supported by the Swiss National Science Foundation (SNSF-professorship PP00P2_123536 to ML), the EPSRC (EP/E042139/1) and the Wellcome Trust (085141 (CNC and JDH) and 081925/Z/07/Z (SCRL and AJT)). SCRL is a Wellcome Trust Senior Research Fellow in Basic Biomedical Science.

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N2 - The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT 3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT 3AR.

AB - The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT 3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT 3AR.

KW - 5-HT receptor

KW - Cys-loop ligand-gated ion channels

KW - Fluorescent ligands

KW - In vivo imaging

KW - Radioligand binding

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