Development of a photoswitchable antagonist of NMDA receptors

Felix W.W. Hartrampf; David M. Barber; Kevin Gottschling; Philipp Leippe; Michael Hollmann; Dirk Trauner

doi:10.1016/j.tet.2017.06.056

Development of a photoswitchable antagonist of NMDA receptors

Felix W.W. Hartrampf, David M. Barber, Kevin Gottschling, Philipp Leippe, Michael Hollmann, Dirk Trauner

Chemistry

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

Abstract

N-methyl–Daspartate receptors (NMDARs) are vital for neurological processes such as learning, memory, and synaptic plasticity. As such, small molecules that modulate their function are of interest in the study of numerous neurological diseases. We have synthesized a small library of photoswitches that modulate NMDAR function. The most efficient photoswitch to date is based on a known ligand of the glycine binding site and shows significant subtype selectivity.

Original language	English (US)
Pages (from-to)	4905-4912
Number of pages	8
Journal	Tetrahedron
Volume	73
Issue number	33
DOIs	https://doi.org/10.1016/j.tet.2017.06.056
State	Published - 2017

Keywords

Antagonist
Azobenzene
Photopharmacology
Photoswitch
glutamate receptor

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

Access to Document

10.1016/j.tet.2017.06.056

Cite this

@article{f4adcbfe3ff64ac2b285999f9e9bd2b5,

title = "Development of a photoswitchable antagonist of NMDA receptors",

abstract = "N-methyl–Daspartate receptors (NMDARs) are vital for neurological processes such as learning, memory, and synaptic plasticity. As such, small molecules that modulate their function are of interest in the study of numerous neurological diseases. We have synthesized a small library of photoswitches that modulate NMDAR function. The most efficient photoswitch to date is based on a known ligand of the glycine binding site and shows significant subtype selectivity.",

keywords = "Antagonist, Azobenzene, Photopharmacology, Photoswitch, glutamate receptor",

author = "Hartrampf, {Felix W.W.} and Barber, {David M.} and Kevin Gottschling and Philipp Leippe and Michael Hollmann and Dirk Trauner",

note = "Funding Information: D. M. B. gratefully acknowledges the European Commission for a Marie Sk{\l}odowska-Curie Intra-European Fellowship (PIEF-GA-2013-627990). D. T. thanks the Munich Center for Integrated Protein Science (CIPSM) and the European Research Council (Advanced Grant 268795). Publisher Copyright: {\textcopyright} 2017",

year = "2017",

doi = "10.1016/j.tet.2017.06.056",

language = "English (US)",

volume = "73",

pages = "4905--4912",

journal = "Tetrahedron",

issn = "0040-4020",

publisher = "Elsevier Ltd",

number = "33",

}

TY - JOUR

T1 - Development of a photoswitchable antagonist of NMDA receptors

AU - Hartrampf, Felix W.W.

AU - Barber, David M.

AU - Gottschling, Kevin

AU - Leippe, Philipp

AU - Hollmann, Michael

AU - Trauner, Dirk

N1 - Funding Information: D. M. B. gratefully acknowledges the European Commission for a Marie Skłodowska-Curie Intra-European Fellowship (PIEF-GA-2013-627990). D. T. thanks the Munich Center for Integrated Protein Science (CIPSM) and the European Research Council (Advanced Grant 268795). Publisher Copyright: © 2017

PY - 2017

Y1 - 2017

N2 - N-methyl–Daspartate receptors (NMDARs) are vital for neurological processes such as learning, memory, and synaptic plasticity. As such, small molecules that modulate their function are of interest in the study of numerous neurological diseases. We have synthesized a small library of photoswitches that modulate NMDAR function. The most efficient photoswitch to date is based on a known ligand of the glycine binding site and shows significant subtype selectivity.

AB - N-methyl–Daspartate receptors (NMDARs) are vital for neurological processes such as learning, memory, and synaptic plasticity. As such, small molecules that modulate their function are of interest in the study of numerous neurological diseases. We have synthesized a small library of photoswitches that modulate NMDAR function. The most efficient photoswitch to date is based on a known ligand of the glycine binding site and shows significant subtype selectivity.

KW - Antagonist

KW - Azobenzene

KW - Photopharmacology

KW - Photoswitch

KW - glutamate receptor

UR - http://www.scopus.com/inward/record.url?scp=85021885818&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85021885818&partnerID=8YFLogxK

U2 - 10.1016/j.tet.2017.06.056

DO - 10.1016/j.tet.2017.06.056

M3 - Article

AN - SCOPUS:85021885818

SN - 0040-4020

VL - 73

SP - 4905

EP - 4912

JO - Tetrahedron

JF - Tetrahedron

IS - 33

ER -

Development of a photoswitchable antagonist of NMDA receptors

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this