Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR

Peter Grundt; Sarah Little Jane Husband; Robert R. Luedtke; Michelle Taylor; Amy Hauck Newman

doi:10.1016/j.bmcl.2006.10.076

Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR

Peter Grundt, Sarah Little Jane Husband, Robert R. Luedtke, Michelle Taylor, Amy Hauck Newman

Chemistry & Biochemistry

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

32 Scopus citations

Abstract

A series of analogues of the dopamine D2 receptor antagonist L741,626 were synthesized and evaluated for binding and function at D2 family receptor subtypes. Several analogues showed comparable binding profiles to the parent ligand, however, in general, chemical modification served to reduce D2 binding affinity and selectivity.

Original language	English (US)
Pages (from-to)	745-749
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2006.10.076
State	Published - Feb 1 2007

Bibliographical note

Funding Information:
The research reported herein was supported by funds from the NIDA Intramural Research Program and 1 DA 13584. P.G. was supported by a National Institutes of Health (NIH) Visiting Fellowship. S.L.J.H. was supported by a NIH summer IRTA fellowship.

Keywords

Dopamine D2 receptor antagonists

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access

10.1016/j.bmcl.2006.10.076

OpenUrl availability

Full text

Cite this

@article{42a2c60de1db42b1806999e83e414473,

title = "Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR",

abstract = "A series of analogues of the dopamine D2 receptor antagonist L741,626 were synthesized and evaluated for binding and function at D2 family receptor subtypes. Several analogues showed comparable binding profiles to the parent ligand, however, in general, chemical modification served to reduce D2 binding affinity and selectivity.",

keywords = "Dopamine D2 receptor antagonists",

author = "Peter Grundt and {Jane Husband}, {Sarah Little} and Luedtke, {Robert R.} and Michelle Taylor and Newman, {Amy Hauck}",

note = "Funding Information: The research reported herein was supported by funds from the NIDA Intramural Research Program and 1 DA 13584. P.G. was supported by a National Institutes of Health (NIH) Visiting Fellowship. S.L.J.H. was supported by a NIH summer IRTA fellowship. ",

year = "2007",

month = feb,

day = "1",

doi = "10.1016/j.bmcl.2006.10.076",

language = "English (US)",

volume = "17",

pages = "745--749",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "3",

}

TY - JOUR

T1 - Analogues of the dopamine D2 receptor antagonist L741,626

T2 - Binding, function, and SAR

AU - Grundt, Peter

AU - Jane Husband, Sarah Little

AU - Luedtke, Robert R.

AU - Taylor, Michelle

AU - Newman, Amy Hauck

N1 - Funding Information: The research reported herein was supported by funds from the NIDA Intramural Research Program and 1 DA 13584. P.G. was supported by a National Institutes of Health (NIH) Visiting Fellowship. S.L.J.H. was supported by a NIH summer IRTA fellowship.

PY - 2007/2/1

Y1 - 2007/2/1

N2 - A series of analogues of the dopamine D2 receptor antagonist L741,626 were synthesized and evaluated for binding and function at D2 family receptor subtypes. Several analogues showed comparable binding profiles to the parent ligand, however, in general, chemical modification served to reduce D2 binding affinity and selectivity.

AB - A series of analogues of the dopamine D2 receptor antagonist L741,626 were synthesized and evaluated for binding and function at D2 family receptor subtypes. Several analogues showed comparable binding profiles to the parent ligand, however, in general, chemical modification served to reduce D2 binding affinity and selectivity.

KW - Dopamine D2 receptor antagonists

UR - http://www.scopus.com/inward/record.url?scp=33846215182&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33846215182&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2006.10.076

DO - 10.1016/j.bmcl.2006.10.076

M3 - Article

C2 - 17095222

AN - SCOPUS:33846215182

SN - 0960-894X

VL - 17

SP - 745

EP - 749

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 3

ER -

Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR

Abstract

Bibliographical note

Keywords

UN SDGs

Access

OpenUrl availability

Other files and links

Fingerprint

Cite this