Synthesis and Biological Evaluation of [125I]- and [123I]-4-Iododexetimide, a Potent Muscarinic Cholinergic Receptor Antagonist

Alan A. Wilson; Robert F. Dannals; Hayden T Ravert; J. James Frost; Henry N. Wagner

doi:10.1021/jm00125a021

Synthesis and Biological Evaluation of [¹²⁵I]- and [¹²³I]-4-Iododexetimide, a Potent Muscarinic Cholinergic Receptor Antagonist

Alan A. Wilson, Robert F. Dannals, Hayden T Ravert, J. James Frost, Henry N. Wagner

School of Medicine

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

58 Scopus citations

Abstract

A series of halogenated racemic analogues of dexetimide (1) was synthesized and their affinity for the muscarinic cholinergic receptor measured. One analogue, 4-iododexetimide (21), was efficiently labeled with¹²⁵I and¹²³I at high specific activity. In vitro binding studies and in vivo biodistribution studies suggest that¹²³I-labeled 21 may be useful for imaging muscarinic cholinergic receptors in the living human brain with single photon emission computed tomography.

Original language	English (US)
Pages (from-to)	1057-1062
Number of pages	6
Journal	Journal of medicinal chemistry
Volume	32
Issue number	5
DOIs	https://doi.org/10.1021/jm00125a021
State	Published - May 1 1989

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

Access to Document

10.1021/jm00125a021

Cite this

@article{590404eaa4f4406abc88ff593d23e884,

title = "Synthesis and Biological Evaluation of [125I]- and [123I]-4-Iododexetimide, a Potent Muscarinic Cholinergic Receptor Antagonist",

abstract = "A series of halogenated racemic analogues of dexetimide (1) was synthesized and their affinity for the muscarinic cholinergic receptor measured. One analogue, 4-iododexetimide (21), was efficiently labeled with125I and123I at high specific activity. In vitro binding studies and in vivo biodistribution studies suggest that123I-labeled 21 may be useful for imaging muscarinic cholinergic receptors in the living human brain with single photon emission computed tomography.",

author = "Wilson, {Alan A.} and Dannals, {Robert F.} and Ravert, {Hayden T} and Frost, {J. James} and Wagner, {Henry N.}",

year = "1989",

month = may,

day = "1",

doi = "10.1021/jm00125a021",

language = "English (US)",

volume = "32",

pages = "1057--1062",

journal = "Journal of medicinal chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "5",

}

TY - JOUR

T1 - Synthesis and Biological Evaluation of [125I]- and [123I]-4-Iododexetimide, a Potent Muscarinic Cholinergic Receptor Antagonist

AU - Wilson, Alan A.

AU - Dannals, Robert F.

AU - Ravert, Hayden T

AU - Frost, J. James

AU - Wagner, Henry N.

PY - 1989/5/1

Y1 - 1989/5/1

N2 - A series of halogenated racemic analogues of dexetimide (1) was synthesized and their affinity for the muscarinic cholinergic receptor measured. One analogue, 4-iododexetimide (21), was efficiently labeled with125I and123I at high specific activity. In vitro binding studies and in vivo biodistribution studies suggest that123I-labeled 21 may be useful for imaging muscarinic cholinergic receptors in the living human brain with single photon emission computed tomography.

AB - A series of halogenated racemic analogues of dexetimide (1) was synthesized and their affinity for the muscarinic cholinergic receptor measured. One analogue, 4-iododexetimide (21), was efficiently labeled with125I and123I at high specific activity. In vitro binding studies and in vivo biodistribution studies suggest that123I-labeled 21 may be useful for imaging muscarinic cholinergic receptors in the living human brain with single photon emission computed tomography.

UR - http://www.scopus.com/inward/record.url?scp=0024599340&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0024599340&partnerID=8YFLogxK

U2 - 10.1021/jm00125a021

DO - 10.1021/jm00125a021

M3 - Article

C2 - 2785211

AN - SCOPUS:0024599340

SN - 0022-2623

VL - 32

SP - 1057

EP - 1062

JO - Journal of medicinal chemistry

JF - Journal of medicinal chemistry

IS - 5

ER -

Synthesis and Biological Evaluation of [¹²⁵I]- and [¹²³I]-4-Iododexetimide, a Potent Muscarinic Cholinergic Receptor Antagonist

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this