[125]I-Spectramide: A novel benzamide displaying potent and selective effects at the D2 dopamine receptor

Patricia M. Sánchez-Roa, Dimitri E. Grigoriadis, Alan A. Wilson, John Sharkey, Robert F Dannals, Victor L. Villemagne, Dean Foster Wong, Henry N. Wagner, Michael J. Kuhar

Research output: Contribution to journalArticle

Abstract

The new substituted benzamide Spectramide, (N-[2-[4-iodobenzyl-N-methylamino]-2-methoxy-4-ethyl]-5-chloro-methylamine] benzamide) labelled with 125I was used as a potent and highly selective dopamine-D2 receptor antagonist in rat striatal homogenates for in vitro receptor binding. Kinetic experiments demonstrated the reversibility of the binding and the estimated Kd from saturation analysis was 25 pM, with a Bmax of 20 pmol/g of tissue. Competition studies showed that spectramide did not interact potently with the D1 or dopamine-uptake site. Drugs known to interact with other receptor systems were weak competitors of the binding, while binding was potently inhibited by other D2 antagonists, such as spiperone and eticlopride. These data indicate that Spectramide binds selectively and with high affinity to the dopamine D2 receptors, and may prove to be a useful tool for the study of these receptors in vivo using PET or SPECT.

Original languageEnglish (US)
Pages (from-to)1821-1829
Number of pages9
JournalLife Sciences
Volume45
Issue number19
DOIs
StatePublished - 1989

Fingerprint

Dopamine D2 Receptors
eticlopride
Corpus Striatum
Spiperone
Single-Photon Emission-Computed Tomography
Rats
Dopamine
Tissue
Kinetics
Pharmaceutical Preparations
benzamide
spectramide
Experiments

ASJC Scopus subject areas

  • Pharmacology

Cite this

Sánchez-Roa, P. M., Grigoriadis, D. E., Wilson, A. A., Sharkey, J., Dannals, R. F., Villemagne, V. L., ... Kuhar, M. J. (1989). [125]I-Spectramide: A novel benzamide displaying potent and selective effects at the D2 dopamine receptor. Life Sciences, 45(19), 1821-1829. https://doi.org/10.1016/0024-3205(89)90523-7

[125]I-Spectramide : A novel benzamide displaying potent and selective effects at the D2 dopamine receptor. / Sánchez-Roa, Patricia M.; Grigoriadis, Dimitri E.; Wilson, Alan A.; Sharkey, John; Dannals, Robert F; Villemagne, Victor L.; Wong, Dean Foster; Wagner, Henry N.; Kuhar, Michael J.

In: Life Sciences, Vol. 45, No. 19, 1989, p. 1821-1829.

Research output: Contribution to journalArticle

Sánchez-Roa, PM, Grigoriadis, DE, Wilson, AA, Sharkey, J, Dannals, RF, Villemagne, VL, Wong, DF, Wagner, HN & Kuhar, MJ 1989, '[125]I-Spectramide: A novel benzamide displaying potent and selective effects at the D2 dopamine receptor', Life Sciences, vol. 45, no. 19, pp. 1821-1829. https://doi.org/10.1016/0024-3205(89)90523-7
Sánchez-Roa, Patricia M. ; Grigoriadis, Dimitri E. ; Wilson, Alan A. ; Sharkey, John ; Dannals, Robert F ; Villemagne, Victor L. ; Wong, Dean Foster ; Wagner, Henry N. ; Kuhar, Michael J. / [125]I-Spectramide : A novel benzamide displaying potent and selective effects at the D2 dopamine receptor. In: Life Sciences. 1989 ; Vol. 45, No. 19. pp. 1821-1829.
@article{8eed337155f44127b24a993ab7893142,
title = "[125]I-Spectramide: A novel benzamide displaying potent and selective effects at the D2 dopamine receptor",
abstract = "The new substituted benzamide Spectramide, (N-[2-[4-iodobenzyl-N-methylamino]-2-methoxy-4-ethyl]-5-chloro-methylamine] benzamide) labelled with 125I was used as a potent and highly selective dopamine-D2 receptor antagonist in rat striatal homogenates for in vitro receptor binding. Kinetic experiments demonstrated the reversibility of the binding and the estimated Kd from saturation analysis was 25 pM, with a Bmax of 20 pmol/g of tissue. Competition studies showed that spectramide did not interact potently with the D1 or dopamine-uptake site. Drugs known to interact with other receptor systems were weak competitors of the binding, while binding was potently inhibited by other D2 antagonists, such as spiperone and eticlopride. These data indicate that Spectramide binds selectively and with high affinity to the dopamine D2 receptors, and may prove to be a useful tool for the study of these receptors in vivo using PET or SPECT.",
author = "S{\'a}nchez-Roa, {Patricia M.} and Grigoriadis, {Dimitri E.} and Wilson, {Alan A.} and John Sharkey and Dannals, {Robert F} and Villemagne, {Victor L.} and Wong, {Dean Foster} and Wagner, {Henry N.} and Kuhar, {Michael J.}",
year = "1989",
doi = "10.1016/0024-3205(89)90523-7",
language = "English (US)",
volume = "45",
pages = "1821--1829",
journal = "Life Sciences",
issn = "0024-3205",
publisher = "Elsevier Inc.",
number = "19",

}

TY - JOUR

T1 - [125]I-Spectramide

T2 - A novel benzamide displaying potent and selective effects at the D2 dopamine receptor

AU - Sánchez-Roa, Patricia M.

AU - Grigoriadis, Dimitri E.

AU - Wilson, Alan A.

AU - Sharkey, John

AU - Dannals, Robert F

AU - Villemagne, Victor L.

AU - Wong, Dean Foster

AU - Wagner, Henry N.

AU - Kuhar, Michael J.

PY - 1989

Y1 - 1989

N2 - The new substituted benzamide Spectramide, (N-[2-[4-iodobenzyl-N-methylamino]-2-methoxy-4-ethyl]-5-chloro-methylamine] benzamide) labelled with 125I was used as a potent and highly selective dopamine-D2 receptor antagonist in rat striatal homogenates for in vitro receptor binding. Kinetic experiments demonstrated the reversibility of the binding and the estimated Kd from saturation analysis was 25 pM, with a Bmax of 20 pmol/g of tissue. Competition studies showed that spectramide did not interact potently with the D1 or dopamine-uptake site. Drugs known to interact with other receptor systems were weak competitors of the binding, while binding was potently inhibited by other D2 antagonists, such as spiperone and eticlopride. These data indicate that Spectramide binds selectively and with high affinity to the dopamine D2 receptors, and may prove to be a useful tool for the study of these receptors in vivo using PET or SPECT.

AB - The new substituted benzamide Spectramide, (N-[2-[4-iodobenzyl-N-methylamino]-2-methoxy-4-ethyl]-5-chloro-methylamine] benzamide) labelled with 125I was used as a potent and highly selective dopamine-D2 receptor antagonist in rat striatal homogenates for in vitro receptor binding. Kinetic experiments demonstrated the reversibility of the binding and the estimated Kd from saturation analysis was 25 pM, with a Bmax of 20 pmol/g of tissue. Competition studies showed that spectramide did not interact potently with the D1 or dopamine-uptake site. Drugs known to interact with other receptor systems were weak competitors of the binding, while binding was potently inhibited by other D2 antagonists, such as spiperone and eticlopride. These data indicate that Spectramide binds selectively and with high affinity to the dopamine D2 receptors, and may prove to be a useful tool for the study of these receptors in vivo using PET or SPECT.

UR - http://www.scopus.com/inward/record.url?scp=0024471492&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0024471492&partnerID=8YFLogxK

U2 - 10.1016/0024-3205(89)90523-7

DO - 10.1016/0024-3205(89)90523-7

M3 - Article

C2 - 2531826

AN - SCOPUS:0024471492

VL - 45

SP - 1821

EP - 1829

JO - Life Sciences

JF - Life Sciences

SN - 0024-3205

IS - 19

ER -