Endogenous indoles as novel polyamine site ligands at the N-methyl-D-aspartate receptor complex

David R. Worthen; D. Alex Gibson; Dennis T. Rogers; Aimee K. Bence; May Fu; John M. Littleton; Peter A. Crooks

doi:10.1016/S0006-8993(00)03201-7

Endogenous indoles as novel polyamine site ligands at the N-methyl-D-aspartate receptor complex

David R. Worthen
, D. Alex Gibson
, Dennis T. Rogers
, Aimee K. Bence
, May Fu
, John M. Littleton
, Peter A. Crooks

Psychology

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

13 Scopus citations

Abstract

High-throughput ligand displacement screens of a series of endogenous indoles revealed that tryptamine, serotonin and 5-methoxytryptamine readily displace [³H]spermidine and [³H]MK-801 from their respective binding sites in rat brain homogenate. These data, coupled with their potent inhibition of spermidine-potentiated [³H]MK-801 binding, suggest that certain endogenous indoles may act as ligands to one or more polyamine binding sites in the brain, including those on the N-methyl-D-aspartate receptor complex.

Original language	English
Pages (from-to)	343-346
Number of pages	4
Journal	Brain Research
Volume	890
Issue number	2
DOIs	https://doi.org/10.1016/S0006-8993(00)03201-7
State	Published - Feb 2 2001

Bibliographical note

Funding Information:
This investigation was supported by National Institutes of Health, National Research Service award DA07304 from the National Institute on Drug Abuse, American Foundation for Pharmaceutical Education Fellowships (A.K.B. and D.R.W.) and National Institute of Alcohol Abuse and Alcoholism Grant AA12600.

Funding

This investigation was supported by National Institutes of Health, National Research Service award DA07304 from the National Institute on Drug Abuse, American Foundation for Pharmaceutical Education Fellowships (A.K.B. and D.R.W.) and National Institute of Alcohol Abuse and Alcoholism Grant AA12600.

Funders	Funder number
National Institutes of Health (NIH)
Author National Institute on Drug Abuse DA031791 Mark J Ferris National Institute on Drug Abuse DA006634 Mark J Ferris National Institute on Alcohol Abuse and Alcoholism AA026117 Mark J Ferris National Institute on Alcohol Abuse and Alcoholism AA028162 Elizabeth G Pitts National Institute of General Medical Sciences GM102773 Elizabeth G Pitts Peter McManus Charitable Trust Mark J Ferris National Institute on Drug Abuse	R01DA007304
Author National Institute on Drug Abuse DA031791 Mark J Ferris National Institute on Drug Abuse DA006634 Mark J Ferris National Institute on Alcohol Abuse and Alcoholism AA026117 Mark J Ferris National Institute on Alcohol Abuse and Alcoholism AA028162 Elizabeth G Pitts National Institute of General Medical Sciences GM102773 Elizabeth G Pitts Peter McManus Charitable Trust Mark J Ferris National Institute on Drug Abuse
National Institute on Alcohol Abuse and Alcoholism	AA12600
National Institute on Alcohol Abuse and Alcoholism
American Foundation for Pharmaceutical Education

Keywords

CNS
Endogenous indole
N-Methyl-D-aspartate
Neuroprotection
Polyamine recognition domain

ASJC Scopus subject areas

General Neuroscience
Molecular Biology
Clinical Neurology
Developmental Biology

Access to Document

10.1016/S0006-8993(00)03201-7

Cite this

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title = "Endogenous indoles as novel polyamine site ligands at the N-methyl-D-aspartate receptor complex",

abstract = "High-throughput ligand displacement screens of a series of endogenous indoles revealed that tryptamine, serotonin and 5-methoxytryptamine readily displace [3H]spermidine and [3H]MK-801 from their respective binding sites in rat brain homogenate. These data, coupled with their potent inhibition of spermidine-potentiated [3H]MK-801 binding, suggest that certain endogenous indoles may act as ligands to one or more polyamine binding sites in the brain, including those on the N-methyl-D-aspartate receptor complex.",

keywords = "CNS, Endogenous indole, N-Methyl-D-aspartate, Neuroprotection, Polyamine recognition domain",

author = "Worthen, \{David R.\} and Gibson, \{D. Alex\} and Rogers, \{Dennis T.\} and Bence, \{Aimee K.\} and May Fu and Littleton, \{John M.\} and Crooks, \{Peter A.\}",

note = "Funding Information: This investigation was supported by National Institutes of Health, National Research Service award DA07304 from the National Institute on Drug Abuse, American Foundation for Pharmaceutical Education Fellowships (A.K.B. and D.R.W.) and National Institute of Alcohol Abuse and Alcoholism Grant AA12600.",

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AU - Gibson, D. Alex

AU - Rogers, Dennis T.

AU - Bence, Aimee K.

AU - Fu, May

AU - Littleton, John M.

AU - Crooks, Peter A.

N1 - Funding Information: This investigation was supported by National Institutes of Health, National Research Service award DA07304 from the National Institute on Drug Abuse, American Foundation for Pharmaceutical Education Fellowships (A.K.B. and D.R.W.) and National Institute of Alcohol Abuse and Alcoholism Grant AA12600.

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N2 - High-throughput ligand displacement screens of a series of endogenous indoles revealed that tryptamine, serotonin and 5-methoxytryptamine readily displace [3H]spermidine and [3H]MK-801 from their respective binding sites in rat brain homogenate. These data, coupled with their potent inhibition of spermidine-potentiated [3H]MK-801 binding, suggest that certain endogenous indoles may act as ligands to one or more polyamine binding sites in the brain, including those on the N-methyl-D-aspartate receptor complex.

AB - High-throughput ligand displacement screens of a series of endogenous indoles revealed that tryptamine, serotonin and 5-methoxytryptamine readily displace [3H]spermidine and [3H]MK-801 from their respective binding sites in rat brain homogenate. These data, coupled with their potent inhibition of spermidine-potentiated [3H]MK-801 binding, suggest that certain endogenous indoles may act as ligands to one or more polyamine binding sites in the brain, including those on the N-methyl-D-aspartate receptor complex.

KW - CNS

KW - Endogenous indole

KW - N-Methyl-D-aspartate

KW - Neuroprotection

KW - Polyamine recognition domain

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Endogenous indoles as novel polyamine site ligands at the N-methyl-D-aspartate receptor complex

Abstract

Bibliographical note

Funding

Keywords

ASJC Scopus subject areas

Access to Document

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