Quantification of Neuroreceptors in the living human brain. II. Inhibition studies of receptor density and affinity.

D F Wong; A Gjedde; H N Wagner; R F Dannals; K H Douglass; J M Links; M J Kuhar

Quantification of Neuroreceptors in the living human brain. II. Inhibition studies of receptor density and affinity.

D F Wong, A Gjedde, H N Wagner, R F Dannals, K H Douglass, J M Links, M J Kuhar

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

117 Citationer (Scopus)

Abstract

Udgivelsesdato: 1986-Apr

Originalsprog	Engelsk
Tidsskrift	Journal of Cerebral Blood Flow and Metabolism
Vol/bind	6
Udgave nummer	2
Sider (fra-til)	147-53
Antal sider	6
ISSN	0271-678X
Status	Udgivet - 1986
Udgivet eksternt	Ja

Citationsformater

Quantification of Neuroreceptors in the living human brain. II. Inhibition studies of receptor density and affinity. / Wong, D F; Gjedde, A; Wagner, H N; Dannals, R F; Douglass, K H; Links, J M; Kuhar, M J.

I: Journal of Cerebral Blood Flow and Metabolism, Bind 6, Nr. 2, 1986, s. 147-53.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

@article{36dc0e90b31511debc73000ea68e967b,

title = "Quantification of Neuroreceptors in the living human brain. II. Inhibition studies of receptor density and affinity.",

abstract = "A method for estimating receptor density (Bmax) in the living human brain by positron emission tomography was exemplified by a ligand, 3-N-[11C]methylspiperone ([11C]NMSP), that binds to D2 dopamine receptors with high affinity. The ligand binds essentially irreversibly (i.e., with very little dissociation) to the receptors during the 2-h scanning period. Transfer constants were estimated at steady state. In a previous article, we presented a method for the determination of k3, the rate of binding of the labeled ligand. In the present work, we varied k3 by reducing the number of available receptors with a previously administered receptor blocking agent, haloperidol. We calculated a receptor density of 9.2 pmol g-1 in the caudate nucleus of four normal volunteers, and an inhibitory constant of haloperidol of 1.4 nM by comparing tracer accumulation in the absence and the presence of the blocking agent. The values agreed with measurements of NMSP receptor density and haloperidol inhibitory potency in vitro in brain homogenates from human autopsy material.",

author = "Wong, {D F} and A Gjedde and Wagner, {H N} and Dannals, {R F} and Douglass, {K H} and Links, {J M} and Kuhar, {M J}",

year = "1986",

language = "English",

volume = "6",

pages = "147--53",

journal = "Journal of Cerebral Blood Flow and Metabolism",

issn = "0271-678X",

publisher = "SAGE Publications",

number = "2",

}

TY - JOUR

T1 - Quantification of Neuroreceptors in the living human brain. II. Inhibition studies of receptor density and affinity.

AU - Wong, D F

AU - Gjedde, A

AU - Wagner, H N

AU - Dannals, R F

AU - Douglass, K H

AU - Links, J M

AU - Kuhar, M J

PY - 1986

Y1 - 1986

N2 - A method for estimating receptor density (Bmax) in the living human brain by positron emission tomography was exemplified by a ligand, 3-N-[11C]methylspiperone ([11C]NMSP), that binds to D2 dopamine receptors with high affinity. The ligand binds essentially irreversibly (i.e., with very little dissociation) to the receptors during the 2-h scanning period. Transfer constants were estimated at steady state. In a previous article, we presented a method for the determination of k3, the rate of binding of the labeled ligand. In the present work, we varied k3 by reducing the number of available receptors with a previously administered receptor blocking agent, haloperidol. We calculated a receptor density of 9.2 pmol g-1 in the caudate nucleus of four normal volunteers, and an inhibitory constant of haloperidol of 1.4 nM by comparing tracer accumulation in the absence and the presence of the blocking agent. The values agreed with measurements of NMSP receptor density and haloperidol inhibitory potency in vitro in brain homogenates from human autopsy material.

AB - A method for estimating receptor density (Bmax) in the living human brain by positron emission tomography was exemplified by a ligand, 3-N-[11C]methylspiperone ([11C]NMSP), that binds to D2 dopamine receptors with high affinity. The ligand binds essentially irreversibly (i.e., with very little dissociation) to the receptors during the 2-h scanning period. Transfer constants were estimated at steady state. In a previous article, we presented a method for the determination of k3, the rate of binding of the labeled ligand. In the present work, we varied k3 by reducing the number of available receptors with a previously administered receptor blocking agent, haloperidol. We calculated a receptor density of 9.2 pmol g-1 in the caudate nucleus of four normal volunteers, and an inhibitory constant of haloperidol of 1.4 nM by comparing tracer accumulation in the absence and the presence of the blocking agent. The values agreed with measurements of NMSP receptor density and haloperidol inhibitory potency in vitro in brain homogenates from human autopsy material.

M3 - Journal article

C2 - 2937795

VL - 6

SP - 147

EP - 153

JO - Journal of Cerebral Blood Flow and Metabolism

JF - Journal of Cerebral Blood Flow and Metabolism

SN - 0271-678X

IS - 2

ER -