In vivo quantification of blood-brain transfer and binding of [125I]HEAT, an alpha 1-adrenoceptor antagonist.

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

In vivo quantification of blood-brain transfer and binding of [125I]HEAT, an alpha 1-adrenoceptor antagonist. / Dyve, S; Gjedde, A; Diksic, M; Sherwin, A; Hakim, A.

In: Synapse, Vol. 3, No. 3, 1989, p. 205-12.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Dyve, S, Gjedde, A, Diksic, M, Sherwin, A & Hakim, A 1989, 'In vivo quantification of blood-brain transfer and binding of [125I]HEAT, an alpha 1-adrenoceptor antagonist.', Synapse, vol. 3, no. 3, pp. 205-12. https://doi.org/10.1002/syn.890030306

APA

Dyve, S., Gjedde, A., Diksic, M., Sherwin, A., & Hakim, A. (1989). In vivo quantification of blood-brain transfer and binding of [125I]HEAT, an alpha 1-adrenoceptor antagonist. Synapse, 3(3), 205-12. https://doi.org/10.1002/syn.890030306

Vancouver

Dyve S, Gjedde A, Diksic M, Sherwin A, Hakim A. In vivo quantification of blood-brain transfer and binding of [125I]HEAT, an alpha 1-adrenoceptor antagonist. Synapse. 1989;3(3):205-12. https://doi.org/10.1002/syn.890030306

Author

Dyve, S ; Gjedde, A ; Diksic, M ; Sherwin, A ; Hakim, A. / In vivo quantification of blood-brain transfer and binding of [125I]HEAT, an alpha 1-adrenoceptor antagonist. In: Synapse. 1989 ; Vol. 3, No. 3. pp. 205-12.

Bibtex

@article{2c457c50b31511debc73000ea68e967b,
title = "In vivo quantification of blood-brain transfer and binding of [125I]HEAT, an alpha 1-adrenoceptor antagonist.",
abstract = "The uptake and binding constants of [125I]iodo-2-[beta-(4-hydroxyphenyl)-ethyl-amino-methyl]tetralone ( [125I]HEAT) in rat brain were determined in vivo. The initial clearance of the radioligand from blood to brain, K1, was calculated from the initial uptake of the radioligand; it averaged 0.21 +/- 0.01 (SD) ml g-1 min -1, consistent with an initial extraction of 25% (i.e., one-quarter of the blood flow). The most strongly binding regions included the olfactory bulb, thalamic nuclei, medial geniculate body, and cerebral cortical layers. We identified saturable, specific binding in frontal cortex layers 1, 5a, and 5c (motor region), frontal cortex layers 3+4, ventral thalamic nuclei, medial geniculate body, striatum, cerebellum, and olfactory bulb. Addition of unlabeled ligand depressed binding in all regions to the same low level (partition coefficient) of 0.8 ml g-1. Displacement of [125 I]HEAT binding by unlabeled HEAT yielded a global affinity constant (KDVd) of 34 +/- 8 pmol g-1 and receptor densities (Bmax) that varied from 50 pmol g-1 in cerebellar cortex and caudate nucleus to 200 pmol g-1 in the region of highest specific binding, the medial geniculate body.",
author = "S Dyve and A Gjedde and M Diksic and A Sherwin and A Hakim",
year = "1989",
doi = "10.1002/syn.890030306",
language = "English",
volume = "3",
pages = "205--12",
journal = "Synapse",
issn = "0887-4476",
publisher = "Wiley",
number = "3",

}

RIS

TY - JOUR

T1 - In vivo quantification of blood-brain transfer and binding of [125I]HEAT, an alpha 1-adrenoceptor antagonist.

AU - Dyve, S

AU - Gjedde, A

AU - Diksic, M

AU - Sherwin, A

AU - Hakim, A

PY - 1989

Y1 - 1989

N2 - The uptake and binding constants of [125I]iodo-2-[beta-(4-hydroxyphenyl)-ethyl-amino-methyl]tetralone ( [125I]HEAT) in rat brain were determined in vivo. The initial clearance of the radioligand from blood to brain, K1, was calculated from the initial uptake of the radioligand; it averaged 0.21 +/- 0.01 (SD) ml g-1 min -1, consistent with an initial extraction of 25% (i.e., one-quarter of the blood flow). The most strongly binding regions included the olfactory bulb, thalamic nuclei, medial geniculate body, and cerebral cortical layers. We identified saturable, specific binding in frontal cortex layers 1, 5a, and 5c (motor region), frontal cortex layers 3+4, ventral thalamic nuclei, medial geniculate body, striatum, cerebellum, and olfactory bulb. Addition of unlabeled ligand depressed binding in all regions to the same low level (partition coefficient) of 0.8 ml g-1. Displacement of [125 I]HEAT binding by unlabeled HEAT yielded a global affinity constant (KDVd) of 34 +/- 8 pmol g-1 and receptor densities (Bmax) that varied from 50 pmol g-1 in cerebellar cortex and caudate nucleus to 200 pmol g-1 in the region of highest specific binding, the medial geniculate body.

AB - The uptake and binding constants of [125I]iodo-2-[beta-(4-hydroxyphenyl)-ethyl-amino-methyl]tetralone ( [125I]HEAT) in rat brain were determined in vivo. The initial clearance of the radioligand from blood to brain, K1, was calculated from the initial uptake of the radioligand; it averaged 0.21 +/- 0.01 (SD) ml g-1 min -1, consistent with an initial extraction of 25% (i.e., one-quarter of the blood flow). The most strongly binding regions included the olfactory bulb, thalamic nuclei, medial geniculate body, and cerebral cortical layers. We identified saturable, specific binding in frontal cortex layers 1, 5a, and 5c (motor region), frontal cortex layers 3+4, ventral thalamic nuclei, medial geniculate body, striatum, cerebellum, and olfactory bulb. Addition of unlabeled ligand depressed binding in all regions to the same low level (partition coefficient) of 0.8 ml g-1. Displacement of [125 I]HEAT binding by unlabeled HEAT yielded a global affinity constant (KDVd) of 34 +/- 8 pmol g-1 and receptor densities (Bmax) that varied from 50 pmol g-1 in cerebellar cortex and caudate nucleus to 200 pmol g-1 in the region of highest specific binding, the medial geniculate body.

U2 - 10.1002/syn.890030306

DO - 10.1002/syn.890030306

M3 - Journal article

C2 - 2566205

VL - 3

SP - 205

EP - 212

JO - Synapse

JF - Synapse

SN - 0887-4476

IS - 3

ER -

ID: 14945529