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(+)-[H-3]MK-801 binding sites in postmortem human brain

(+)-[H-3]MK-801 binding sites in postmortem human brain
(+)-[H-3]MK-801 binding sites in postmortem human brain
The pharmacological specificity and the regional distribution of the N-methyl-D-aspartate receptor-associated 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5, 10-imine maleate (MK-801) binding sites in human postmortem brain tissue were determined by binding studies using (+)-[3H]MK-801. Scatchard analysis revealed a high-affinity (KD= 0.9 ± 0.2 nM, Bmax= 499 ± 33 fmol/mg of protein) and a low-affinity (KD= 3.6 ± 0.9 nM, Bmax= 194 ± 44 fmol/ mg of protein) binding site. The high-affinity site showed a different regional distribution of receptor density (cortex > hippocampus > striatum) compared to the low-affinity binding site (cerebellum > brainstem). The rank order pharmacological specificity and stereoselectivity of the high-(cortex) and low-(cerebellar) affinity binding sites were identical. However, all compounds tested showed greater potency at the high-affinity site in cortex. The results indicate that (+)[3H]MK-801 binding in human postmortem brain tissue shows pharmacological and regional specificity.
0022-3042
1163-1168
Quarum, Merrit L.
42c39c87-e5d5-4a86-93fa-f170d5a294fd
Parker, Joel D.
31d7a4f1-e316-43da-9d09-c183b5388eb5
Keana, John F. W.
5ec48cc7-d3d5-4a2d-9492-10d3e2c03569
Weber, Eckard
bc457f54-ee84-4be8-af09-5da53b0807f4
Quarum, Merrit L.
42c39c87-e5d5-4a86-93fa-f170d5a294fd
Parker, Joel D.
31d7a4f1-e316-43da-9d09-c183b5388eb5
Keana, John F. W.
5ec48cc7-d3d5-4a2d-9492-10d3e2c03569
Weber, Eckard
bc457f54-ee84-4be8-af09-5da53b0807f4

Quarum, Merrit L., Parker, Joel D., Keana, John F. W. and Weber, Eckard (1990) (+)-[H-3]MK-801 binding sites in postmortem human brain. Journal of Neurochemistry, 54 (4), 1163-1168. (doi:10.1111/j.1471-4159.1990.tb01944.x).

Record type: Article

Abstract

The pharmacological specificity and the regional distribution of the N-methyl-D-aspartate receptor-associated 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5, 10-imine maleate (MK-801) binding sites in human postmortem brain tissue were determined by binding studies using (+)-[3H]MK-801. Scatchard analysis revealed a high-affinity (KD= 0.9 ± 0.2 nM, Bmax= 499 ± 33 fmol/mg of protein) and a low-affinity (KD= 3.6 ± 0.9 nM, Bmax= 194 ± 44 fmol/ mg of protein) binding site. The high-affinity site showed a different regional distribution of receptor density (cortex > hippocampus > striatum) compared to the low-affinity binding site (cerebellum > brainstem). The rank order pharmacological specificity and stereoselectivity of the high-(cortex) and low-(cerebellar) affinity binding sites were identical. However, all compounds tested showed greater potency at the high-affinity site in cortex. The results indicate that (+)[3H]MK-801 binding in human postmortem brain tissue shows pharmacological and regional specificity.

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Published date: April 1990

Identifiers

Local EPrints ID: 143687
URI: https://eprints.soton.ac.uk/id/eprint/143687
ISSN: 0022-3042
PURE UUID: 1a7bbc9a-c207-4973-8d7e-f331cbcb57c2

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Date deposited: 21 Jul 2010 10:40
Last modified: 18 Jul 2017 23:09

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