CNS putative L-prolyl-L-leucyl-glycinamide (PLG) receptors, brain and lymphocyte dopamine receptors

Simon Chiu; James A. Ferris; Rodney L Johnson; Ram K. Mishra

doi:10.1016/S0278-5846(82)80108-5

CNS putative L-prolyl-L-leucyl-glycinamide (PLG) receptors, brain and lymphocyte dopamine receptors

Simon Chiu, James A. Ferris, Rodney L Johnson, Ram K. Mishra

Medicinal Chemistry

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

19 Scopus citations

Abstract

Abstract1.In view of previously demonstrated modulatory effects of PLG on the sensitivity of central dopamine receptors, we developed a radioligand binding assay to identify specific binding sites of PLG in rat and normal human brain.2.³H-PLG binds specifically to rat striatum exhibiting high affinity (K_D = 4.69 ± 0.50 nM) saturability (B_max = 9.20 ± 0.30 fmoles/mg protein) and reversibility; the highest density of specific PLG binding sites occurring in the striatum, followed by the hypothalamus and cerebral cortex.3.Saturable, high-affinity binding sites of PLG were identified in human striatum. The substantia nigra was enriched with the highest level of specific PLG binding sites.4.Dopamine receptors were identified in human lymphocytes.5.The results are compatible with the hypothesis that differential modulation of CNS dopamine receptors by PLG is functionally associated with interacting with specific PLG binding sites in the rat and human brain, and pose implications for Parkinson's disease and tardive dyskinesia.

Original language	English (US)
Pages (from-to)	365-368
Number of pages	4
Journal	Progress in Neuropsychopharmacology and Biological Psychiatry
Volume	6
Issue number	4-6
DOIs	https://doi.org/10.1016/S0278-5846(82)80108-5
State	Published - 1982

Bibliographical note

Funding Information:
This study was supported by the Medical Research Council (Canada) and the Ontario Mental Health Foundation. Gifts of drugs from Ayerst Co., Janssen Pharmaceutica, Endo Laboratories are gratefully acknowledged. S. Chiu would like to thank Burroughs Wellcome (Canada), Ciba-Geigy and the Medical Research Council of Canada for the award of research studentship.

Keywords

L-Prolyl-L-Leucyl-Glycinamide
dopamine receptors
lymphocytes
striatum

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title = "CNS putative L-prolyl-L-leucyl-glycinamide (PLG) receptors, brain and lymphocyte dopamine receptors",

abstract = "Abstract1.In view of previously demonstrated modulatory effects of PLG on the sensitivity of central dopamine receptors, we developed a radioligand binding assay to identify specific binding sites of PLG in rat and normal human brain.2.3H-PLG binds specifically to rat striatum exhibiting high affinity (KD = 4.69 ± 0.50 nM) saturability (Bmax = 9.20 ± 0.30 fmoles/mg protein) and reversibility; the highest density of specific PLG binding sites occurring in the striatum, followed by the hypothalamus and cerebral cortex.3.Saturable, high-affinity binding sites of PLG were identified in human striatum. The substantia nigra was enriched with the highest level of specific PLG binding sites.4.Dopamine receptors were identified in human lymphocytes.5.The results are compatible with the hypothesis that differential modulation of CNS dopamine receptors by PLG is functionally associated with interacting with specific PLG binding sites in the rat and human brain, and pose implications for Parkinson's disease and tardive dyskinesia.",

keywords = "L-Prolyl-L-Leucyl-Glycinamide, dopamine receptors, lymphocytes, striatum",

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note = "Funding Information: This study was supported by the Medical Research Council (Canada) and the Ontario Mental Health Foundation. Gifts of drugs from Ayerst Co., Janssen Pharmaceutica, Endo Laboratories are gratefully acknowledged. S. Chiu would like to thank Burroughs Wellcome (Canada), Ciba-Geigy and the Medical Research Council of Canada for the award of research studentship.",

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AU - Johnson, Rodney L

AU - Mishra, Ram K.

N1 - Funding Information: This study was supported by the Medical Research Council (Canada) and the Ontario Mental Health Foundation. Gifts of drugs from Ayerst Co., Janssen Pharmaceutica, Endo Laboratories are gratefully acknowledged. S. Chiu would like to thank Burroughs Wellcome (Canada), Ciba-Geigy and the Medical Research Council of Canada for the award of research studentship.

PY - 1982

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N2 - Abstract1.In view of previously demonstrated modulatory effects of PLG on the sensitivity of central dopamine receptors, we developed a radioligand binding assay to identify specific binding sites of PLG in rat and normal human brain.2.3H-PLG binds specifically to rat striatum exhibiting high affinity (KD = 4.69 ± 0.50 nM) saturability (Bmax = 9.20 ± 0.30 fmoles/mg protein) and reversibility; the highest density of specific PLG binding sites occurring in the striatum, followed by the hypothalamus and cerebral cortex.3.Saturable, high-affinity binding sites of PLG were identified in human striatum. The substantia nigra was enriched with the highest level of specific PLG binding sites.4.Dopamine receptors were identified in human lymphocytes.5.The results are compatible with the hypothesis that differential modulation of CNS dopamine receptors by PLG is functionally associated with interacting with specific PLG binding sites in the rat and human brain, and pose implications for Parkinson's disease and tardive dyskinesia.

AB - Abstract1.In view of previously demonstrated modulatory effects of PLG on the sensitivity of central dopamine receptors, we developed a radioligand binding assay to identify specific binding sites of PLG in rat and normal human brain.2.3H-PLG binds specifically to rat striatum exhibiting high affinity (KD = 4.69 ± 0.50 nM) saturability (Bmax = 9.20 ± 0.30 fmoles/mg protein) and reversibility; the highest density of specific PLG binding sites occurring in the striatum, followed by the hypothalamus and cerebral cortex.3.Saturable, high-affinity binding sites of PLG were identified in human striatum. The substantia nigra was enriched with the highest level of specific PLG binding sites.4.Dopamine receptors were identified in human lymphocytes.5.The results are compatible with the hypothesis that differential modulation of CNS dopamine receptors by PLG is functionally associated with interacting with specific PLG binding sites in the rat and human brain, and pose implications for Parkinson's disease and tardive dyskinesia.

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CNS putative L-prolyl-L-leucyl-glycinamide (PLG) receptors, brain and lymphocyte dopamine receptors

Abstract

Bibliographical note

Keywords

UN SDGs

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