Dopamine receptors in human brain: Autoradiographic distribution of D1 sites

The distribution of dopamine D1 receptors has been determined in post mortem human brain tissues using in vitro receptor autoradiography, with ([3H]N-methyl) SCH 23390 as ligand. The highest densities of dopamine D1 sites were seen in the nucleus caudatus, putamen, globus pallidus pars medialis and substantia nigra. Intermediate densities were associated with the amygdala, mammillary bodies, cerebral cortex and CA1. The remaining part of the hippocampus as well as the diencephalon, brainstem and cerebellum contained low levels of [3H]SCH 23390 binding sites. The distribution of D1 receptors in the human brain closely resembles that reported for the rat brain. In addition, there was a good correlation between the anatomical localization of D1 sites and the distribution of dopaminergic nerve terminals in the central nervous system. The densities of D1 receptors in the human brain were observed to markedly decrease with age during the first decades of life. However, no further modifications were found beyond the age of 40 years. We did not observe any significant influence of other parameters such as gender and post mortem delay in our samples.

[1]  O. Hornykiewicz 9 – Dopamine and Its Physiological Significance in Brain Function , 1972 .

[2]  O. Hornykiewicz,et al.  OCCURRENCE AND DISTRIBUTION OF AROMATIC l‐AMINO ACID (l‐DOPA) DECARBOXYLASE IN THE HUMAN BRAIN , 1972, Journal of neurochemistry.

[3]  Michael J. Schmidt,et al.  Cyclic AMP and cyclic GMP accumulation in vitro in brain regions of young, old and aged rats , 1978, Brain Research.

[4]  M. Starr,et al.  Differential effects of dopamine D1 and D2 agonists and antagonists on velocity of movement, rearing and grooming in the mouse Implications for the roles of D1 and D2 receptors , 1986, Neuropharmacology.

[5]  F E Bloom,et al.  Central catecholamine neuron systems: anatomy and physiology of the dopamine systems. , 1978, Annual review of neuroscience.

[6]  J. Palacios,et al.  Mapping receptors in the human brain , 1986, Trends in Neurosciences.

[7]  B. Berger,et al.  Tyrosine hydroxylase and methionine-enkephalin in the human mesencephalon Immunocytochemical localization and relationships , 1983, Journal of the Neurological Sciences.

[8]  P. Davies,et al.  REGIONAL DISTRIBUTION OF ENZYMES ASSOCIATED WITH NEUROTRANSMISSION BY MONOAMINES, ACETYLCHOLINE AND GABA IN THE HUMAN BRAIN , 1978, Journal of neurochemistry.

[9]  P. Mcgeer,et al.  Aging and extrapyramidal function. , 1977, Archives of neurology.

[10]  J. Waddington,et al.  Sniffing, rearing and locomotor responses to the D-1 dopamine agonist R-SK&F 38393 and to apomorphine: differential interactions with the selective D-1 and D-2 antagonists SCH 23390 and metoclopramide. , 1985, European journal of pharmacology.

[11]  J. Pearson,et al.  Human brainstem catecholamine neuronal anatomy as indicated by immunocytochemistry with antibodies to tyrosine hydroxylase , 1983, Neuroscience.

[12]  Jan Voogd,et al.  The human central nervous system : a synopsis and atlas , 1978 .

[13]  J. Larsen,et al.  Pharmacological effects of a specific dopamine D-1 antagonist SCH 23390 in comparison with neuroleptics. , 1984, Life sciences.

[14]  J. C. Stoof,et al.  Two dopamine receptors: biochemistry, physiology and pharmacology. , 1984, Life sciences.

[15]  P. Mcgeer,et al.  Aging and neurotransmitter systems. , 1980, Advances in biochemical psychopharmacology.

[16]  H. Sarau,et al.  Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines. , 1980, Journal of medicinal chemistry.

[17]  C. Finch,et al.  [3H]Fluphenazine Binding to Brain Membranes: Simultaneous Measurement of D‐1 and D‐2 Receptor Sites , 1986, Journal of neurochemistry.

[18]  J. Hyttel Similarities between the binding of 3H-piflutixol and 3H-flupentixol to rat striatal dopamine receptors in vitro. , 1981, Life sciences.

[19]  J. Hyttel Functional evidence for selective dopamine D-1 receptor blockade by SCH 23390 , 1984, Neuropharmacology.

[20]  J. Kebabian,et al.  The D1 dopamine receptor: new perspectives , 1986 .

[21]  A. Barnett,et al.  SCH 23390, a potential benzazepine antipsychotic with unique interactions on dopaminergic systems. , 1983, The Journal of pharmacology and experimental therapeutics.

[22]  P. Beart,et al.  Characteristics of D-1 dopamine receptors labelled by [3H]fluphenazine in homogenates of rat neostriatum , 1985, Neuroscience Letters.

[23]  J. Waddington,et al.  Kainic acid lesions dissociate [3H] spiperone and [3H]cis-flupenthixol binding sites in rat striatum. , 1981, European journal of pharmacology.

[24]  E. Spokes,et al.  Neurochemical alterations in Huntington's chorea: a study of post-mortem brain tissue. , 1980, Brain : a journal of neurology.

[25]  S. Wyrick,et al.  [3H]SCH23390 has the characteristics of a dopamine receptor ligand in the rat central nervous system. , 1984, European journal of pharmacology.

[26]  J. Hyttel SCH 23390 - the first selective dopamine D-1 antagonist. , 1983, European journal of pharmacology.

[27]  J. C. Stoof,et al.  Opposing roles for D-1 and D-2 dopamine receptors in efflux of cyclic AMP from rat neostriatum , 1981, Nature.

[28]  T. Dawson,et al.  D-1 dopamine receptors in the rat brain: autoradiographic localization using [3H]SCH 23390. , 1985, European journal of pharmacology.

[29]  J. Kebabian,et al.  Multiple receptors for dopamine , 1979, Nature.

[30]  P. Mcgeer,et al.  DISTRIBUTION OF TYROSINE HYDROXYLASE IN HUMAN AND ANIMAL BRAIN 1 , 1971, Journal of neurochemistry.

[31]  B. Berger,et al.  Dopamine and methionine-enkephalin in human brain , 1982, Neuroscience Letters.

[32]  F. Owen,et al.  Characteristics of 3H-cis-flupenthixol binding to calf brain membranes. , 1980, European journal of pharmacology.

[33]  G. Gessa,et al.  Selective blockade of dopamine D-1 receptors by SCH 23390 discloses striatal dopamine D-2 receptors mediating the inhibition of adenylate cyclase in rats. , 1984, European journal of pharmacology.

[34]  G. Reynolds,et al.  [3H]SCH 23390 labeled D1 dopamine receptors are unchanged in schizophrenia and Parkinson's disease. , 1985, European journal of pharmacology.

[35]  C. Marsden,et al.  The dopamine D2 agonist LY 141865, but not the D1 agonist SKF 38393, reverses parkinsonism induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in the common marmoset , 1985, Neuroscience Letters.

[36]  B. Berger,et al.  Catecholaminergic innervation of the septal area in man: Immunocytochemical study using TH and DBH antibodies , 1985, The Journal of comparative neurology.

[37]  O. Bugiani,et al.  Nerve cell loss with aging in the putamen. , 1978, European neurology.

[38]  B. Berger Histochemical identification and localization of dopaminergic axons in rat and human cerebral cortex. , 1977, Advances in biochemical psychopharmacology.

[39]  P. Seeman Brain dopamine receptors. , 1980, Pharmacological reviews.

[40]  J. Waddington,et al.  Loss of rat striatal dopamine receptors with ageing is selective for D-2 but not D-1 sites: association with increased non-specific binding of the D-1 ligand [3H]piflutixol. , 1984, European journal of pharmacology.

[41]  B. Bogerts A brainstem atlas of catecholaminergic neurons in man, using melanin as a natural marker , 1981, The Journal of comparative neurology.

[42]  E. Ongini,et al.  Stimulation of dopamine D-1 receptors by SKF 38393 induces EEG desynchronization and behavioral arousal. , 1985, Life sciences.

[43]  M. Savasta,et al.  Autoradiographic distribution of the D1 agonist [3H]SKF 38393, in the rat brain and spinal cord. Comparison with the distribution of D2 dopamine receptors , 1986, Neuroscience.

[44]  L. Volicer,et al.  Effect of aging on cyclic AMP levels and adenylate cyclase and phosphodiesterase activities in the rat corpus striatum , 1977, Mechanisms of Ageing and Development.

[45]  H. Sarau,et al.  The central effects of a novel dopamine agonist. , 1978, European journal of pharmacology.

[46]  J. Hyttel,et al.  Differential inhibition by dopamine D-1 and D-2 antagonists of circling behaviour induced by dopamine agonists in rats with unilateral 6-hydroxydopamine lesions. , 1984, European journal of pharmacology.

[47]  J. Rinne,et al.  Dopamine D-1 receptors in the parkinsonian brain , 1985, Brain Research.

[48]  D. Sibley,et al.  The classification of dopamine receptors: relationship to radioligand binding. , 1983, Annual review of neuroscience.

[49]  T. Dawson,et al.  D-1 dopamine receptors in the rat brain: a quantitative autoradiographic analysis , 1986, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[50]  O. DeJesus,et al.  Positron tomography of a radio-brominated analog of the D1/DA1 antagonist, SCH 23390. , 1985, European journal of pharmacology.

[51]  H. Sarau,et al.  Binding of a novel dopaminergic agonist radioligand [3H]-fenoldopam (SKF 82526) to D-1 receptors in rat striatum. , 1985, Life sciences.

[52]  J. Palacios,et al.  Dopamine receptors in human brain: Autoradiographic distribution of D2 sites , 1989, Neuroscience.

[53]  P. H. Andersen,et al.  Specific binding of 3H-SCH 23390 to dopamine D1 receptors in vivo. , 1986, Life sciences.

[54]  Y. Agid,et al.  Binding of [3H]SCH 23390 to D-1 receptors in the putamen of control and parkinsonian subjects. , 1985, European journal of pharmacology.

[55]  A. Barnett,et al.  Characterization of the binding of 3H-SCH 23390, a selective D-1 receptor antagonist ligand, in rat striatum. , 1984, Life sciences.

[56]  I. Creese,et al.  Guanine nucleotide regulation of agonist interactions at [3H]SCH23390-labeled D1 dopamine receptors in rat striatum. , 1986, European journal of pharmacology.

[57]  P. Davies,et al.  REGIONAL DISTRIBUTION OF MONOAMINES AND THEIR METABOLITES IN THE HUMAN BRAIN , 1978, Journal of neurochemistry.

[58]  M. Savasta,et al.  Autoradiographic localization of D1 dopamine receptors in the rat brain with [3H]SCH 23390 , 1986, Brain Research.

[59]  J. Palacios,et al.  Quantitative light microscopic autoradiographic localization of cholinergic muscarinic receptors in the human brain: Brainstem , 1984, Neuroscience.