The interaction between neuroactive steroids and the σ1 receptor function: behavioral consequences and therapeutic opportunities

The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.

1976 • 2,883 citations

Age Changes and Sex Differences in Serum Dehydroepiandrosterone Sulfate Concentrations throughout Adulthood

1984 • 1,345 citations

Norepinephrine in Depressive Reactions

1965 • 1,127 citations

Stress-induced elevations of gamma-aminobutyric acid type A receptor-active steroids in the rat brain.

1991 • 943 citations

Purification, molecular cloning, and expression of the mammalian sigma1-binding site.

1996 • 880 citations

Neurosteroids: Biosynthesis and Function of These Novel Neuromodulators

2000 • 807 citations

Functional antagonists at the NMDA receptor complex exhibit antidepressant actions

1990 • 754 citations

A proposal for the classification of sigma binding sites

1992 • 743 citations

Increase in the cerebrospinal fluid content of neurosteroids in patients with unipolar major depression who are receiving fluoxetine or fluvoxamine

1998 • 658 citations

Characterization and measurement of dehydroepiandrosterone sulfate in rat brain.

1981 • 645 citations

Steroid Binding at σ Receptors Suggests a Link Between Endocrine, Nervous, and Immune Systems

1988 • 531 citations

Neurosteroids: A new brain function?

1990 • 526 citations

Amnesia induced in mice by centrally administered β-amyloid peptides involves cholinergic dysfunction

1996 • 503 citations

Effects of Antidepressant Treatment on Neuroactive Steroids in Major Depression

1998 • 445 citations

Dehydroepiandrosterone (DHEA) and DHEA-sulfate (DHEAS) protect hippocampal neurons against excitatory amino acid-induced neurotoxicity

1998 • 444 citations

The neurosteroid dehydroepiandrosterone sulfate is an allosteric antagonist of the GABAA receptor

1990 • 433 citations

Neurosteroids, via sigma receptors, modulate the [3H]norepinephrine release evoked by N-methyl-D-aspartate in the rat hippocampus.

1995 • 426 citations

Rat liver and kidney contain high densities of σ1 and σ2 receptors: characterization by ligand binding and photoaffinity labeling

1994 • 423 citations

Double-Blind Treatment of Major Depression With Dehydroepiandrosterone

1999 • 411 citations

Cloning and Functional Expression of the Human Type 1 Sigma Receptor (hSigmaR1)

1996 • 409 citations

Evidence for sigma opioid receptor: binding of [3H]SKF-10047 to etorphine-inaccessible sites in guinea-pig brain.

1982 • 409 citations

Autoradiographic localization of sigma receptor binding sites in guinea pig and rat central nervous system with (+)3H-3-(3-hydroxyphenyl)-N-(1- propyl)piperidine

1986 • 385 citations

Pregnenolone and its sulfate ester in the rat brain

1983 • 382 citations

A sigma-like binding site in rat pheochromocytoma (PC12) cells: decreased affinity for (+)-benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain

1990 • 376 citations

Neurosteroids: Biosynthesis of Pregnenolone and Progesterone in Primary Cultures of Rat Glial Cells*

1989 • 372 citations

Anesthetic Effect of Steroid Hormones.

1941 • 363 citations

Sigma opiates and certain antipsychotic drugs mutually inhibit (+)-[3H] SKF 10,047 and [3H]haloperidol binding in guinea pig brain membranes.

1984 • 348 citations

Immunocytochemical localization of the sigma1 receptor in the adult rat central nervous system

2000 • 346 citations

Pharmacological and autoradiographic discrimination of sigma and phencyclidine receptor binding sites in brain with (+)-[3H]SKF 10,047, (+)-[3H]-3-[3-hydroxyphenyl]-N-(1-propyl)piperidine and [3H]-1-[1-(2-thienyl)cyclohexyl]piperidine.

1986 • 339 citations

Relationship between symptom severity and steroid variation in women with premenstrual syndrome: study on serum pregnenolone, pregnenolone sulfate, 5 alpha-pregnane-3,20-dione and 3 alpha-hydroxy-5 alpha-pregnan-20-one.

1996 • 334 citations

Fluoxetine-elicited changes in brain neurosteroid content measured by negative ion mass fragmentography.

1996 • 329 citations

Dehydroepiandrosterone (DHEA) treatment of depression

1997 • 317 citations

Regulating ankyrin dynamics: Roles of sigma-1 receptors

2001 • 305 citations

Time-Dependent Changes in Rat Brain Neuroactive Steroid Concentrations and GABA<sub>A</sub> Receptor Function after Acute Stress

1996 • 303 citations

Neurosteroids: Deficient cognitive performance in aged rats depends on low pregnenolone sulfate levels in the hippocampus

1997 • 299 citations

Potentiation of neuronal NMDA response induced by dehydroepiandrosterone and its suppression by progesterone: effects mediated via sigma receptors

1996 • 296 citations

Neurosteroids: oligodendrocyte mitochondria convert cholesterol to pregnenolone.

1987 • 294 citations

Cloning and Functional Characterization of a σ Receptor from Rat Brain

1998 • 288 citations

Ca(2+) signaling via sigma(1)-receptors: novel regulatory mechanism affecting intracellular Ca(2+) concentration.

2000 • 287 citations

Sigma1 (σ1) receptor agonists and neurosteroids attenuate β25–35-amyloid peptide-induced amnesia in mice through a common mechanism

1998 • 280 citations

Classification and nomenclature of phencyclidine and sigma receptor sites

1987 • 272 citations

Neurosteroids: biochemistry, modes of action, and clinical relevance.

1994 • 271 citations

Dehydroepiandrosterone sulfate improves memory in aging mice

1988 • 262 citations

Sigma receptors: recent advances and new clinical potentials

2000 • 239 citations

Dehydroepiandrosterone and its sulfate enhance memory retention in mice

1988 • 232 citations

Pregnenolone sulfate potentiation of N-methyl-D-aspartate receptor channels in hippocampal neurons.

1993 • 223 citations

Antischizophrenic drugs of the diphenylbutylpiperidine type act as calcium channel antagonists.

1983 • 219 citations

Neuroactive steroids: potential therapeutic use in neurological and psychiatric disorders

1999 • 216 citations

Infusion of neurosteroids into the nucleus basalis magnocellularis affects cognitive processes in the rat

1993 • 214 citations

Distinct Sites for Inverse Modulation ofN-Methyl-d-Aspartate Receptors by Sulfated Steroids

1997 • 211 citations

Behavioral evidence for a modulating role of σ ligands in memory processes. I. Attenuation of dizocilpine (MK-801)-induced amnesia

1994 • 211 citations

Neuroprotective and anti-amnesic potentials of sigma (σ) receptor ligands

1997 • 209 citations

Cloning and Structural Analysis of the cDNA and the Gene Encoding the Murine Type 1 Sigma Receptor

1997 • 199 citations

Naltrexone fails to antagonize the σ effects of PCP and SKF 10,047 in the dog

1983 • 187 citations

The effects of inhibitors of GABAergic transmission and stress on brain and plasma allopregnanolone concentrations

1997 • 184 citations

Neuroactive Neurosteroids as Endogenous Effectors for the Sigma1 (.SIGMA.1) Receptor. Pharmacological Evidence and Therapeutic Opportunities.

1999 • 181 citations

Autoradiographic visualization of haloperidol-sensitive sigma receptors in guinea-pig brain

1988 • 176 citations

Pregnenolone sulfate enhances post-training memory processes when injected in very low doses into limbic system structures: the amygdala is by far the most sensitive.

1995 • 172 citations

Intracellular σ ₁ receptor modulates phospholipase C and protein kinase C activities in the brainstem

1999 • 166 citations

Exon‐Intron Structure, Analysis of Promoter Region, and Chromosomal Localization of the Human Type 1 σ Receptor Gene

1998 • 161 citations

Pregnenolone sulfate augments NMDA receptor mediated increases in intracellular Ca2+ in cultured rat hippocampal neurons

1992 • 154 citations

Relationship between symptom severity and steroid variation in women with premenstrual syndrome: study on serum pregnenolone, pregnenolone sulfate, 5 alpha-pregnane-3,20-dione and 3 alpha-hydroxy-5 alpha- pregnan-20-one

1996 • 153 citations

Cloning and Characterization of a Mouse σ₁ Receptor

1998 • 149 citations

3 alpha-Hydroxy-5 beta-pregnan-20-one sulfate: a negative modulator of the NMDA-induced current in cultured neurons.

1994 • 142 citations

Steroid hormones as mediators of neural plasticity

1991 • 139 citations

Sigma (σ1) receptor mediated antidepressant-like effects of neurosteroids in the Porsolt forced swim test

1998 • 138 citations

Neurosteroids: biochemistry, modes of action, and clinical relevance

1994 • 137 citations

Potential antipsychotic BMY 14802 selectively binds to sigma sites

1987 • 128 citations

The neurosteroid pregnenolone sulfate blocks NMDA antagonist-induced deficits in a passive avoidance memory task

1994 • 126 citations

Dehydroepiandrosterone sulfate attenuates dizocilpine-induced learning impairment in mice via σ1-receptors

1997 • 125 citations

Marked Decrease of Plasma Neuroactive Steroids During Alcohol Withdrawal

1996 • 124 citations

PRE-084, a σ selective PCP derivative, attenuates MK-801-induced impairment of learning in mice

1994 • 123 citations

σ1 Receptor subtype is involved in the relief of behavioral despair in the mouse forced swimming test

1996 • 119 citations

Neuroleptic-sensitive binding sites in the nigrostriatal system: evidence for differential distribution of sigma sites in the substantia nigra, pars compacta of the cat.

1989 • 116 citations

Neuroprotective activity of a new class of steroidal inhibitors of the N -methyl- <scp>d</scp> -aspartate receptor

1997 • 114 citations

Biosynthesis and assay of neurosteroids in rats and mice: Functional correlates

1995 • 109 citations

Neuroprotection by dehydroepiandrosteronesulfate

1998 • 109 citations

Neuroleptic-sensitive binding sites in the nigrostriatal system: evidence for differential distribution of sigma sites in the substantia nigra, pars compacta of the cat

1989 • 108 citations

The modulation by neurosteroids of the scopolamine-induced learning impairment in mice involves an interaction with sigma1 (σ1) receptors

1998 • 108 citations

Stress-induced increase in brain neuroactive steroids: Antagonism by abecarnil

1996 • 106 citations

Sigma receptor ligands modulate contractility, Ca++ influx and beating rate in cultured cardiac myocytes.

1994 • 106 citations

CSF neuroactive steroids in affective disorders: Pregnenolone, progesterone, and DBI

1994 • 103 citations

Neurosteroids: Molecular mechanisms of action and psychopharmacological significance

1996 • 99 citations

Sigma binding states in the brain; An emerging concept for multiple sites and their relevance for psychiatric disorders

1990 • 99 citations

Drug specificity of pharmacological dystonia

1990 • 97 citations

Modulation by neurosteroids of the in vivo (+)-[3H]SKF-10,047 binding to ?1 receptors in the mouse forebrain

1996 • 97 citations

Neurosteroid modulation of native and recombinant GABAA receptors

1996 • 96 citations

The effects of neurosteroids on acquisition and retention of a modified passive-avoidance learning task in mice

1998 • 91 citations

Differential regulation of σ and PCP receptors after chronic administration of haloperidol and phencyclidine in mice

1989 • 91 citations

SA4503, a novel cognitive enhancer with σ1 receptor agonist properties, facilitates NMDA receptor-dependent learning in mice

1997 • 89 citations

The neurosteroid pregnenolone sulfate blocks deficits induced by a competitive NMDA antagonist in active avoidance and lever-press learning tasks in mice

1996 • 89 citations

Multiple affinity binding states of the sigma receptor: effect of GTP-binding protein-modifying agents.

1989 • 85 citations

Neurosteroids and Brain Function

2001 • 81 citations

Stress and neurosteroids in adult and aged rats

1998 • 80 citations

Beneficial Effects of Acute and Repeated Administrations of σ Receptor Agonists on Behavioral Despair in Mice Exposed to Tail Suspension

1998 • 76 citations

Regulating ankyrin dynamics: Roles of sigma-1 receptors

2001 • 76 citations

Purification and Characterization of the Human SR 31747A-binding Protein

1997 • 76 citations

The neurosteroid pregnenolone sulfate reduces learning deficits induced by scopolamine and has promnestic effects in mice performing an appetitive learning task

1996 • 74 citations

Steroid synthesis in rat brain cell cultures

1989 • 73 citations

Screen of receptor and uptake-site activity of hypericin component of St. John's wort reveals σ receptor binding

1998 • 71 citations

Pregnenolone sulfate antagonizes dizocilpine amnesia

1995 • 69 citations

SA4503, a novel cognitive enhancer, with σ1 receptor agonistic properties

1997 • 68 citations

Electrophysiological and binding studies on intact NCB-20 cells suggest presence of a low affinity sigma receptor.

1991 • 68 citations

Evidence for an anti-amnesic effect of JO 1784 in the rat: a potent and selective ligand for the sigma receptor

1991 • 67 citations

Solubilization and characterization of haloperidol-sensitive (+)-[3H]SKF-10,047 binding sites (sigma sites) from rat liver membranes.

1991 • 66 citations

Ameliorating effects of σ receptor ligands on the impairment of passive avoidance tasks in mice: involvement in the central acetylcholinergic system

1994 • 65 citations

Pregnenolone sulfate increases the convulsant potency of N-methyl-D-aspartate in mice

1992 • 64 citations

Pregnenolone sulfate exacerbates NMDA-induced death of hippocampal neurons

1998 • 58 citations

Reversion of β25–35-amyloid peptide-induced amnesia by NMDA receptor-associated glycine site agonists

1996 • 57 citations

Neurosteroids Ameliorate Conditioned Fear Stress An Association with Sigma1 Receptors

2000 • 56 citations

Mitochondrial diazepam-binding inhibitor receptor complex agonists antagonize dizocilpine amnesia: putative role for allopregnanolone.

1994 • 54 citations

Severity of depression in abstinent alcoholics is associated with monoamine metabolites and dehydroepiandrosterone-sulfate concentrations

1999 • 54 citations

Dehydroepiandrosterone Decreases Behavioral Despair in High-but not Low-Anxiety Rats

1997 • 53 citations

Modulation of steroidal levels by adrenalectomy/castration and inhibition of neurosteroid synthesis enzymes affect σ₁ receptor‐mediated behaviour in mice

1999 • 51 citations

Autoradiographic distribution of phencyclidine receptors in the rat brain using [3H]1-(1-(2-thienyl)cyclohexyl)piperidine ([3H]TCP)

1986 • 50 citations

High affinity dextromethorphan binding sites in guinea pig brain: further characterization and allosteric interactions.

1988 • 49 citations

Pregnenolone—from selye to Alzheimer and a model of the pregnenolone sulfate binding site on the GABAA receptor

1995 • 48 citations

Effects of Hypericum perforatum Extract on Ethanol Intake, and on Behavioral Despair

2000 • 45 citations

Similar ameliorating effects of benzomorphans and 5-HT2 antagonists on drug-induced impairment of passive avoidance response in mice: comparison with acetylcholinesterase inhibitors

1993 • 43 citations

The anti-amnesic effects of sigma1 (σ1) receptor agonists confirmed by in vivo antisense strategy in the mouse

2001 • 43 citations

(+)-SKF-10,047 and dextromethorphan ameliorate conditioned fear stress through the activation of phenytoin-regulated σ1 sites

1996 • 40 citations

N‐メチル‐D‐アスパラギン酸レセプターの新規ステロイド阻害剤の神経保護効果

1997 • 40 citations

Relationship between Sigma-like site and progesterone-binding site of adult male rat liver microsomes

1994 • 40 citations

Are high-affinity progesterone binding site(s) from porcine liver microsomes members of the σ receptor family?

1998 • 40 citations

NE-100, a novel sigma receptor ligand: Effect on phencyclidine-induced behaviors in rats, dogs and monkeys

1994 • 39 citations

σ Receptor ligands (+)-SKF10,047 and SA4503 improve dizocilpine-induced spatial memory deficits in rats

1998 • 39 citations

Intrahippocampal administration of (+)-SKF 10,047, a σ ligand, reverses MK-801-induced impairment of working memory in rats

1995 • 36 citations

Inhibition of rubral neurons by a specific ligand for σ receptors

1988 • 32 citations

Is the σ2 receptor in rat brain related to the K+ channel of class III antiarrhythmic drugs?

1993 • 30 citations

Differential effect of dehydroepiandrosterone and its steroid precursor pregnenolone against the behavioural deficits in CO-exposed mice

2000 • 29 citations

Ameliorative Effect of SA4503, a Novel Cognitive Enhancer, on the Basal Forebrain Lesion-Induced Impairment of the Spatial Learning Performance in Rats

1998 • 29 citations

Pregnenolone sulfate modulates NMDA receptors, inducing and potentiating acute excitotoxicity in isolated retina

1998 • 29 citations

Down-regulation of sigma receptors by chronic haloperidol.

1990 • 25 citations

Haloperidol blocks voltage-activated Ca2+ channels in hippocampal neurones

1994 • 22 citations

Effects of haloperidol and reduced haloperidol on binding to σ sites

1994 • 22 citations

σ2 Site-mediated inhibition of electrically evoked guinea pig ileum longitudinal muscle/myenteric plexus contractions

1995 • 21 citations

Comparative potencies of calcium channel antagonists and antischizophrenic drugs on central and peripheral calcium channel binding sites

1985 • 19 citations

Central action of σ receptor ligand, JO 1784, to suppress CRF-induced inhibition of gastric function in conscious rats

1992 • 8 citations

Effect of 1,3-di-o-tolylguanidine (DTG), rimcazole and EMD 57445, the sigma receptor ligands, in the forced swimming test.

1998 • 7 citations

Antidepressant effect of OPC-14823 in the forced swimming test in mice

1997 • 5 citations

Antidepressant effect of OPC-14523 in the forced swimming test in mice

1997 • 4 citations