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Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
Bioorganic & medicinal chemistry 20120815
-
Characterization of ligand binding to the σ(1) receptor in a human tumor cell line (RPMI 8226) and establishment of a competitive receptor binding assay.
Assay and drug development technologies 20120801
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Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance.
European journal of medicinal chemistry 20120701
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Thiophene bioisosteres of spirocyclic σ receptor ligands: relationships between substitution pattern and σ receptor affinity.
Journal of medicinal chemistry 20120614
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Effects of the sigma-1 receptor agonist 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)-piperazine dihydro-chloride on inflammation after stroke.
PloS one 20120101
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Synthesis and binding assays of novel 3,3-dimethylpiperidine derivatives with various lipophilicities as σ₁ receptor ligands.
Bioorganic & medicinal chemistry 20111215
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Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with high σ₁ receptor affinity.
Journal of medicinal chemistry 20111013
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Afobazole modulates neuronal response to ischemia and acidosis via activation of sigma-1 receptors.
The Journal of pharmacology and experimental therapeutics 20111001
-
Sigma receptor binding of tetrabenazine series tracers targeting VMAT2 in rat pancreas.
Nuclear medicine and biology 20111001
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Arylamides hybrids of two high-affinity σ2 receptor ligands as tools for the development of PET radiotracers.
European journal of medicinal chemistry 20110901
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Lack of cocaine-like discriminative-stimulus effects of σ-receptor agonists in rats.
Behavioural pharmacology 20110901
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Fluorescent derivatives of σ receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) as a tool for uptake and cellular localization studies in pancreatic tumor cells.
Journal of medicinal chemistry 20110825
-
Expression of σ receptors of human urinary bladder tumor cells (RT-4 cells) and development of a competitive receptor binding assay for the determination of ligand affinity to human σ(2) receptors.
Journal of pharmaceutical and biomedical analysis 20110715
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Synthesis of 4-(aminoalkyl) substituted 1,3-dioxanes as potent NMDA and σ receptor antagonists.
European journal of medicinal chemistry 20110601
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Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore.
European journal of medicinal chemistry 20110601
-
Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties.
Journal of medicinal chemistry 20110526
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Activation of σ-receptors induces binge-like drinking in Sardinian alcohol-preferring rats.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20110501
-
Role of sigma receptors in methamphetamine-induced neurotoxicity.
Current neuropharmacology 20110301
-
Analogues of σ receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with added polar functionality and reduced lipophilicity for potential use as positron emission tomography radiotracers.
Journal of medicinal chemistry 20110224
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Sigma receptor agonists: receptor binding and effects on mesolimbic dopamine neurotransmission assessed by microdialysis.
Biological psychiatry 20110201
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Antagonist action of progesterone at σ-receptors in the modulation of voltage-gated sodium channels.
American journal of physiology. Cell physiology 20110201
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Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols.
Bioorganic & medicinal chemistry 20101115
-
The sigma agonist 1,3-di-o-tolyl-guanidine directly blocks SK channels in dopaminergic neurons and in cell lines.
European journal of pharmacology 20100901
-
Synthesis and NMDA receptor affinity of fluorinated dioxadrol analogues.
Bioorganic & medicinal chemistry 20100601
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Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Journal of medicinal chemistry 20100527
-
Reinforcing effects of sigma-receptor agonists in rats trained to self-administer cocaine.
The Journal of pharmacology and experimental therapeutics 20100201
-
The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine.
Molecular cancer 20100101
-
Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28).
Journal of medicinal chemistry 20091210
-
Delayed treatments for stroke influence neuronal death in rat organotypic slice cultures subjected to oxygen glucose deprivation.
Neuroscience 20091201
-
Synthesis of sigma receptor ligands with unsymmetrical spiro connection of the piperidine moiety.
European journal of medicinal chemistry 20091101
-
Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.
Journal of medicinal chemistry 20091008
-
Synthesis, biological evaluation, and three-dimensional in silico pharmacophore model for sigma(1) receptor ligands based on a series of substituted benzo[d]oxazol-2(3H)-one derivatives.
Journal of medicinal chemistry 20090910
-
Synthesis of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability.
Bioorganic & medicinal chemistry 20090515
-
Voltage-gated sodium channel modulation by sigma-receptors in cardiac myocytes and heterologous systems.
American journal of physiology. Cell physiology 20090501
-
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
Journal of medicinal chemistry 20090409
-
Relationships between the structure of 6-substituted 6,8-diazabicyclo[3.2.2]nonan-2-ones and their sigma receptor affinity and cytotoxic activity.
Bioorganic & medicinal chemistry 20090215
-
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
European journal of medicinal chemistry 20090201
-
Relationships between the structure of 6-allyl-6,8-diazabicyclo[3.2.2]nonane derivatives and their sigma receptor affinity and cytotoxic activity.
Bioorganic & medicinal chemistry 20090115
-
Substituted benzo[d]oxazol-2(3H)-one derivatives with preference for the sigma1 binding site.
European journal of medicinal chemistry 20090101
-
Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity.
Journal of medicinal chemistry 20081211
-
Pharmacology and therapeutic potential of sigma(1) receptor ligands.
Current neuropharmacology 20081201
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sigma-1 receptor modulation of acid-sensing ion channel a (ASIC1a) and ASIC1a-induced Ca2+ influx in rat cortical neurons.
The Journal of pharmacology and experimental therapeutics 20081101
-
Thiophene bioisosteres of spirocyclic sigma receptor ligands. 1. N-substituted spiro[piperidine-4,4'-thieno[3,2-c]pyrans].
Journal of medicinal chemistry 20081023
-
Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure.
Bioorganic & medicinal chemistry 20080315
-
Synthesis of bridged piperazines with sigma receptor affinity.
European journal of medicinal chemistry 20071001
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Design and evaluation of naphthol- and carbazole-containing fluorescent sigma ligands as potential probes for receptor binding studies.
Journal of medicinal chemistry 20070920
-
sigma(2)-receptor ligand-mediated inhibition of inwardly rectifying K(+) channels in the heart.
The Journal of pharmacology and experimental therapeutics 20070701
-
Novel sigma receptor ligands: synthesis and biological profile.
Journal of medicinal chemistry 20070308
-
Sigma-1 receptor activation prevents intracellular calcium dysregulation in cortical neurons during in vitro ischemia.
The Journal of pharmacology and experimental therapeutics 20061201
-
Prenatal developmental toxicity study of the basic rubber accelerator, 1,3-di-o-tolylguanidine, in rats.
Reproductive toxicology (Elmsford, N.Y.) 20061101
-
Reproductive and developmental toxicity screening test of basic rubber accelerator, 1,3-di-o-tolylguanidine, in rats.
Reproductive toxicology (Elmsford, N.Y.) 20060701
-
Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503.
Synapse (New York, N.Y.) 20060501
-
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501
-
Sigma receptor activation reduces infarct size at 24 hours after permanent middle cerebral artery occlusion in rats.
Current neurovascular research 20060501
-
Prenatal cocaine alters dopamine and sigma receptor binding in nucleus accumbens and striatum in dams and adolescent offspring.
Neurotoxicology and teratology 20060101
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Dermal absorption of aromatic amines in workers with different skin lesions: a report on 4 cases.
Journal of occupational medicine and toxicology (London, England) 20060101
-
Methyl substitution on the piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as a probe for selective binding and activity at the sigma(1) receptor.
Journal of medicinal chemistry 20051229
-
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
Journal of medicinal chemistry 20050728
-
sigma Receptor activation blocks potassium channels and depresses neuroexcitability in rat intracardiac neurons.
The Journal of pharmacology and experimental therapeutics 20050601
-
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
Journal of medicinal chemistry 20050113
-
Female sex hormones decrease constitutive endothelin-1 release via endothelial sigma-1/cocaine receptors: an action independent of the steroid hormone receptors.
Endothelium : journal of endothelial cell research 20050101
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Inhibition of tumor cell proliferation by sigma ligands is associated with K+ Channel inhibition and p27kip1 accumulation.
The Journal of pharmacology and experimental therapeutics 20041201
-
Antiproliferative and cytotoxic effects of some sigma2 agonists and sigma1 antagonists in tumour cell lines.
Naunyn-Schmiedeberg's archives of pharmacology 20040801
-
Sigma-2 receptors are specifically localized to lipid rafts in rat liver membranes.
European journal of pharmacology 20040616
-
Chiral, nonracemic (piperazin-2-yl)methanol derivatives with sigma-receptor affinity.
Bioorganic & medicinal chemistry 20040615
-
4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity.
Journal of medicinal chemistry 20040422
-
Intrastriatal administration of sigma ligands inhibits basal dopamine release in vivo.
Neuropharmacology 20031201
-
Identification and pharmacological characterization of a specific agmatine transport system in human tumor cell lines.
Annals of the New York Academy of Sciences 20031201
-
Protein kinase C-dependent potentiation of intracellular calcium influx by sigma1 receptor agonists in rat hippocampal neurons.
The Journal of pharmacology and experimental therapeutics 20031101
-
Synthesis of chiral 1-[omega-(4-chlorophenoxy)alkyl]-4-methylpiperidines and their biological evaluation at sigma1, sigma2, and sterol delta8-delta7 isomerase sites.
Journal of medicinal chemistry 20030522
-
Age-related changes of the binding of [3h]SA4503 to sigma1 receptors in the rat brain.
Annals of nuclear medicine 20030201
-
Sigma1 receptor antagonists attenuate antidepressant-like effect induced by co-administration of 1,3 di-o-tolylguanidine (DTG) and memantine in the forced swimming test in rats.
Polish journal of pharmacology 20030101
-
Sigma sites mediate DTG-evoked hypothermia in rats.
Pharmacology, biochemistry, and behavior 20021101
-
Synthesis of (+)-cis-N-(4-isothiocyanatobenzyl)-N-normetazocine, an isothiocyanate derivative of N-benzylnormetazocine as acylant agent for the sigma(1) receptor.
Journal of medicinal chemistry 20020606
-
Sigma receptors inhibit high-voltage-activated calcium channels in rat sympathetic and parasympathetic neurons.
Journal of neurophysiology 20020601
-
Evidence for sigma-1-like receptors in isolated rat liver mitochondrial membranes.
British journal of pharmacology 20020401
-
Noradrenaline release-inhibiting receptors on PC12 cells devoid of alpha(2(-)) and CB(1) receptors: similarities to presynaptic imidazoline and edg receptors.
Neurochemistry international 20020201
-
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
Journal of medicinal chemistry 20020117
-
Effects of AH-9700, (+)-pentazocine, DTG and oxybutynin on micturition in anesthetized rats with acetone-induced cystitis.
Life sciences 20010824
-
Role of the NMDA receptor subunit in the expression of the discriminative stimulus effect induced by ketamine.
European journal of pharmacology 20010629
-
Agmatine and putrescine uptake in the human glioma cell line SK-MG-1.
Naunyn-Schmiedeberg's archives of pharmacology 20010601
-
Conformationally restricted analogs of BD1008 and an antisense oligodeoxynucleotide targeting sigma1 receptors produce anti-cocaine effects in mice.
European journal of pharmacology 20010511
-
A multireceptorial binding reinvestigation on an extended class of sigma ligands: N-[omega-(indan-1-yl and tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine reveal high affinities towards sigma1 and EBP sites.
Bioorganic & medicinal chemistry 20010501
-
Pharmacological actions of AH-9700 on micturition reflex in anesthetized rats.
European journal of pharmacology 20010126
-
N-alkyl substituted analogs of the sigma receptor ligand BD1008 and traditional sigma receptor ligands affect cocaine-induced convulsions and lethality in mice.
European journal of pharmacology 20010112
-
Pharmacology of [3H]R(+)-7-OH-DPAT binding in the rat caudate-putamen.
Neurochemistry international 20010101
-
Biperiden hydrochlorate ameliorates dystonia of rats produced by microinjection of sigma ligands into the red nucleus.
Pharmacology, biochemistry, and behavior 20001101
-
Effect of sigma ligands on the cocaine-induced convulsions in mice.
Polish journal of pharmacology 19990101
-
Cocaine increases the endothelial release of immunoreactive endothelin and its concentrations in human plasma and urine: reversal by coincubation with sigma-receptor antagonists.
Circulation 19980804
-
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
Journal of medicinal chemistry 19960105
-
BMY-14802 reversed the sigma receptor agonist-induced neck dystonia in rats.
Journal of neural transmission (Vienna, Austria : 1996) 19960101
-
Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism.
European journal of pharmacology 19950714
-
The sigma receptor ligand (+/-)-BMY 14802 prevents methamphetamine-induced dopaminergic neurotoxicity via interactions at dopamine receptors.
The Journal of pharmacology and experimental therapeutics 19940401
-
Influence of 1,3-di-o-tolylguanidine and rimcazole, selective sigma ligands, on apomorphine and neuroleptic effects.
Polish journal of pharmacology 19930101
