Proteins > Sigma non-opioid intracellular receptor 1
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Sigma non-opioid intracellular receptor 1
A sigma non-opioid intracellular receptor 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99720]
Synonyms
Aging-associated gene 8 protein;
SR31747-binding protein;
SR-BP;
Sigma 1-type opioid receptor;
SIG-1R;
Sigma1-receptor;
Sigma1R;
hSigmaR1
Research
Bioassay Publications (105)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (0.95) | 18.7374 |
| 1990's | 29 (27.62) | 18.2507 |
| 2000's | 16 (15.24) | 29.6817 |
| 2010's | 45 (42.86) | 24.3611 |
| 2020's | 14 (13.33) | 2.80 |
Compounds (181)
Drugs with Potency Measurements
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
[no title available],
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.Journal of medicinal chemistry, , Jun-19, Volume: 46, Issue:13, 2003
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.Journal of medicinal chemistry, , Jun-19, Volume: 46, Issue:13, 2003
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).Journal of medicinal chemistry, , Nov-22, Volume: 39, Issue:24, 1996
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 72, 2022
[no title available]RSC medicinal chemistry, , Jun-23, Volume: 12, Issue:6, 2021
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
EST64454: a Highly Soluble σJournal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Novel multitarget-directed ligands targeting acetylcholinesterase and σEuropean journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands.Bioorganic & medicinal chemistry, , 05-01, Volume: 27, Issue:9, 2019
New analogs of SYA013 as sigma-2 ligands with anticancer activity.Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 27, Issue:10, 2017
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Tetrahydroprotoberberine alkaloids with dopamine and σ receptor affinity.Bioorganic & medicinal chemistry, , May-01, Volume: 24, Issue:9, 2016
Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines.Journal of medicinal chemistry, , Apr-10, Volume: 57, Issue:7, 2014
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Synthesis and biological evaluation of a new series of hexahydro-2H-pyrano[3,2-c]quinolines as novel selective σ1 receptor ligands.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Sigma-1 ligands: Tic-hydantoin as a key pharmacophore.European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.Journal of medicinal chemistry, , Oct-24, Volume: 45, Issue:22, 2002
Radioiodinated N-(2-diethylaminoethyl)benzamide derivatives with high melanoma uptake: structure-affinity relationships, metabolic fate, and intracellular localization.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.Journal of medicinal chemistry, , Dec-16, Volume: 42, Issue:25, 1999
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity binding to MCF-7 breast tumor cells.Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.Journal of medicinal chemistry, , Mar-05, Volume: 36, Issue:5, 1993
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.Journal of medicinal chemistry, , Volume: 34, Issue:6, 1991
[no title available],
Thioxanthene-derived analogs as sigma(1) receptor ligands.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.Journal of medicinal chemistry, , Jun-19, Volume: 46, Issue:13, 2003
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
EST64454: a Highly Soluble σJournal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands.Bioorganic & medicinal chemistry, , 05-01, Volume: 27, Issue:9, 2019
Development of Novel Alkoxyisoxazoles as Sigma-1 Receptor Antagonists with Antinociceptive Efficacy.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines.Journal of medicinal chemistry, , Apr-10, Volume: 57, Issue:7, 2014
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
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, , Jun-06, Volume: 45, Issue:12, 2002
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity binding to MCF-7 breast tumor cells.Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Structural features important for sigma 1 receptor binding.Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.Journal of medicinal chemistry, , Jun-19, Volume: 46, Issue:13, 2003
Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Reevaluation of fenpropimorph as a σ receptor ligand: Structure-affinity relationship studies at human σBioorganic & medicinal chemistry letters, , 07-01, Volume: 27, Issue:13, 2017
Synthesis and characterization of N,N-dialkyl and N-alkyl-N-aralkyl fenpropimorph-derived compounds as high affinity ligands for sigma receptors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.Journal of medicinal chemistry, , Oct-24, Volume: 45, Issue:22, 2002
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
1,4-dibenzylpiperazines possess anticocaine activity.Bioorganic & medicinal chemistry letters, , Feb-24, Volume: 13, Issue:4, 2003
A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
Structural features important for sigma 1 receptor binding.Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.Journal of medicinal chemistry, , Mar-05, Volume: 36, Issue:5, 1993
Synthesis, characterization, and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: structural requirements and binding affinity at the sigma receptor.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents.Journal of medicinal chemistry, , Jun-12, Volume: 35, Issue:12, 1992
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 72, 2022
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.Journal of medicinal chemistry, , Jun-19, Volume: 46, Issue:13, 2003
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.Journal of medicinal chemistry, , Sep-16, Volume: 37, Issue:19, 1994
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.Journal of medicinal chemistry, , Sep-16, Volume: 37, Issue:19, 1994
Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands.European journal of medicinal chemistry, , Mar-10, Volume: 147, 2018
Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
The σ2 receptor: a novel protein for the imaging and treatment of cancer.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.Nature, , Volume: 583, Issue:7816, 2020
Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands.European journal of medicinal chemistry, , Mar-10, Volume: 147, 2018
Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Involvement of apoptosis and autophagy in the death of RPMI 8226 multiple myeloma cells by two enantiomeric sigma receptor ligands.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
[no title available]RSC medicinal chemistry, , Jun-23, Volume: 12, Issue:6, 2021
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Tricyclic Triazoles as σJournal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
EST64454: a Highly Soluble σJournal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands.Bioorganic & medicinal chemistry, , 05-01, Volume: 27, Issue:9, 2019
Pyrazolo[3,4-MedChemComm, , Jun-01, Volume: 8, Issue:6, 2017
Pyrazolo[3,4-MedChemComm, , Jun-01, Volume: 8, Issue:6, 2017
Synthesis and structure-activity relationship study of a new series of selective σ(1) receptor ligands for the treatment of pain: 4-aminotriazoles.Journal of medicinal chemistry, , Mar-12, Volume: 58, Issue:5, 2015
Synthesis and biological evaluation of a new series of hexahydro-2H-pyrano[3,2-c]quinolines as novel selective σ1 receptor ligands.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
Structural features important for sigma 1 receptor binding.Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled opioid receptor activity | molecular function | Combining with an opioid (any narcotic derived from or resembling opium), and transmitting the signal across the membrane by activating an associated G-protein. [GOC:ai, GOC:bf, PMID:20494127] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
Located In
This protein is located in 13 target(s):
| Target | Category | Definition |
|---|
| nuclear envelope | cellular component | The double lipid bilayer enclosing the nucleus and separating its contents from the rest of the cytoplasm; includes the intermembrane space, a gap of width 20-40 nm (also called the perinuclear space). [ISBN:0198547684] |
| nuclear inner membrane | cellular component | The inner, i.e. lumen-facing, lipid bilayer of the nuclear envelope. [GOC:ma] |
| nuclear outer membrane | cellular component | The outer, i.e. cytoplasm-facing, lipid bilayer of the nuclear envelope; continuous with the endoplasmic reticulum of the cell and sometimes studded with ribosomes. [ISBN:0198547684] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| lipid droplet | cellular component | An intracellular non-membrane-bounded organelle comprising a matrix of coalesced lipids surrounded by a phospholipid monolayer. May include associated proteins. [GOC:mah, GOC:tb] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| postsynaptic density | cellular component | An electron dense network of proteins within and adjacent to the postsynaptic membrane of an asymmetric, neuron-neuron synapse. Its major components include neurotransmitter receptors and the proteins that spatially and functionally organize them such as anchoring and scaffolding molecules, signaling enzymes and cytoskeletal components. [GOC:BHF, GOC:dos, GOC:ef, GOC:jid, GOC:pr, GOC:sjp, http://molneuro.kaist.ac.kr/psd, PMID:14532281, Wikipedia:Postsynaptic_density] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| growth cone | cellular component | The migrating motile tip of a growing neuron projection, where actin accumulates, and the actin cytoskeleton is the most dynamic. [GOC:aruk, GOC:bc, ISBN:0815316194, PMID:10082468] |
| cytoplasmic vesicle | cellular component | A vesicle found in the cytoplasm of a cell. [GOC:ai, GOC:mah, GOC:vesicles] |
| anchoring junction | cellular component | A cell junction that mechanically attaches a cell (and its cytoskeleton) to neighboring cells or to the extracellular matrix. [ISBN:0815332181] |
| postsynaptic density membrane | cellular component | The membrane component of the postsynaptic density. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
Involved In
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|
| lipid transport | biological process | The directed movement of lipids into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Lipids are compounds soluble in an organic solvent but not, or sparingly, in an aqueous solvent. [ISBN:0198506732] |
| nervous system development | biological process | The process whose specific outcome is the progression of nervous tissue over time, from its formation to its mature state. [GOC:dgh] |
| G protein-coupled opioid receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by an opioid binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:bf, PMID:20494127] |
| regulation of neuron apoptotic process | biological process | Any process that modulates the occurrence or rate of cell death by apoptotic process in neurons. [GOC:go_curators, GOC:mtg_apoptosis] |
| protein homotrimerization | biological process | The formation of a protein homotrimer, a macromolecular structure consisting of three noncovalently associated identical subunits. [GOC:hjd] |