Proteins > Sigma non-opioid intracellular receptor 1
Page last updated: 2024-08-07 17:29:30
Sigma non-opioid intracellular receptor 1
A sigma non-opioid intracellular receptor 1 that is encoded in the genome of rat. [OMA:Q9R0C9, PRO:DNx]
Synonyms
Sigma 1-type opioid receptor;
Sigma1-receptor;
Sigma1R
Research
Bioassay Publications (43)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 3 (6.98) | 18.7374 |
| 1990's | 17 (39.53) | 18.2507 |
| 2000's | 9 (20.93) | 29.6817 |
| 2010's | 12 (27.91) | 24.3611 |
| 2020's | 2 (4.65) | 2.80 |
Compounds (73)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 7-hydroxy-2-n,n-dipropylaminotetralin | Rattus norvegicus (Norway rat) | Ki | 0.0232 | 1 | 1 |
| carbetapentane | Rattus norvegicus (Norway rat) | Ki | 0.0180 | 3 | 3 |
| citalopram | Rattus norvegicus (Norway rat) | Ki | 0.2920 | 1 | 1 |
| amphetamine | Rattus norvegicus (Norway rat) | Ki | 50.0000 | 1 | 1 |
| fentanyl | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 1 | 1 |
| fluoxetine | Rattus norvegicus (Norway rat) | Ki | 0.2400 | 1 | 1 |
| vanoxerine | Rattus norvegicus (Norway rat) | Ki | 0.1160 | 1 | 1 |
| haloperidol | Rattus norvegicus (Norway rat) | IC50 | 0.0013 | 4 | 5 |
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 0.0148 | 7 | 7 |
| ifenprodil | Rattus norvegicus (Norway rat) | Ki | 0.0049 | 1 | 1 |
| imipramine | Rattus norvegicus (Norway rat) | Ki | 0.3430 | 1 | 1 |
| lamotrigine | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| ondansetron | Rattus norvegicus (Norway rat) | Ki | 0.6800 | 1 | 1 |
| imatinib | Rattus norvegicus (Norway rat) | Ki | 14.3000 | 1 | 1 |
| thioridazine | Rattus norvegicus (Norway rat) | IC50 | 0.7500 | 1 | 1 |
| vesamicol | Rattus norvegicus (Norway rat) | Ki | 0.0221 | 1 | 1 |
| phencyclidine | Rattus norvegicus (Norway rat) | IC50 | 0.5300 | 1 | 1 |
| phencyclidine | Rattus norvegicus (Norway rat) | Ki | 1.0900 | 1 | 1 |
| 1,3-ditolylguanidine | Rattus norvegicus (Norway rat) | IC50 | 0.1816 | 3 | 5 |
| 1,3-ditolylguanidine | Rattus norvegicus (Norway rat) | Ki | 0.0945 | 3 | 3 |
| n-phenethylpiperidine | Rattus norvegicus (Norway rat) | Ki | 0.0885 | 1 | 1 |
| 2-methyl-1,2,3,4-tetrahydroisoquinoline | Rattus norvegicus (Norway rat) | IC50 | 2.7000 | 1 | 1 |
| rimcazole | Rattus norvegicus (Norway rat) | IC50 | 1.4152 | 3 | 5 |
| rimcazole | Rattus norvegicus (Norway rat) | Ki | 0.6050 | 2 | 2 |
| opc 14117 | Rattus norvegicus (Norway rat) | IC50 | 15.0000 | 1 | 2 |
| tenocyclidine | Rattus norvegicus (Norway rat) | IC50 | 0.2400 | 1 | 1 |
| sertraline | Rattus norvegicus (Norway rat) | Ki | 0.0570 | 1 | 1 |
| 1,2,3,4-tetrahydro-1-(phenylmethyl)isoquinoline | Rattus norvegicus (Norway rat) | IC50 | 0.4300 | 1 | 1 |
| 1,2,3,4-tetrahydro-1-phenylisoquinoline | Rattus norvegicus (Norway rat) | IC50 | 2.0000 | 1 | 1 |
| alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol | Rattus norvegicus (Norway rat) | IC50 | 0.0730 | 3 | 4 |
| alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol | Rattus norvegicus (Norway rat) | Ki | 0.3910 | 2 | 2 |
| 5-iodobenzovesamicol | Rattus norvegicus (Norway rat) | Ki | 0.2660 | 1 | 1 |
| l 687384 | Rattus norvegicus (Norway rat) | IC50 | 0.0003 | 2 | 3 |
| 1-(3-fluoropropyl)-4-(4-cyanophenoxymethyl)piperidine | Rattus norvegicus (Norway rat) | Ki | 0.0043 | 1 | 1 |
| dizocilpine | Rattus norvegicus (Norway rat) | IC50 | 1.7000 | 1 | 1 |
| dizocilpine | Rattus norvegicus (Norway rat) | Ki | 59.1670 | 1 | 1 |
| preclamol | Rattus norvegicus (Norway rat) | IC50 | 0.0311 | 2 | 2 |
| vesamicol | Rattus norvegicus (Norway rat) | Ki | 0.0204 | 1 | 1 |
| 4-phenyl-1,2,3,4-tetrahydroisoquinoline | Rattus norvegicus (Norway rat) | IC50 | 4.2000 | 1 | 1 |
| sb 408124 | Rattus norvegicus (Norway rat) | Ki | 1.4050 | 1 | 1 |
| naloxone | Rattus norvegicus (Norway rat) | Ki | 0.0030 | 1 | 1 |
| preclamol | Rattus norvegicus (Norway rat) | IC50 | 0.1599 | 2 | 2 |
| fluvoxamine | Rattus norvegicus (Norway rat) | Ki | 0.0360 | 2 | 2 |
| dextromethorphan | Rattus norvegicus (Norway rat) | Ki | 5.0700 | 1 | 1 |
| 7-hydroxy-2-(n-n-propyl-n-(3-iodo-2'-propenyl)-amino)tetralin | Rattus norvegicus (Norway rat) | Ki | 0.0032 | 1 | 1 |
| cilansetron | Rattus norvegicus (Norway rat) | Ki | 0.3400 | 1 | 1 |
| n-demethylloperamide | Rattus norvegicus (Norway rat) | Ki | 0.0008 | 1 | 1 |
| lu 28-179 | Rattus norvegicus (Norway rat) | IC50 | 0.0170 | 2 | 3 |
| jnj 10397049 | Rattus norvegicus (Norway rat) | Ki | 0.0060 | 1 | 1 |
| sa 4503 | Rattus norvegicus (Norway rat) | Ki | 0.0046 | 1 | 1 |
| sb674042 | Rattus norvegicus (Norway rat) | Ki | 0.1290 | 1 | 1 |
| tcs ox2 29 | Rattus norvegicus (Norway rat) | IC50 | 0.0400 | 1 | 1 |
| PB28 | Rattus norvegicus (Norway rat) | Ki | 0.0710 | 1 | 1 |
| benzovesamicol | Rattus norvegicus (Norway rat) | Ki | 0.0261 | 1 | 1 |
| almorexant | Rattus norvegicus (Norway rat) | Ki | 0.0080 | 1 | 1 |
| suvorexant | Rattus norvegicus (Norway rat) | Ki | 0.0004 | 1 | 1 |
| mk-6096 | Rattus norvegicus (Norway rat) | Ki | 0.0003 | 1 | 1 |
| sb 649868 | Rattus norvegicus (Norway rat) | Ki | 0.0004 | 1 | 1 |
| act-335827 | Rattus norvegicus (Norway rat) | IC50 | 0.4170 | 1 | 1 |
| clozapine | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| preclamol | Rattus norvegicus (Norway rat) | Log IC50 | 1.5200 | 1 | 1 |
| preclamol | Rattus norvegicus (Norway rat) | Log IC50 | 0.8100 | 1 | 1 |
| gsk 1059865 | Rattus norvegicus (Norway rat) | Kb | 0.1260 | 1 | 1 |
Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics.RSC medicinal chemistry, , Aug-17, Volume: 13, Issue:8, 2022
Synthesis and evaluation of novel (18)F-labeled spirocyclic piperidine derivatives as σ1 receptor ligands for positron emission tomography imaging.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 20, Issue:16, 2012
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
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. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
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 biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
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
Synthesis, configuration, and activity of isomeric 2-phenyl-2-(N-piperidinyl)bicyclo[3.1.0]hexanes at phencyclidine and sigma binding sites.Journal of medicinal chemistry, , Dec-11, Volume: 35, Issue:25, 1992
Phencyclidine-like effects of tetrahydroisoquinolines and related compounds.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).Bioorganic & medicinal chemistry, , Aug-15, Volume: 20, Issue:16, 2012
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, , Dec-10, Volume: 52, Issue:23, 2009
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.Journal of medicinal chemistry, , Jan-27, Volume: 43, Issue:2, 2000
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
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 biological evaluation of new aryl-alkyl(alkenyl)-4-benzylpiperidines, novel Sigma Receptor (SR) modulators, as potential anticancer-agents.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.Journal of medicinal chemistry, , Jan-27, Volume: 43, Issue:2, 2000
Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
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
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. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
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 biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
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 binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencycliJournal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
Phencyclidine-like effects of tetrahydroisoquinolines and related compounds.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Molecular similarity, quantitative chirality, and QSAR for chiral drugs.Journal of medicinal chemistry, , May-27, Volume: 37, Issue:11, 1994
N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors.Journal of medicinal chemistry, , Volume: 30, Issue:12, 1987
Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines.Journal of medicinal chemistry, , Volume: 30, Issue:12, 1987
Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Molecular similarity, quantitative chirality, and QSAR for chiral drugs.Journal of medicinal chemistry, , May-27, Volume: 37, Issue:11, 1994
N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors.Journal of medicinal chemistry, , Volume: 30, Issue:12, 1987
Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines.Journal of medicinal chemistry, , Volume: 30, Issue:12, 1987
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Thiophene bioisosteres of spirocyclic σ receptor ligands: relationships between substitution pattern and σ receptor affinity.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.Journal of medicinal chemistry, , May-26, Volume: 38, Issue:11, 1995
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