| S0106 |
BD-1047 dihydrobromide
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BD-1047 dihydrobromide (HBr) is a selective functional antagonist of sigma-1 (σ1) receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia.
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Brain Res, 2024, 1838:149011
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Authorea Preprints, 2023,
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Neuropharmacology, 2021, 196:108360
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| S6950 |
PRE-084 hydrochloride
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PRE-084 hydrochloride (HCl) is a potent, selective sigma-1 receptor (σ1, S1R) agonist with IC50 of 44 nM in the sigma receptor assay.
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Free Radic Biol Med, 2025, 226:96-108
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| E7191 |
Ditolylguanidine
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Ditolylguanidine (1,3-di-o-tolylguanidine) is a non-selective agonist of sigma receptor (σ receptor) with high affinity Ki values of 69 nM and 21 nM for σ1 and σ2 receptors, respectively. It effectively inhibits the growth of small cell lung cancer cells and can be used for the research of lung cancer.
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HIV Med, 2025, 26(2):285-294
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| S6754 |
S1RA
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S1RA (E-52862) is a selective sigma-1 receptor (σ1R) antagonist with a reported binding affinity of Ki = 17.0 ± 7.0 nM for human σ1 receptor , selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels.
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Int Immunopharmacol, 2024, 128:111524
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| S6756 |
Siramesine HCl
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Siramesine (Lu 28-179) is a sigma receptor agonist, selective for the σ2 subtype with IC50 values of 0.12 nM and 17 nM for σ2 and σ1 receptors respectively.
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J Transl Med, 2025, 23(1):780
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| S6981 |
Glycerol phenylbutyrate
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Glycerol phenylbutyrate (GT4P, HPN-100M, Ravicti) is a nitrogen-binding agent and acts as a sigma-2 (σ2) receptor ligand with a pKi of 8.02. This compound is a prodrug in which phenylbutyrate (PBA) is released from the glycerol backbone by lipases in the gastrointestinal tract.
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| S0295 |
Anavex 2-73 HCl
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Anavex 2-73 (Blarcamesine, AVex-73, AE-37), an aminotetrahydrofuran derivative, is a mixed muscarinic and sigma-1/σ1 Receptor agonist with IC50 of 0.86 μM.
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| S0869 |
Carbetapentane
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Carbetapentane (Pentoxyverine, CB) is an antitussive anticonvulsant nonselective sigma-1 (σ1) agonist.
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| S6561 |
4-IBP
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4-IBP is a selective σ1 receptor agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM).
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| E0388 |
WQ 1
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WQ 1 is a high affinity and selective σ1 receptor antagonist with pKi values of 10.85, 6.53 and 5.80 at σ1, σ2 receptors and dopamine transporter (DAT), displaying σ1/σ2 selectivity ratio of 20893.
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