| S0106 |
BD-1047 dihydrobromide
|
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. |
-
Brain Res, 2024, 1838:149011
-
Authorea Preprints, 2023,
-
Neuropharmacology, 2021, 196:108360
|
|
| S6981 |
Glycerol phenylbutyrate
|
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. Glycerol phenylbutyrate is a prodrug in which phenylbutyrate (PBA) is released from the glycerol backbone by lipases in the gastrointestinal tract. |
|
|
| E7418New |
Noscapine
|
Noscapine ((S,R)-Noscapine) is an alkaloid derived from the opium poppy (Papaver somniferum) and is a centrally acting antitussive opiate derivative. It is a non-competitive antagonist of the bradykinin B2 receptor. It also exhibits neuroprotection by activating sigma-1 opioid receptors, which help suppress intracellular NO levels and calcium, thereby providing protection against ischemic injury. |
|
|
| S0295 |
Anavex 2-73 HCl
|
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. |
|
|
| S0869 |
Carbetapentane
|
Carbetapentane (Pentoxyverine, CB) is an antitussive anticonvulsant nonselective sigma-1 (σ1) agonist. |
|
|
| S6561 |
4-IBP
|
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). |
|
|
| E0388 |
WQ 1
|
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. |
|
|
| E7744New |
Siramesine
|
Siramesine (Lu 28-179) is a potent agonist of sigma-2 receptor(σ1R) with an IC50 of 0.12 nM, exhibiting 140-fold selectivity over sigma-1 receptors. It shows strong anxiolytic effects and induces cancer cell death, highlighting its potential anticancer activity. |
|
|
| S2917 |
Cutamesine Dihydrochloride
|
Cutamesine dihydrochloride (SA4503 dihydrochloride,AGY94806 dihydrochloride) is a potent Sigma-1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. |
|
|
| S0191 |
BD1063 2HCL
|
BD1063 2HCL (BD1063 dihydrochloride) is a potent and selective sigma-1 receptor (σ1R) antagonist with Ki of 4.43 nM. |
|
|
| S6950 |
PRE-084 hydrochloride
|
PRE-084 hydrochloride (HCl) is a potent, selective sigma-1 receptor (σ1, S1R) agonist with IC50 of 44 nM in the sigma receptor assay. |
-
Free Radic Biol Med, 2025, 226:96-108
|
|
| E7191New |
Ditolylguanidine
|
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. |
-
HIV Med, 2025, 26(2):285-294
|
|
| S6754 |
S1RA
|
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. |
-
Int Immunopharmacol, 2024, 128:111524
|
|
| S6756 |
Siramesine HCl
|
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. |
-
J Transl Med, 2025, 23(1):780
|
|
| S0295 |
Anavex 2-73 HCl
|
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. |
|
|
| S0869 |
Carbetapentane
|
Carbetapentane (Pentoxyverine, CB) is an antitussive anticonvulsant nonselective sigma-1 (σ1) agonist. |
|
|
| S6561 |
4-IBP
|
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). |
|
|
| E7744New |
Siramesine
|
Siramesine (Lu 28-179) is a potent agonist of sigma-2 receptor(σ1R) with an IC50 of 0.12 nM, exhibiting 140-fold selectivity over sigma-1 receptors. It shows strong anxiolytic effects and induces cancer cell death, highlighting its potential anticancer activity. |
|
|
| S2917 |
Cutamesine Dihydrochloride
|
Cutamesine dihydrochloride (SA4503 dihydrochloride,AGY94806 dihydrochloride) is a potent Sigma-1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. |
|
|
| S6950 |
PRE-084 hydrochloride
|
PRE-084 hydrochloride (HCl) is a potent, selective sigma-1 receptor (σ1, S1R) agonist with IC50 of 44 nM in the sigma receptor assay. |
-
Free Radic Biol Med, 2025, 226:96-108
|
|
| E7191New |
Ditolylguanidine
|
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. |
-
HIV Med, 2025, 26(2):285-294
|
|
| S6756 |
Siramesine HCl
|
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. |
-
J Transl Med, 2025, 23(1):780
|
|
| S0106 |
BD-1047 dihydrobromide
|
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. |
- Brain Res, 2024, 1838:149011
- Authorea Preprints, 2023,
- Neuropharmacology, 2021, 196:108360
|
|
| E0388 |
WQ 1
|
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. |
|
|
| S0191 |
BD1063 2HCL
|
BD1063 2HCL (BD1063 dihydrochloride) is a potent and selective sigma-1 receptor (σ1R) antagonist with Ki of 4.43 nM. |
|
|
| S6754 |
S1RA
|
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. |
- Int Immunopharmacol, 2024, 128:111524
|
|
| S0295 |
Anavex 2-73 HCl
|
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. |
|
|
| S0869 |
Carbetapentane
|
Carbetapentane (Pentoxyverine, CB) is an antitussive anticonvulsant nonselective sigma-1 (σ1) agonist. |
|
|
| S6561 |
4-IBP
|
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). |
|
|
| E7744New |
Siramesine
|
Siramesine (Lu 28-179) is a potent agonist of sigma-2 receptor(σ1R) with an IC50 of 0.12 nM, exhibiting 140-fold selectivity over sigma-1 receptors. It shows strong anxiolytic effects and induces cancer cell death, highlighting its potential anticancer activity. |
|
|
| S2917 |
Cutamesine Dihydrochloride
|
Cutamesine dihydrochloride (SA4503 dihydrochloride,AGY94806 dihydrochloride) is a potent Sigma-1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. |
|
|
| S6950 |
PRE-084 hydrochloride
|
PRE-084 hydrochloride (HCl) is a potent, selective sigma-1 receptor (σ1, S1R) agonist with IC50 of 44 nM in the sigma receptor assay. |
- Free Radic Biol Med, 2025, 226:96-108
|
|
| E7191New |
Ditolylguanidine
|
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. |
- HIV Med, 2025, 26(2):285-294
|
|
| S6756 |
Siramesine HCl
|
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. |
- J Transl Med, 2025, 23(1):780
|
|
| E7418New |
Noscapine
|
Noscapine ((S,R)-Noscapine) is an alkaloid derived from the opium poppy (Papaver somniferum) and is a centrally acting antitussive opiate derivative. It is a non-competitive antagonist of the bradykinin B2 receptor. It also exhibits neuroprotection by activating sigma-1 opioid receptors, which help suppress intracellular NO levels and calcium, thereby providing protection against ischemic injury. |
|
|
| E7744New |
Siramesine
|
Siramesine (Lu 28-179) is a potent agonist of sigma-2 receptor(σ1R) with an IC50 of 0.12 nM, exhibiting 140-fold selectivity over sigma-1 receptors. It shows strong anxiolytic effects and induces cancer cell death, highlighting its potential anticancer activity. |
|
|
| E7191New |
Ditolylguanidine
|
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. |
- HIV Med, 2025, 26(2):285-294
|
|
| E7744New |
Siramesine
|
Siramesine (Lu 28-179) is a potent agonist of sigma-2 receptor(σ1R) with an IC50 of 0.12 nM, exhibiting 140-fold selectivity over sigma-1 receptors. It shows strong anxiolytic effects and induces cancer cell death, highlighting its potential anticancer activity. |
|
|
| E7191New |
Ditolylguanidine
|
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. |
- HIV Med, 2025, 26(2):285-294
|
|