Sigma receptor is a non-opioid receptor that binds diverse classes of psychotropic drugs. Sigma receptors are subdivided into two subtypes, sigma-1 and sigma-2. The sigma-1 receptor is a 25-kDa protein possessing one putative transmembrane domain and an endoplasmic reticulum retention signal. Sigma-1 receptors are highly expressed in deeper laminae of the cortex, olfactory bulb, nuclei of mesencephalon, hypothalamus, and Purkinje cells in the brain. Sigma-1 receptors are predominantly localized at the endoplasmic reticulum of both neurons and oligodendrocytes. From behavioral studies, sigma-1 receptors were shown to be involved in higher-ordered brain functions including memory and drug dependence. The sigma-2 receptor (σ2R) is a sigma receptor subtype which preferentially binds to siramesine and PB28. PGRMC1 was recently identified as the sigma-2 receptor. Unlike sigma-1 receptor, it has not yet been cloned. Activation of the receptor can cause apoptosis. A pharmacophore model based on benzooxazolone derivatives has been developed.


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AH-5183 hydrochloride

(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively[1][2].

  • CAS Number: 120447-62-3
  • MF: C17H26ClNO
  • MW: 295.84700
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: 393.5ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 97ºC

CM 572

A potent, selective, irreversible sigma-2 receptor partial agonist with Ki of 14.6 nM, >700-fold selectivity over sigma-1 receptors; induces dose-dependent cell death in SK-N-SH cells with EC50 of 7.6 uM, also demonstrates selective cytotoxic activity against PANC-1 pancreatic and MCF-7 breast cancer cell lines, with no significant effect on normal cells.

  • CAS Number: 1121932-91-9
  • MF: C22H23FN4O2S
  • MW: 426.51
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S1RA hydrochloride

S1RA Hcl(E-52862 Hcl) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).IC50 value: 17 nM (Ki) [1]Target: σ1R antagonistin vitro: S1RA behaved as a highly selective σ1 receptor antagonist. It showed high affinity for human (Ki= 17 nM) and guinea pig (Ki= 23.5 nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki= 328 nM) and antagonistic activity, with very low potency (IC50= 4700 nM) was found at the human 5-HT2B receptor. S1RA showed no significant affinity (Ki > 1 μM or % inhibition at 1 μM < 50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes) [2].in vivo: Control (non-operated) and nerve-injured mice received a single or repeated (twice daily for 12 days) i.p. administration of S1RA at 25 mg·kg?1, the same dose used for the assessment of behavioural hypersensitivity in the chronic treatment study. Acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery, as in the behavioural studies [2]. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior [3].

  • CAS Number: 1265917-14-3
  • MF: C20H24ClN3O2
  • MW: 373.87600
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BD 1008 dihydrobromide

BD-1008 dihydrobromide is an antagonist of sigma Receptor. BD-1008 dihydrobromide attenuates the toxicity and stimulants effects of cocaine in mice[1].

  • CAS Number: 138356-09-9
  • MF: C15H24Br2Cl2N2
  • MW: 463.08
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: 454.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 228.8ºC

opipramol

Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD)[1][2].

  • CAS Number: 315-72-0
  • MF: C23H29N3O
  • MW: 363.49600
  • Catalog: Sigma Receptor
  • Density: 1.129 g/cm3
  • Boiling Point: 555.1ºC at 760 mmHg
  • Melting Point: 100-101ºC
  • Flash Point: 290.5ºC

S1R agonist 1 hydrochloride

S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].

  • CAS Number: 242487-82-7
  • MF: C20H26ClNO
  • MW: 331.88
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CM398

CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice[1].

  • CAS Number: 1121931-70-1
  • MF: C23H29N3O3
  • MW: 395.49
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CYR-101

MIN-101 is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).

  • CAS Number: 359625-79-9
  • MF: C22H23FN2O2
  • MW: 366.429
  • Catalog: 5-HT Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 551.7±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 287.4±30.1 °C

(Rac)-E1R

(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders[1].

  • CAS Number: 787623-60-3
  • MF: C13H16N2O2
  • MW: 232.28
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Siramesine fumarate salt

Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity[1][2][3].

  • CAS Number: 163630-79-3
  • MF: C34H35FN2O5
  • MW: 570.65
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SKF 83959 hydrobromide

SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression[1][2][3][4].

  • CAS Number: 67287-95-0
  • MF: C18H21BrClNO2
  • MW: 398.72200
  • Catalog: Dopamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E1R

E1R is a positive allosteric modulator of sigma-1 receptors with cognition-enhancing activity[1].

  • CAS Number: 1301211-78-8
  • MF: C13H16N2O2
  • MW: 232.28
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pentoxyverine

Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[1][2][3][4].

  • CAS Number: 77-23-6
  • MF: C20H31NO3
  • MW: 333.465
  • Catalog: Sigma Receptor
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 435.5±30.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 217.2±24.6 °C

(2R,3R)-E1R

(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders[1].

  • CAS Number: 1400888-63-2
  • MF: C13H16N2O2
  • MW: 232.28
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KB-5492 anhydrous

KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent[1][2].

  • CAS Number: 129200-10-8
  • MF: C27H34N2O10
  • MW: 546.56600
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: 553.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 288.3ºC

threo Ifenprodil hemitartrate

threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity[1][2][3].

  • CAS Number: 1312991-83-5
  • MF: C21H27NO2.1/2C4H6O6
  • MW: 400.50
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sigma-2 Radioligand 1

Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts[1].

  • CAS Number: 2860554-32-9
  • MF: C24H30FN3O3
  • MW: 427.51
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SKF 83959 HYDROBROMIDE

SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression[1][2][3][4].

  • CAS Number: 80751-85-5
  • MF: C18H21BrClNO2
  • MW: 398.72200
  • Catalog: Dopamine Receptor
  • Density: 1.249g/cm3
  • Boiling Point: 464.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 234.8ºC

6-(6-(4-hydroxypiperidinyl)hexyloxy)-3-methylflavone HCl

Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor[1].

  • CAS Number: 139652-86-1
  • MF: C27H34ClNO4
  • MW: 472.01600
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: 615.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 326.1ºC

SARS-CoV-2-IN-57

SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 (IC50: 80 nM). SARS-CoV-2-IN-57 has high affinity for Sigma Receptor with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) respectively[1].

  • CAS Number: 1265624-68-7
  • MF: C23H37N3O
  • MW: 371.56
  • Catalog: SARS-CoV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PRE-084 (hydrochloride)

PRE-084 hydrochloride is a high affinity, selective σ1 agonist, has an IC50 of 44 nM in the sigma receptor assay.IC50 value: 44 nMTarget: sigma receptorin vitro: PRE-084 has an IC50 of more than 100,000 nM for PCP receptors and an IC50 higher than 10,000 nM in a variety of other receptor systems. [1]in vivo: PRE-084 improves motor neuron survival and motor performance in wobbler mice. PRE-084 enhances BDNF-mediated trophic support.[2]

  • CAS Number: 75136-54-8
  • MF: C19H28ClNO3
  • MW: 353.884
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(2S,3S)-E1R

(2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders[1].

  • CAS Number: 1424832-57-4
  • MF: C13H16N2O2
  • MW: 232.28
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

phenyltoloxamine

Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (Ki: 160 nM)[1][2][3].

  • CAS Number: 92-12-6
  • MF: C17H21NO
  • MW: 255.35500
  • Catalog: Histamine Receptor
  • Density: 1.022g/cm3
  • Boiling Point: 359.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 106ºC

Dimemorfan phosphate

Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.

  • CAS Number: 36304-84-4
  • MF: C18H28NO4P
  • MW: 353.393
  • Catalog: Sigma Receptor
  • Density: 1.07g/cm3
  • Boiling Point: 366.9ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 158.3ºC

PRE-084 hydrochloride

PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway[1][2][3][4].

  • CAS Number: 138847-85-5
  • MF: C19H27NO3
  • MW: 317.42
  • Catalog: Sigma Receptor
  • Density: 1.103g/cm3
  • Boiling Point: 446.6ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 223.9ºC

Pentoxyverine-d8

Pentoxyverine-d8 (Carbetapentane-d8) is the deuterium labeled Pentoxyverine. Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[1][2][3][4].

  • CAS Number: 1329797-10-5
  • MF: C20H23D8NO3
  • MW: 341.51
  • Catalog: Sigma Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KSK68

KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain[1].

  • CAS Number: 2566715-91-9
  • MF: C23H28N2O2
  • MW: 364.48
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KSK67

KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain[1].

  • CAS Number: 2566715-93-1
  • MF: C22H27N3O2
  • MW: 365.47
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S1RA

S1RA(E-52862) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).IC50 value: 17 nM (Ki) [1]Target: σ1Rin vitro: S1RA behaved as a highly selective σ1 receptor antagonist. It showed high affinity for human (Ki= 17 nM) and guinea pig (Ki= 23.5 nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki= 328 nM) and antagonistic activity, with very low potency (IC50= 4700 nM) was found at the human 5-HT2B receptor. S1RA showed no significant affinity (Ki > 1 μM or % inhibition at 1 μM < 50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes) [2].in vivo: Control (non-operated) and nerve-injured mice received a single or repeated (twice daily for 12 days) i.p. administration of S1RA at 25 mg·kg?1, the same dose used for the assessment of behavioural hypersensitivity in the chronic treatment study. Acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery, as in the behavioural studies [2]. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior [3].

  • CAS Number: 878141-96-9
  • MF: C20H23N3O2
  • MW: 337.415
  • Catalog: Sigma Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 528.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 273.2±30.1 °C

PB 28 dihydrochloride

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively; inhibits cancer cell growth, modulates P-glycoprotein, and synergizes with doxorubicin in MCF7 and MCF ADR cells with IC50 in nanomolar range; increase G0-G1-phase fraction and caspase-independent apoptosis, also reduces P-gp expression.

  • CAS Number: 172907-03-8
  • MF: C24H40Cl2N2O
  • MW: 443.493
  • Catalog: SARS-CoV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A