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Blarcamesine hydrochloride is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
The pre-administration of Blarcamesine leads to a dose-dependent attenuation of the scopolamine induced alternation deficit, significant at 1 and 3 mg/kg. The pre-treatment with Blarcamesine hydrochloride attenuates the impairments of step-through latency, dose dependently and significantly at doses higher than 0.3 mg/kg.
The Blarcamesine hydrochloride treatment dose-dependently blocks the recognition memory deficit, with a significant effect measured at 1 mg/kg. One day after injections, the significant Aβ25-35-induced decrease in Akt phosphorylation is significantly attenuated by Blarcamesine hydrochloride at 0.1 and 1 mg/kg dose. Seven days after injections, Blarcamesine hydrochloride attenuates the decrease in Ser9 phosphorylation induced by the peptide at 0.3 and 1 mg/kg.
The Blarcamesine hydrochloride treatment dose-dependently prevents the Aβ25-35-induced increase in Aβ1-42 content, with a significant effect at the highest dose tested.
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| Animal models | Male mice |
| Formulation | physiological saline solution |
| Dosages | 100 μL/20 g |
| Administration | i.c.v. |
| Molecular Weight | 317.85 |
| Formula | C19H23NO.HCl |
| CAS Number | 195615-84-0 |
| Solubility (25°C) | Water 100 mg/mL DMSO 25 mg/mL |
| Storage | 4°C, dry, sealed |
[2] Collina S, et al. Expert Opin Ther Pat. Sigma receptor modulators: a patent review.
| Related Sigma Receptor Products |
|---|
| Siramesine hydrochloride
Siramesine (Lu 28-179) hydrochloride is an effective sigma-2 receptor agonist. Siramesine has a nanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and is 140 times more selective for sigma-2 receptors (IC50=17 nM). Siramesine has xC-system inhibitory activity associated with iron death. |
| Siramesine
Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine 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 triggers cell death through destabilisation of mitochondria, but not lysosomes. |
| S1RA
S1RA (E-52862) is a potent and selective sigma-1 receptor (σ1R, Ki=17 nM), which showes good selectivity against σ2R (Ki > 1000 nM). |
| Pentoxyverine Citrate
Pentoxyverine citrate is an orally active sigma-1 receptor agonist with Ki values of 41 nM for σ1, 894 nM for σ2, and 75 nM for σ1 in guinea pig brain membranes.Pentoxyverine citrate is also a muscarinic antagonist. |
| Cutamesine dihydrochloride
Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a novel and selective opioid sigma1 receptor agonist with IC50 of 17.4 nM. |
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