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.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Collina S, et al. Expert Opin Ther Pat. Sigma receptor modulators: a patent review.
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Blarcamesine is a Sigma-1 receptor agonist and muscarinic receptor modulator with neuroprotective and antidepressant activity. In addition, Blarcamesine ameliorates neurological impairment in a mouse model of Rett syndrome. |
| AB10
AB10 is a selective S1R antagonist. |
| WLB-89462
WLB-89462 is a selective σ2 receptor ligand (Ki: 13 nM). |
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