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PRE-084 hydrochloride

Cat. No. M10722
PRE-084 hydrochloride  Structure
Size Price Availability Quantity
10mg USD 75  USD75 In stock
50mg USD 300  USD300 In stock
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Quality Control & Documentation
Biological Activity

PRE-084 hydrochloride is a highly affinity selective σ1 agonist with an IC50 value of 44 nM in the sigma receptor detection.

Chemical Information
Molecular Weight 353.88352
Formula C19H28ClNO3
CAS Number 75136-54-8
Form Solid
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Parthena Martin, et al. Epilepsy Behav. Fenfluramine acts as a positive modulator of sigma-1 receptors

[2] Takato Hiranita, et al. J Pharmacol Exp Ther. Stimulants as specific inducers of dopamine-independent σ agonist self-administration in rats

[3] Takato Hiranita, et al. J Pharmacol Exp Ther. Reinforcing effects of sigma-receptor agonists in rats trained to self-administer cocaine

[4] T Maurice. Eur J Pharmacol. Beneficial effect of the sigma(1) receptor agonist PRE-084 against the spatial learning deficits in aged rats

[5] T P Su, et al. J Pharmacol Exp Ther. Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand

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