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RTI 336

Cat. No. M42670
RTI 336 Structure
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Biological Activity

RTI 336 is a phenyltropane analog, as well as a potent and selective dopamine transporter (DAT) inhibitor.

Chemical Information
Molecular Weight 429.38
Formula C24H26Cl2N2O
CAS Number 204069-50-1
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] F Ivy Carroll et al. Front Pharmacol. A Double-Blind, Placebo-Controlled Trial Demonstrating the Safety, Tolerability, and Pharmacokinetics of Single, Escalating Oral Doses of RTI-336

[2] Monica L Andersen et al. Exp Clin Psychopharmacol. Influence of chronic dopamine transporter inhibition by RTI-336 on motor behavior, sleep, and hormone levels in rhesus monkeys

[3] Paul W Czoty et al. Pharmacol Biochem Behav. Lower reinforcing strength of the phenyltropane cocaine analogs RTI-336 and RTI-177 compared to cocaine in nonhuman primates

[4] F Ivy Carroll et al. AAPS J. Development of the dopamine transporter selective RTI-336 as a pharmacotherapy for cocaine abuse

[5] Colin N Haile et al. Brain Res. Cocaine self-administration and locomotor activity are altered in Lewis and F344 inbred rats by RTI 336, a 3-phenyltropane analog that binds to the dopamine transporter

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Keywords: RTI 336 supplier, Dopamine Transporter, inhibitors, activators

 
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