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Setiptiline

Cat. No. M30309
Setiptiline Structure
Synonym:

Org-8282

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Quality Control & Documentation
Biological Activity

Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.

Chemical Information
Molecular Weight 261.36
Formula C19H19N
CAS Number 57262-94-9
Form Solid
Solubility (25°C) DMSO 25 mg/mL (ultrasonic)
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] Michele Protti, et al. Med Res Rev. New-generation, non-SSRI antidepressants: Drug-drug interactions and therapeutic drug monitoring. Part 2: NaSSAs, NRIs, SNDRIs, MASSAs, NDRIs, and others

[2] A Ishii, et al. Leg Med (Tokyo). Sensitive determination of mianserin and setiptiline in body fluids by gas chromatography with surface ionization detection (GC-SID)

[3] H Kodama. Nihon Shinkei Seishin Yakurigaku Zasshi. [Effect of lithium, carbamazepine, and setiptiline on diacylglycerol in rat brain ex vivo]

[4] M Kuniyoshi, et al. Prog Neuropsychopharmacol Biol Psychiatry. Effectiveness of concomitant setiptiline maleate (Tecipul) on negative symptoms of schizophrenia

[5] K Yamada, et al. Nihon Yakurigaku Zasshi. [Behavioral effects of a new antidepressant, setiptiline]

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