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SB242084

Cat. No. M3772
SB242084 Structure
Size Price Availability
10mg USD 160 Out of stock
50mg USD 750 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

SB242084 has anxiolytic effects, and enhances dopamine signalling in the limbic system, as well as having complex effects on the dopamine release produced by cocaine, increasing it in some brain regions but reducing it in others. It has been shown to increase the effectiveness of the selective serotonin reuptake inhibitor (SSRI) class of antidepressants, and may also reduce their side effects. In animal studies, SB-242,084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines. SB 242084 is the first reported selective potent and brain penetrant 5-HT2C receptor antagonist and has anxiolytic-like activity, but does not possess either proconvulsant or hyperphagic properties which are characteristic of mutant mice lacking the 5-HT2C receptor.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 394.85
Formula C21H19ClN4O2
CAS Number 181632-25-7
Purity >98%
Solubility DMSO
Storage at -20°C
References

SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.
Kennett GA, et al. Neuropharmacology. 1997 Apr-May;36(4-5):609-20. PMID: 9225286.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB242084 supplier, 5-HT Receptor, inhibitors

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