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Melperone hydrochloride

Cat. No. M6946
Melperone hydrochloride Structure
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10mg USD 280  USD280 4-7 Days
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Biological Activity

Melperone hydrochloride is a atypical neuroleptic; 5-HT2A/D2 receptor antagonist (Ki values are 120 and 180 nM respectively). Causes an increase in dopamine levels in the medial prefrontal cortex (mPFC) and nucleus accumbens and an increase in ACh in the mPFC. Also binds adrenergic α1 and α2 receptors (Ki values are 180 and 150 nM respectively).

Chemical Information
Molecular Weight 299.81
Formula C16H22FNO.HCl
CAS Number 1622-79-3
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] Najafov, et al. Biochem J. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1.

[2] P Seeman, et al. Neuropsychopharmacology. Atypical Neuroleptics Have Low Affinity for Dopamine D2 Receptors or Are Selective for D4 Receptors

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