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Lisuride maleate

Cat. No. M6909
Lisuride maleate Structure
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Biological Activity

Lisuride maleate is a dopamine receptor agonist and an anti-parkinson's disease compound. They showed high affinity for D2, D3 and D4 receptors as well as 5-HT1A. They exhibit some characteristics of 5-HT2B receptor antagonists. Decreased prolactin release; Reduces inflammatory mediators such as TNF-α and IL6. Exhibit anticonvulsant effect. The action is similar to bromocriptine.

Chemical Information
Molecular Weight 454.52
Formula C20H26N4O.C4H4O4
CAS Number 19875-60-6
Solubility (25°C) DMSO 44.66 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] Demma, et al. J Biol Chem. SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53.

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