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Mezilamine 

Cat. No. M30198
Mezilamine  Structure
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Biological Activity

Mezilamine is a potent antidopaminergic agent. Mezilamine induces a concentration dependent increase in the electrically stimulated overflow of 3H-noradrenaline from rat cortical slices, without affecting the basal overflow. Mezilamine acts as a presynaptic α-adrenoceptor antagonist and a postsynaptic α-adrenoceptor agonist.

Chemical Information
Molecular Weight 287.81
Formula C11H18ClN5S
CAS Number 50335-55-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] R Neale, et al. Psychopharmacology (Berl). Acute dyskinesias in monkeys elicited by halopemide, mezilamine and the "antidyskinetic" drugs, oxiperomide and tiapride

[2] J D Leander. Psychopharmacology (Berl). Interactions of clozapine, thioridazine, and mezilamine with oxotremorine on schedule-controlled responding

[3] R G Browne. Psychopharmacology (Berl). Anxiolytics antagonize yohimbine's discriminative stimulus properties

[4] G Le Fur, et al. Eur J Pharmacol. Mezilamine, a new dopamine antagonist, blocks presynaptic but stimulates postsynaptic alpha-adrenoceptors

[5] A Uzan, et al. Life Sci. Effects on striatal and mesolimbic dopamine systems of a new potential antipsychotic drug -mezilamine- with weak cataleptogenic properties

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