(-)-Huperzine A is an Acetylcholinesterase inhibitor and NMDA receptor antagonist with an IC50 of 126 μM for NMDA-induced current. Huperzine A, is a naturally occurring sesquiterpene alkaloid compound found in the plant firmoss Huperzia serrata. The IC (50) values of huperzine A were neither altered by changing the concentrations of glycine (2-0.2 μM) and pH (7.4-6.7) in the external solution, nor by addition of Zn (2+) (5 μM) and dithiothreitol (5 mM) to the external solution.
|Animal models||Male Sprague-Dawley rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 10 mg/mL|
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Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively.
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.
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Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
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