Linopirdine dihydrochloride is a blocker of KV7 (KCNQ) voltage-gated potassium channels; blocks KV7.1 + 7.3 (KCNQ2 + 3) / M-currents (IC50 = 4 - 7 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 8.9 μM). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo.
|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||Water 40 mg/mL|
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L-palmitoyl carnitine is a long-chain acylcarnitine and fatty acid metabolite that accumulates in the sarcoid during ischemia and disrupts the membrane lipid environment. L-palmitoylcarnitine inhibits KATP channel activity by interacting with Kir6.2 without affecting single channel conductance.
Or-1896 is an active longevity metabolite of Levosimendan. Or-1896, a highly selective phosphodiesterase (PDE III) inhibitor, is a powerful vasodilator.
Tetraethylammonium chloride is a non-selective potassium channel blocker with antitumor properties.
Charybdotoxin TFA, a 37-amino acid peptide, is a K+ channel blocker.
AUT1 is a Kv3 potassium channel modulator which increases whole currents mediated by human Kv3.1b and Kv3.2a channels, with a concomitant leftward shift in the voltage-dependence of activation, while having a less potent effect on hKv3.3 currents.
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