Cyclohexyl-[2-(3,5-dimethyl-pyrazol-1-yl)-6-methyl-pyrimidin-4-yl]-amine

CyPPA is a positive SK3/SK2 modulator that reduces the activity of dopaminergic neurons, inhibits dopamine release, and counteracts hyperdopaminergic behaviors induced by methyl phenidate.

CyPPA has been used:

• to test its inhibitory functionality on melanogenesis
• as an activator of small conductance potassium channel-3 (SK3) in mesenteric artery segments
• in the activation of calcium-activated potassium (SK) channels in murine hippocampal neurons HT-22 cells

Activator of small conductance Ca 2+ -activated K + channels that displays selectivity for SK2 and SK3 channels (EC 50 values are 5.6 and 14 μ M for SK3 and SK2 respectively). Displays no activity at SK1 and IK channels.

CyPPA is a positive modulator of small conductance Ca2+-activated K+ channels; selective for SK3 and SK2. CyPPA is a first subtype selective SK channel positive modulator with an EC50 of 5.6 μM and 14 μM, efficacy 90% and 71% for hSK3 and hSK2, respectively. CyPPA is a tool for distinguishing SK2 and SK3 from SK1 and IK; no other agents distinguish these channels.

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