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Re: Norepinehprine D4 receptor

Posted by undopaminergic on May 29, 2020, at 11:05:18

In reply to Norepinehprine D4 receptor, posted by linkadge on May 28, 2020, at 7:44:50

> Apparently norepinephrine itself is a potent activator of dopamine d4 receptors. D4 receptors have been implicated in ADHD. I wonder if this is behind the efficacy of NRIs in ADHD.
> Linkadge

Cite: "... noradrenaline and adrenaline exhibited a high affinity binding component (KH = 12.1 nM and 5.0 nM, respectively), similar to that of dopamine (KH = 2.6 nM), ...", and: "These results indicate that dopamine D4 receptors are activated by noradrenaline and adrenaline, although at 50-100-fold higher concentrations than dopamine.".

How do they calculate the "50-100"? 12.1 / 2.6 is ~ 4.7.

What do these affinities mean at physiological concentrations of these neurotransmitters?





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