Posted by linkadge on August 24, 2021, at 7:17:23
In reply to Re: Dopamine agonists downreg/SLS/UD/Linkadge/all?, posted by undopaminergic on August 24, 2021, at 1:56:36
Well, as a presynaptic agonist, it blocks dopamine release (i.e. a functional antagonist properties). But it can also activate or block post synaptic receptors to some degree as you mention depending on the circumstance. I'm not really up on this, however.
Wikipedia says:
It appears to show predominantly antagonist activity on postsynaptic D2 receptors and partial agonist activity on presynaptic D2 receptors,[53] D3,[45][54][55] and partially D4
and
Since the actions of aripiprazole differ markedly across receptor systems aripiprazole was sometimes an antagonist (e.g. at 5-HT6 and D2L), sometimes an inverse agonist (e.g. 5-HT2B), sometimes a partial agonist (e.g. D2L), and sometimes a full agonist (D3, D4). Aripiprazole was frequently found to be a partial agonist, with an intrinsic activity that could be low (D2L, 5-HT2A, 5-HT7), intermediate (5-HT1A), or high (D4, 5-HT2C). This mixture of agonist actions at D2-dopamine receptors is consistent with the hypothesis that aripiprazole has 'functionally selective' actions.[61]
Linkadge
poster:linkadge
thread:1116533
URL: http://www.dr-bob.org/babble/20210723/msgs/1116673.html