Words similar to agonist-induced
Example sentences for: agonist-induced
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There are three subtypes of the alpha-2 adrenergic receptor: alpha-2A; alpha-2B; and alpha-2C [ 15 ] . The human alpha-2A subtype undergoes phosphorylation and short-term desensitization [ 11 12 ] , whereas the human alpha-2C subtype is not phosphorylated [ 16 ] and does not desensitize [ 11 ] . The human alpha-2C subtype, however, does undergo arrestin-dependent internalization [ 17 ] . Many studies [ 11 18 ] , including those from our laboratory [ 10 19 20 ] , have demonstrated agonist-induced down-regulation of alpha-2 receptors, although much less is known about the specific mechanisms for down-regulation as compared to the beta-2 receptor.
All three alpha-2 adrenergic receptor subtypes from nearly all species that have been tested undergo agonist-induced down-regulation [ 24 25 ] . Interestingly, we have shown that the potency of norepinephrine to produce down-regulation differs among alpha-2 receptor subtypes [ 19 24 ] . The concentration of norepinephrine required to produce half-maximal down-regulation is approximately 2 μM for the alpha-2A receptor.
These findings raise two related questions: 1) can δ-opioid receptors be internalized in vivo by the same agonist-induced endocytosis observed in vitro ? and if this is the case, 2) does the internalization process have the same kinetics reported from in vitro studies?
Sequentially mutating each of the four serines to alanine decreased the phosphorylation of the receptor by approximately 25% for each serine, and mutating either the first two or the last two serines to alanines prevented agonist-induced desensitization, but not agonist-induced sequestration/internalization [ 12 ] . The influence of mutations in this motif on down-regulation has not been investigated.
The human alpha-2A adrenergic receptor has an acidic serine-rich motif (EESSSSD) in the third intracellular loop that has been shown to be important in agonist-induced desensitization but not in agonist-induced sequestration/internalization.
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